OPRK1

Summary

Gene Symbol: OPRK1
Description: opioid receptor kappa 1
Alias: K-OR-1, KOR, KOR-1, OPRK, kappa-type opioid receptor, Opiate receptor, kappa-1, kappa opioid receptor
Species: human

Top Publications

  1. ncbi Serotonergic involvement in the antinociceptive action of and the development of tolerance to the kappa-opioid receptor agonist, U-50, 488H
    B Y Ho
    Department of Pharmacology, Medical School, University of Minnesota, Minneapolis
    J Pharmacol Exp Ther 250:508-14. 1989
  2. ncbi Discriminative stimulus effects of opioids in pigeons trained to discriminate fentanyl, bremazocine and water: evidence of pharmacological selectivity
    M J Picker
    Department of Psychology, University of North Carolina at Chapel Hill 27599 3270, USA
    Behav Pharmacol 8:160-73. 1997
  3. pmc Local inhibitory effects of dynorphin A-(1-17) on capsaicin-induced thermal allodynia in rhesus monkeys
    M C Ko
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, Ann Arbor, MI 48109 0632, USA
    Eur J Pharmacol 402:69-76. 2000
  4. ncbi Dynorphin modulates ocular hydrodynamics and releases atrial natriuretic peptide via activation of kappa-Opioid receptors
    Karen R M Russell
    Morehouse School of Medicine, Atlanta, GA, 30310 1495, USA
    Exp Eye Res 75:259-70. 2002
  5. doi Possible involvement of dynorphin A release via mu1-opioid receptor on supraspinal antinociception of endomorphin-2
    Shinobu Sakurada
    Department of Physiology and Anatomy, Tohoku Pharmaceutical University, 4 4 1 Komatsushima, Sendai 981 8558, Japan
    Peptides 29:1554-60. 2008
  6. ncbi Kappa-opioid receptor agonist inhibition of HIV-1 envelope glycoprotein-mediated membrane fusion and CXCR4 expression on CD4(+) lymphocytes
    James R Lokensgard
    Neuroimmunology Laboratory, Minneapolis Medical Research Foundation, 914 South 8th Street, Bldg D 3, Minneapolis, MN 55404, USA
    Biochem Pharmacol 63:1037-41. 2002
  7. ncbi Human kappa opiate receptor second extracellular loop elevates dynorphin's affinity for human mu/kappa chimeras
    J B Wang
    Molecular Neurobiology Branch, National Institute on Drug Abuse, Baltimore, Maryland
    J Biol Chem 269:25966-9. 1994
  8. ncbi Mu-, delta- and kappa-opioid receptor populations are differentially altered in distinct areas of postmortem brains of Alzheimer's disease patients
    A M Mathieu-Kia
    The Rockefeller University, Laboratory of the Biology of Addictive Diseases, 1230 York Avenue, New York, NY 10021, USA
    Brain Res 893:121-34. 2001
  9. ncbi Endogenous opioid receptor genes and alcohol dependence among Taiwanese Han
    El Wui Loh
    National Genotyping Center at Academia Sinica, Academia Sinica, Taipei, Taiwan
    Alcohol Clin Exp Res 28:15-9. 2004
  10. ncbi Association of the kappa-opioid system with alcohol dependence
    X Xuei
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Mol Psychiatry 11:1016-24. 2006

Research Grants

  1. Charles Chavkin; Fiscal Year: 2016
  2. Jane V Aldrich; Fiscal Year: 2016
  3. Evan D Morris; Fiscal Year: 2016
  4. Novel Glycosylated Delta Opioid Receptor Agonists for Chronic Inflammatory Pain
    Mark S Kleven; Fiscal Year: 2012
  5. Yan Zhang; Fiscal Year: 2016
  6. JOHN ELLIOTT ROBINSON; Fiscal Year: 2016
  7. The Role of Kappa Opioid Receptor-induced Activation of Astrocytes in the Reinsta
    Charles Chavkin; Fiscal Year: 2009
  8. Michael R Bruchas; Fiscal Year: 2016
  9. Susan M Lunte; Fiscal Year: 2014
  10. NAIJIANG LIU; Fiscal Year: 2014

Detail Information

Publications216 found, 100 shown here

  1. ncbi Serotonergic involvement in the antinociceptive action of and the development of tolerance to the kappa-opioid receptor agonist, U-50, 488H
    B Y Ho
    Department of Pharmacology, Medical School, University of Minnesota, Minneapolis
    J Pharmacol Exp Ther 250:508-14. 1989
    ..There were no significant changes in the maximum binding values of [3H]ethylketazocine, [3H]-5-HT or [3H]ketanserin. The Kd values of all ligands increased approximately 2-fold in most of the regions.(ABSTRACT TRUNCATED AT 250 WORDS)..
  2. ncbi Discriminative stimulus effects of opioids in pigeons trained to discriminate fentanyl, bremazocine and water: evidence of pharmacological selectivity
    M J Picker
    Department of Psychology, University of North Carolina at Chapel Hill 27599 3270, USA
    Behav Pharmacol 8:160-73. 1997
    ..A series of opioids with activity at both the mu and kappa opioid receptor sites, including nalorphine, butorphanol, buprenorphine, nalbuphine, ethylketocyclazocine, (-)-..
  3. pmc Local inhibitory effects of dynorphin A-(1-17) on capsaicin-induced thermal allodynia in rhesus monkeys
    M C Ko
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, Ann Arbor, MI 48109 0632, USA
    Eur J Pharmacol 402:69-76. 2000
    ..These results suggest that in vivo opioid actions of dynorphin-related peptides can be differentiated locally in this procedure. They also indicate that local application of peptidic ligands may be a useful medication for localized pain...
  4. ncbi Dynorphin modulates ocular hydrodynamics and releases atrial natriuretic peptide via activation of kappa-Opioid receptors
    Karen R M Russell
    Morehouse School of Medicine, Atlanta, GA, 30310 1495, USA
    Exp Eye Res 75:259-70. 2002
    The present study was designed to investigate the effect of the kappa opioid receptor (KOR) agonist, dynorphin A (Dyn), on aqueous humor dynamics (intraocular pressure (IOP), aqueous humor flow rate (AFR)), pupil diameter (PD) and atrial ..
  5. doi Possible involvement of dynorphin A release via mu1-opioid receptor on supraspinal antinociception of endomorphin-2
    Shinobu Sakurada
    Department of Physiology and Anatomy, Tohoku Pharmaceutical University, 4 4 1 Komatsushima, Sendai 981 8558, Japan
    Peptides 29:1554-60. 2008
    ....
  6. ncbi Kappa-opioid receptor agonist inhibition of HIV-1 envelope glycoprotein-mediated membrane fusion and CXCR4 expression on CD4(+) lymphocytes
    James R Lokensgard
    Neuroimmunology Laboratory, Minneapolis Medical Research Foundation, 914 South 8th Street, Bldg D 3, Minneapolis, MN 55404, USA
    Biochem Pharmacol 63:1037-41. 2002
    Our previous studies have shown that the suppressive effect of kappa-opioid receptor (KOR) ligand treatment on HIV-1(AT) (a T-tropic strain) expression in acutely infected CD4(+) lymphocytes is time-dependent...
  7. ncbi Human kappa opiate receptor second extracellular loop elevates dynorphin's affinity for human mu/kappa chimeras
    J B Wang
    Molecular Neurobiology Branch, National Institute on Drug Abuse, Baltimore, Maryland
    J Biol Chem 269:25966-9. 1994
    ..These data suggest that the putative second extracellular loop contributes substantially to the kappa receptor's selectivity in dynorphin ligand recognition...
  8. ncbi Mu-, delta- and kappa-opioid receptor populations are differentially altered in distinct areas of postmortem brains of Alzheimer's disease patients
    A M Mathieu-Kia
    The Rockefeller University, Laboratory of the Biology of Addictive Diseases, 1230 York Avenue, New York, NY 10021, USA
    Brain Res 893:121-34. 2001
    ..These results may suggest an involvement of the endogenous opioid system in some of the multitude of effects that accompany this dementia...
  9. ncbi Endogenous opioid receptor genes and alcohol dependence among Taiwanese Han
    El Wui Loh
    National Genotyping Center at Academia Sinica, Academia Sinica, Taipei, Taiwan
    Alcohol Clin Exp Res 28:15-9. 2004
    ..reduce alcohol consumption under various experimental situations, and several association studies have examined possible roles of opioid receptor mu (OPRM), delta (OPRD), and kappa (OPRK) genes in the development of alcohol dependence.
  10. ncbi Association of the kappa-opioid system with alcohol dependence
    X Xuei
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Mol Psychiatry 11:1016-24. 2006
    ..We genotyped SNPs throughout OPRK1, encoding the kappa-opioid receptor, and PDYN, which encodes its ligand prodynorphin, in a group of 1860 European ..
  11. ncbi Differential helical orientations among related G protein-coupled receptors provide a novel mechanism for selectivity. Studies with salvinorin A and the kappa-opioid receptor
    Timothy A Vortherms
    Department of Biochemistry, Case Western Reserve University School of Medicine, Cleveland, Ohio 44106, USA
    J Biol Chem 282:3146-56. 2007
    ..of the hallucinogenic sage Salvia divinorum, is an apparently selective and highly potent kappa-opioid receptor (KOR) agonist...
  12. ncbi Human kappa opioid receptor gene (OPRK1) polymorphism is associated with opiate addiction
    G Gerra
    Programma Dipendenze Patologiche, Ser T, AUSL Parma, Italy
    Am J Med Genet B Neuropsychiatr Genet 144:771-5. 2007
    Variants of the opioid receptors are the obvious candidates underlying addiction. The kappa opioid receptor (KOR) system seems to play a role in stress responsivity, opiate withdrawal and responses to psycho-stimulants, inhibiting ..
  13. pmc The OPRD1 and OPRK1 loci in alcohol or drug dependence: OPRD1 variation modulates substance dependence risk
    H Zhang
    VA Connecticut Healthcare System, West Haven Campus, West Haven, CT 06516, USA
    Mol Psychiatry 13:531-43. 2008
    ..86, odds ratio (OR)=6.43) and especially on OD (P<0.001, beta=3.92, OR=50.57). Moreover, seven SNPs covering OPRK1 were examined in the majority of the above subjects (390 cases, including 327 AD, 177 CD and 97 OD subjects, and ..
  14. pmc A regulatory variation in OPRK1, the gene encoding the kappa-opioid receptor, is associated with alcohol dependence
    Howard J Edenberg
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Hum Mol Genet 17:1783-9. 2008
    Variations in OPRK1, which encodes the kappa-opioid receptor, are associated with the risk for alcohol dependence...
  15. pmc Structure of the human κ-opioid receptor in complex with JDTic
    Huixian Wu
    Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Nature 485:327-32. 2012
    ....
  16. pmc kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system
    F Simonin
    Ecole Supérieure de Biotechnologie, Parc d Innovation, Boulevard Sebastien Brandt, Illkirch Graffenstaden, France
    Proc Natl Acad Sci U S A 92:7006-10. 1995
    ..Some divergences in structural, pharmacological, and anatomical properties are noted between the cloned human and rodent receptors...
  17. pmc kappa opioid receptors in human microglia downregulate human immunodeficiency virus 1 expression
    C C Chao
    Neuroimmunobiology and Host Defense Laboratory, Minneapolis Medical Research Foundation and University of Minnesota Medical School, 55404, USA
    Proc Natl Acad Sci U S A 93:8051-6. 1996
    ..human fetal microglia and inhibition of HIV-1 expression in acutely infected microglial cell cultures treated with KOR ligands...
  18. ncbi Redefinition of the human kappa opioid receptor gene (OPRK1) structure and association of haplotypes with opiate addiction
    Vadim Yuferov
    aLaboratory of the Biology of Addictive Diseases, The Rockefeller University, New York, NY 10021, USA
    Pharmacogenetics 14:793-804. 2004
    The kappa opioid receptor (KOR) plays a role in stress responsivity, opiate withdrawal and responses to cocaine. KOR activation by its endogenous ligand dynorphin A(1-17) decreases basal and drug-induced striatal levels of dopamine...
  19. pmc Differential effects of K+ channel blockers on antinociception induced by alpha 2-adrenoceptor, GABAB and kappa-opioid receptor agonists
    M Ocana
    Department of Pharmacology, School of Medicine, University of Granada, Spain
    Br J Pharmacol 110:1049-54. 1993
    ..The K+ channels opened by alpha2-adrenoceptor agonists seem to be ATP-dependent channels, whereas those opened by GABAB receptor agonists are not...
  20. pmc Effects of the kappa-opioid agonist U50,488 on parturition in rats
    A J Douglas
    Department of Physiology, University of Edinburgh
    Br J Pharmacol 109:251-8. 1993
    ..The inhibitory effect may well have been potentiated by a direct non-opioid depressant action on contractile activity of the uterus...
  21. pmc A pharmacological profile of the novel, peripherally-selective kappa-opioid receptor agonist, EMD 61753
    A Barber
    Preclinical Pharmaceutical Research, E Merck, Darmstadt, Germany
    Br J Pharmacol 113:1317-27. 1994
    ..The inhibitory actions of systemically-applied EMD 61753 against hyperalgesic pressure nociception and neurogenic inflammation are mediated peripherally, probably by opioid receptors on the endings of sensory nerve fibres...
  22. ncbi Roles of kappa opioid receptors in cardioprotection against ischemia: the signaling mechanisms
    Tak Ming Wong
    Department of Physiology, The University of Hong Kong, 4 F, Laboratory Block, Faculty of Medicine Building, Hong Kong SAR, PR China
    Sheng Li Xue Bao 55:115-20. 2003
    There is evidence that the myocytes produce dynorphin and dynorphin-like peptides, which are kappa opioid receptor (kappa-OR) agonists...
  23. ncbi Study of the involvement of K+ channels in the peripheral antinociception of the kappa-opioid receptor agonist bremazocine
    Luiz H Amarante
    Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais UFMG, Av Antonio Carlos 6627, Belo Horizonte MG, 31 270 100, Brazil
    Eur J Pharmacol 494:155-60. 2004
    ..On the basis of these results, we suggest that K(+) channels are not involved in the peripheral antinociceptive effect of bremazocine, although this opioid receptor agonist induces nitric oxide/cGMP pathway activation...
  24. ncbi Opioid efficacy in a C6 glioma cell line stably expressing the human kappa opioid receptor
    A E Remmers
    Department of Pharmacology, University of Michigan, Ann Arbor 48109 0632, USA
    J Pharmacol Exp Ther 288:827-33. 1999
    A C6 glioma cell line stably transfected with the human kappa opioid receptor (kappaOR) was used to characterize receptor binding and G protein activation via the kappaOR by a comprehensive series of opioid ligands...
  25. ncbi Synthesis and in vitro characterization of fluorinated U-50488 analogs for PET studies of kappa opioid receptors
    P L Chesis
    Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110
    Int J Rad Appl Instrum A 41:267-73. 1990
    ..The in vitro binding affinity (Ki) of these fluorinated ligands for the kappa opioid receptor is reduced two orders of magnitude relative to U-50488...
  26. doi The effect of kappa-opioid receptor agonists on tetrodotoxin-resistant sodium channels in primary sensory neurons
    Xin Su
    Icagen, Inc, Durham, North Carolina, USA
    Anesth Analg 109:632-40. 2009
    ..In this study, we examined structurally diverse kappa-ORAs for their abilities to inhibit tetrodotoxin-resistant (TTX-r) sodium channels in adult rat DRGs...
  27. pmc Central and peripheral actions of the novel kappa-opioid receptor agonist, EMD 60400
    A Barber
    Preclinical Pharmaceutical Research, E Merck, Darmstadt, Germany
    Br J Pharmacol 111:843-51. 1994
    ..The peripheral actions of systemically-applied EMD 60400 against hyperalgesic pressure pain and neurogenic inflammation are very probably mediated by opioid receptors on the endings of sensory nerve fibres...
  28. pmc Metabolic activities of metronidazole-sensitive and -resistant strains of Helicobacter pylori: repression of pyruvate oxidoreductase and expression of isocitrate lyase activity correlate with resistance
    P S Hoffman
    Department of Microbiology and Immunology, Faculty of Medicine, Dalhousie University, Halifax, Nova Scotia, Canada
    J Bacteriol 178:4822-9. 1996
    ..All strains expressed pyruvate oxidoreductase (POR) and alpha-ketoglutarate oxidoreductase (KOR) as measured with the redox-active dye benzyl viologen (30 to 96 nmol/min/mg of protein for POR and 30 nmol/min/mg ..
  29. pmc Kappa1- and kappa2-opioid receptors mediating presynaptic inhibition of dopamine and acetylcholine release in rat neostriatum
    A N Schoffelmeer
    Research Institute Neurosciences Vrije Universiteit, Department of Pharmacology, Free University, Medical Faculty, Amsterdam, The Netherlands
    Br J Pharmacol 122:520-4. 1997
    ..As such, this study is the first to provide unequivocal in vitro evidence for the existence of functionally distinct kappa-opioid receptor subtypes in the brain...
  30. ncbi Influence of salmon calcitonin on the analgesic effect of selective kappa-opioid agonist in mice
    B Borowicz
    Department of Human Physiology, Medical University of Lublin
    Ann Univ Mariae Curie Sklodowska Med 56:407-11. 2001
    ..The obtained results suggest that the increase in the effectiveness of kappa-opioid receptor agonist may be one of the mechanisms involved in the analgesia induced by salmon calcitonin...
  31. pmc Structure, expression, and regulation of the kilC operon of promiscuous IncP alpha plasmids
    M H Larsen
    Department of Microbiology, College of Physicians and Surgeons, Columbia University, New York, New York 10032
    J Bacteriol 176:5022-32. 1994
    The kil-kor regulon was first identified on the broad-host-range IncP alpha plasmid RK2 by the presence of multiple kil loci (kilA, kilB, kilC, and recently kilE) that are lethal to Escherichia coli host cells in the absence of ..
  32. ncbi kappa-Opioid receptor agonist-induced prolactin release in primates is blocked by dopamine D(2)-like receptor agonists
    E R Butelman
    Laboratory on the Biology of Addictive Diseases, The Rockefeller University Box 171, 1230 York Avenue, New York, NY 10021, USA
    Eur J Pharmacol 423:243-9. 2001
    ....
  33. ncbi Decreased oral self-administration of alcohol in kappa-opioid receptor knock-out mice
    Krisztina M Kovacs
    Laboratory of Neurobehavioral GeneticsNathan S Kline Institute for Psychiatric Research, 140 Old Orangeburg Road, Orangeburg, NY 10962, USA
    Alcohol Clin Exp Res 29:730-8. 2005
    ..Here we examined the effects of targeted disruption of kappa-opioid receptor (KOR) on oral alcohol self-administration and other behaviors.
  34. ncbi Naloxone rapidly evokes endogenous kappa opioid receptor-mediated hyperalgesia in naïve mice pretreated briefly with GM1 ganglioside or in chronic morphine-dependent mice
    Stanley M Crain
    Department of Neuroscience, Albert Einstein College of Medicine, Yeshiva University, 1300 Morris Park Ave Bronx, NY 10461, USA
    Brain Res 1167:31-41. 2007
    ..1 ng/kg, s.c.) of the broad-spectrum opioid receptor antagonist, naltrexone or the selective kappa opioid receptor antagonist, nor-binaltorphimine, blocks naloxone-evoked hyperalgesia in GM1-pretreated naïve mice and ..
  35. pmc Influence of age and 17beta-estradiol on kisspeptin, neurokinin B, and prodynorphin gene expression in the arcuate-median eminence of female rhesus macaques
    Dominique H Eghlidi
    Division of Neuroscience, Oregon National Primate Research Center, Beaverton, Oregon 97006, USA
    Endocrinology 151:3783-94. 2010
    ..receptor 54 (encoded by GPR54), neurokinin 3 receptor (encoded by NK3), and kappa-opioid receptor (encoded by KOR), in the female rhesus macaque ARC-median eminence (ARC-ME)...
  36. ncbi Differential regulation of the human kappa opioid receptor by agonists: etorphine and levorphanol reduced dynorphin A- and U50,488H-induced internalization and phosphorylation
    Jian Guo Li
    Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    J Pharmacol Exp Ther 305:531-40. 2003
    ..U50,488H) promoted internalization and phosphorylation of the FLAG-tagged human kappa opioid receptor (FLAG-hkor) stably expressed in Chinese hamster ovary (CHO) cells...
  37. ncbi Subclass opioid receptors associated with the cardiovascular depression after traumatic shock and the antishock effects of its specific receptor antagonists
    Liang Ming Liu
    State Key Laboratory of Trauma, Burns, and Combined Injury, The Second Department of Research Institute of Surgery, Daping Hospital, The Third Military Medical University, Chongqing 400042, People s Republic of China
    Shock 24:470-5. 2005
    ..of myocardial and brain opioid receptors after traumatic shock, the antagonizing effects of mu, delta, and kappa opioid receptor antagonists on the cardiovascular depression of traumatic shock and the antishock effects of delta and ..
  38. pmc Mu and kappa opioid receptor expression in the mediobasal hypothalamus and effectiveness of selective antagonists on prolactin release during lactation
    M Tavakoli-Nezhad
    Department of Physiology, Mail Code 6523, School of Medicine, Southern Illinois University, Carbondale, IL 62901, USA
    Neuroscience 166:359-67. 2010
    ..study was to investigate effects of mu opioid receptor antagonist, beta-funaltrexamine (beta-FNA), and kappa opioid receptor antagonist, nor-binaltorphimine (nor-BNI), on prolactin secretion and TIDA neuronal activity in lactating ..
  39. doi Inhibitory and excitatory effects of micro-, delta-, and kappa-opioid receptor activation on breathing in awake turtles, Trachemys scripta
    Stephen M Johnson
    Dept of Comparative Biosciences, School of Veterinary Medicine, Univ of Wisconsin, 2015 Linden Dr, Madison, WI 53706, USA
    Am J Physiol Regul Integr Comp Physiol 295:R1599-612. 2008
    ..receptor (MOR and DOR, respectively) activation would cause respiratory depression, whereas kappa-opioid receptor (KOR) activation would have no effect...
  40. ncbi kappa-Opioid receptor effects of butorphanol in rhesus monkeys
    J A Vivian
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, USA
    J Pharmacol Exp Ther 290:259-65. 1999
    ....
  41. doi Blockade of central kappa-opioid receptors inhibits the antidipsogenic effect of interleukin-1beta
    P A Luz
    Department of Biological Sciences, State University of Southwest Bahia, 45200 000 Jequié, Bahia, Brazil
    Neuropeptides 43:93-103. 2009
    The objective of the present study was to investigate the role of brain kappa-opioid receptors (KOR) in the antidipsogenic effect promoted by third ventricle injections of interleukin-1beta (IL-1beta)...
  42. ncbi A monoclonal antibody recognizing kappa- but not mu- and delta-opioid receptors
    K Maderspach
    Institute of Biochemistry, Biological Research Center, Hungarian Academy of Sciences, Szeged
    J Neurochem 56:1897-904. 1991
    ..abstract truncated at 250 words)..
  43. ncbi Differential agonist regulation of the human kappa-opioid receptor
    A D Blake
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104, U S A
    J Neurochem 68:1846-52. 1997
    ..Taken together, these results demonstrate that the human kappa receptor is differentially regulated by selective and nonselective opioid agonists, with selective agonists able to desensitize the receptor...
  44. ncbi Nalmefene induced elevation in serum prolactin in normal human volunteers: partial kappa opioid agonist activity?
    Gavin Bart
    The Laboratory of the Biology of Addictive Diseases, The Rockefeller University, 1230 York Avenue, New York, NY 10021, USA
    Neuropsychopharmacology 30:2254-62. 2005
    ....
  45. ncbi The use of specific opioid agonists and antagonists to delineate the vagally mediated antinociceptive and cardiovascular effects of intravenous morphine
    A Randich
    Department of Psychology, University of Alabama, Birmingham 35294
    Brain Res 603:186-200. 1993
    ..The present studies used the relatively specific mu, delta, and kappa opioid receptor agonists (DAGO, DPDPE or U-50,488H) and the relatively specific mu, delta, and kappa opioid receptor ..
  46. ncbi Gastric effects of mu-, delta- and kappa-opioid receptor agonists on brainstem unitary responses in the neonatal rat
    C S Yuan
    Committee on Clinical Pharmacology, University of Chicago Medical Center, IL 60637, USA
    Eur J Pharmacol 314:27-32. 1996
    ..These results suggest that the mu- and kappa-opioid receptors of the distal stomach are important in modulation of brainstem neuronal activity and may play a role in regulating the digestive process...
  47. ncbi Dynorphin-A(1-17) decreases nitric oxide release and cytotoxicity induced with lipopolysaccharide plus interferon-gamma in murine macrophage cell line J774
    Jelka Gabrilovac
    Ruder Boskovic Institute, Division of Molecular Medicine, Laboratory of Experimental Haematology, Immunology and Oncology, Bijenicka c 54, P O Box 1016, 10000 Zagreb, Croatia
    Biomed Pharmacother 57:351-8. 2003
    ..reported in the presence of endogenous (peptide) and synthetic (non-peptide) agonists with kappa opioid-receptors (KOR) selectivity...
  48. doi An atopic dermatitis-like skin disease with hyper-IgE-emia develops in mice carrying a spontaneous recessive point mutation in the Traf3ip2 (Act1/CIKS) gene
    Yoshibumi Matsushima
    Research Institute for Clinical Oncology, Saitama Cancer Center, Saitama, Japan
    J Immunol 185:2340-9. 2010
    ..that showed high levels of serum IgE and an atopic dermatitis (AD)-like skin disease were found in a colony of the KOR inbred strain that was derived from Japanese wild mice...
  49. ncbi Endogenous opioid peptides contribute to antinociceptive potency of intrathecal [Dmt1]DALDA
    Hazel H Szeto
    Department of Pharmacology, Joan and Sanford I Weill Medical College of Cornell University, 1300 York Avenue, New York, NY 10021, USA
    J Pharmacol Exp Ther 305:696-702. 2003
    ..67 +/- 0.04 microM for delta opioid receptor (DOR), and K(i) of 4.4 +/- 1.7 nM for kappa opioid receptor (KOR), respectively...
  50. ncbi Pharmacological characterization of human kappa/mu opioid receptor chimeras that retain high affinity for dynorphin A
    Robert N DeHaven
    Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341 1129, USA
    Curr Top Med Chem 5:303-13. 2005
    ..As part of our effort to discover kappa opioid receptor analgesics lacking side effects, we designed and constructed two mu/kappa chimeric receptors, composed ..
  51. doi Effect of endothelin-A receptor antagonist on mu, delta and kappa opioid receptor-mediated antinociception in mice
    Shaifali Bhalla
    Department of Pharmaceutical Sciences, Chicago College of Pharmacy, Midwestern University, Downers Grove, IL 60515, USA
    Eur J Pharmacol 635:62-71. 2010
    ..BMS182874, with DAMGO (micro opioid receptor agonist), SNC80 (delta opioid receptor agonist), U50,488H (kappa opioid receptor agonist), and oxycodone (micro and kappa opioid receptor agonist) towards antinociception, tolerance to ..
  52. ncbi Pharmacological characterization of the ameliorating effect on short-term memory impairment and antinociceptive effect of KT-90 in mice
    Masayuki Hiramatsu
    Laboratory of Neuropsychopharmacology, Graduate School of Environmental and Human Sciences, Meijo University, Nagoya, Japan
    Behav Brain Res 160:374-81. 2005
    ....
  53. ncbi Modulation of ocular hydrodynamics and iris function by bremazocine, a kappa opioid receptor agonist
    K R Russell
    Department of Pharmacology and Toxicology, Morehouse School of Medicine, Atlanta, GA 30310 1495, USA
    Exp Eye Res 70:675-82. 2000
    This study was designed to determine the activity of bremazocine (BRE), a relatively selective kappa opioid receptor agonist, on intraocular pressure (IOP), aqueous humor formation and pupil diameter (PD) in conscious, normal, dark-..
  54. ncbi Modulation of pre- and postsynaptic dopamine D2 receptor function by the selective kappa-opioid receptor agonist U69593
    J B Acri
    Integrative Neuroscience Unit, Behavioral Neuroscience Branch, NIDA IRP, 6001 Executive Blvd Room 4123, MSC 9551, Bethesda, MD 20892 9551, USA
    Synapse 39:343-50. 2001
    ..These results suggest that both pre- and postsynaptic striatal DA D2 receptors may be downregulated following repeated kappa-opioid receptor agonist administration. Synapse 39:343-350, 2001. Published 2001 Wiley-Liss, Inc...
  55. ncbi Lack of effect of kappa-opioid receptor agonism on long-term methamphetamine-induced neurotoxicity in rats
    Kamisha L Johnson-Davis
    Department of Pharmacology and Toxicology, University of Utah, 30 South 2000 East, Rm 201, Salt Lake City, UT 84112, USA
    Neurotox Res 5:273-81. 2003
    ..These data suggest that Kappa-agonists do not protect against methamphetamine-induced toxicity to monoamines in rats, and may potentiate mortality when co-administered with methamphetamine...
  56. ncbi Bremazocine increases C-type natriuretic peptide levels in aqueous humor and enhances outflow facility
    David E Potter
    Medical University of South Carolina, Storm Eye Institute, Department of Ophthalmology, Charleston, SC 29425, USA
    J Pharmacol Exp Ther 309:548-53. 2004
    A relatively selective agonist of kappa opioid receptors (KOR), bremazocine (BRE), lowers intraocular pressure in rabbits, in part, by increasing natriuretic peptide levels in aqueous humor and by enhancing total outflow facility (TOF)...
  57. ncbi Dynorphin A, kappa opioid receptors and the antinociceptive efficacy of asimadoline in streptozotocin-induced diabetic rats
    C G Jolivalt
    Department of Pathology, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093 0612, USA
    Diabetologia 49:2775-85. 2006
    ..We investigated spinal and peripheral kappa opioid systems in diabetic rats...
  58. ncbi A select set of opioid ligands induce up-regulation by promoting the maturation and stability of the rat kappa-opioid receptor in human embryonic kidney 293 cells
    KENNETH M WANNEMACHER
    Graduate School of Biomedical Science, University of Medicine and Dentistry of New Jersey New Jersey Medical School, Newark, New Jersey, USA
    J Pharmacol Exp Ther 323:614-25. 2007
    ....
  59. ncbi Four strains of spontaneously hyperlipidemic (SHL) mice: phenotypic distinctions determined by genetic backgrounds
    Y Matsushima
    Research Institute, Saitama Cancer Center, Ina, Japan
    J Atheroscler Thromb 8:71-9. 2001
    Spontaneously hyperlipidemic (SHL) mice are Japanese wild mice (KOR) with disruption of the apolipoprotein E (Apo E) gene...
  60. pmc Glial-restricted precursors: patterns of expression of opioid receptors and relationship to human immunodeficiency virus-1 Tat and morphine susceptibility in vitro
    S K Buch
    Department of Anatomy and Neurobiology, University of Kentucky, College of Medicine, 800 Rose Street, Lexington, KY 40536 0298, USA
    Neuroscience 146:1546-54. 2007
    ..At 1 day in vitro (DIV), GRPs failed to express mu opioid receptors (MOR or MOP) or kappa-opioid receptors (KOR or KOP); however, at 5 DIV, most GRPs expressed MOR and KOR...
  61. pmc Effects of butorphanol on morphine-induced itch and analgesia in primates
    Heeseung Lee
    Department of Anesthesiology and Pain Medicine, School of Medicine, Ewha Womans University, Seoul, South Korea
    Anesthesiology 107:478-85. 2007
    Butorphanol is an opioid analgesic with partial agonist actions at micro- and kappa-opioid receptors (MOR and KOR)...
  62. doi The kappa-opioid receptor is upregulated in the spinal cord and locus ceruleus but downregulated in the dorsal root ganglia of morphine tolerant rats
    Xuan ying Li
    Department of Pain Medicine, Xuan Wu Hospital, Capital Medical University, Beijing, China
    Brain Res 1326:30-9. 2010
    As a non-selective agonist of opioid receptors, morphine can also act on the kappa-opioid receptor (KOR) when activating the mu-opioid receptor (MOR) and delta-opioid receptor (DOR)...
  63. ncbi Agonist-induced regulation and trafficking of kappa opioid receptors
    Lee Yuan Liu-Chen
    Department of Pharmacology and Center for Substance Abuse Research, Temple University, School of Medicine, Philadelphia, PA 19140, USA
    Life Sci 75:511-36. 2004
    ..focuses on agonist-induced phosphorylation, desensitization, internalization and down-regulation of the kappa opioid receptor. In vivo studies on the rat and guinea pig brains are reviewed, followed by in vitro investigations on ..
  64. ncbi U69593, a kappa-opioid agonist, decreases cocaine self-administration and decreases cocaine-produced drug-seeking
    S Schenk
    Texas A and M University, Department of Psychology, College Station 77843, USA
    Psychopharmacology (Berl) 144:339-46. 1999
    ..These agents also block the development of sensitization that occurs following repeated exposure to cocaine, which is thought to be important in the maintenance and reinstatement of compulsive drug-seeking behavior...
  65. ncbi Analysis of [3H]bremazocine binding in single and combinatorial opioid receptor knockout mice
    F Simonin
    UPR 9050 CNRS, ESBS Université Louis Pasteur, 67400 Illkirch, Strasbourg, France
    Eur J Pharmacol 414:189-95. 2001
    ..multiple mu-, delta- and kappa-opioid receptor subtypes, only three genes encoding mu-(MOR), delta-(DOR) and kappa-(KOR) opioid receptor have been cloned...
  66. ncbi Involvement of mu-, delta- and kappa-opioid receptor subtypes in the discriminative-stimulus effects of delta-9-tetrahydrocannabinol (THC) in rats
    Marcello Solinas
    Behavioral Neuroscience Research Branch, National Institute on Drug Abuse, Division of Intramural Research, National Institute of Health, Room 318, 5500 Nathan Shock Drive, Baltimore, MD, 21224, USA
    Psychopharmacology (Berl) 179:804-12. 2005
    ..Many behavioral effects of delta-9-tetrahydrocannabinol (THC), including its discriminative-stimulus effects, are modulated by endogenous opioid systems...
  67. ncbi The role of gonadal hormones on opioid receptor protein density in arthritic rats
    Matthew C Kren
    Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia 23298 0524, USA
    Eur J Pharmacol 578:177-84. 2008
    ..nociception assay, the midbrain and spinal cord tissues were collected for comparison of mu, delta, and kappa opioid receptor protein levels...
  68. doi Effects of opioid receptor activation on thermal antinociception in red-eared slider turtles (Trachemys scripta)
    Kurt K Sladky
    Department of Surgical Sciences, Center for Global Health, School of Veterinary Medicine and Public Health, University of Wisconsin, Madison, WI 53706, USA
    Am J Vet Res 70:1072-8. 2009
    To determine the effects of mu-, delta-, and kappa-opioid receptor (MOR, DOR, and KOR, respectively) activation on thermal antinociception in red-eared slider turtles Trachemys scripta.
  69. pmc Comparison of the kappa-opioid receptor antagonist DIPPA in tests of anxiety-like behavior between Wistar Kyoto and Sprague Dawley rats
    Gregory V Carr
    Department of Psychiatry, University of Pennsylvania, 125 South 31st Street, Room 2204, Philadelphia, PA, USA
    Psychopharmacology (Berl) 210:295-302. 2010
    Recent evidence suggests a role for the dynorphin/kappa-opioid receptor (KOR) system in the expression of stress-induced behaviors...
  70. ncbi Implications of Ca(2+)-activated Cl(-) channels in the delta-opioid receptor-mediated antinociception in the mouse spinal cord
    M Yamazaki
    Department of Anesthesiology, Toyama Medical and Pharmaceutical University, 2630 Sugitani, Toyama, 930 0194, Toyama, Japan
    Neurosci Lett 295:113-5. 2000
    ..The present results provide evidence for the first time that the Ca(2+)-activated Cl(-) channel is, at least in part, implicated in the delta-, but not the mu- and kappa-opioid receptor-mediated antinociception in the mouse spinal cord...
  71. ncbi TRK-820, a selective kappa-opioid agonist, produces potent antinociception in cynomolgus monkeys
    T Endoh
    Pharmaceutical Laboratories, Toray Industries Inc, Kamakura, Kanagawa, Japan
    Jpn J Pharmacol 85:282-90. 2001
    ....
  72. ncbi Social and environmental enrichment enhances sensitivity to the effects of kappa opioids: studies on antinociception, diuresis and conditioned place preference
    Mark A Smith
    Department of Psychology, Davidson College, Davidson NC 28035, USA
    Pharmacol Biochem Behav 76:93-101. 2003
    ..the effects of social and environmental enrichment on sensitivity to drugs possessing activity at the kappa opioid receptor. Rats were obtained at weaning and randomly assigned to one of two housing conditions: isolated rats were ..
  73. pmc Peripheral kappa-opioid agonists for visceral pain
    Pierre J M Riviere
    Ferring Research Institute, Building 2, Room 442, 3550 General Atomics Court, San Diego, CA 92121, U S A
    Br J Pharmacol 141:1331-4. 2004
    ..The most suitable tools to address this question in the future appear to be the newly discovered class of tetrapeptide-based kappa-agonists, which have shown unprecedented levels of peripheral selectivity...
  74. ncbi Drug design and synthesis of epsilon opioid receptor agonist: 17-(cyclopropylmethyl)-4,5alpha-epoxy-3,6beta-dihydroxy-6,14-endoethenomorphinan-7alpha-(N-methyl-N-phenethyl)carboxamide (TAN-821) inducing antinociception mediated by putative epsilon opioid
    Hideaki Fujii
    Pharmaceutical Research Laboratories, Toray Industries Inc, 1111Tebiro, Kamakura, Kanagawa 248 8555, Japan
    Bioorg Med Chem 12:4133-45. 2004
    ..1-27], but not a mu opioid receptor antagonist beta-FNA, a delta opioid receptor antagonist NTI, or a kappa opioid receptor antagonist nor-BNI...
  75. ncbi Cloning, heterologous expression and pharmacological characterization of a kappa opioid receptor from the brain of the rough-skinned newt, Taricha granulosa
    C Samuel Bradford
    Department of Zoology, 3029 Cordley Hall, Oregon State University, Corvallis, Oregon 97331, USA
    J Mol Endocrinol 34:809-23. 2005
    ..has 75% sequence identity to kappa opioid receptors cloned from mammals, and 66% sequence identity to the kappa opioid receptor reported for the zebrafish, with the greatest divergence in the extracellular N-terminus, the second and ..
  76. ncbi Kappa-opioid receptor-mediated effects of the plant-derived hallucinogen, salvinorin A, on inverted screen performance in the mouse
    William E Fantegrossi
    Division of Neuroscience, Yerkes National Primate Research Center, Emory University, Atlanta, Georgia 30322, USA
    Behav Pharmacol 16:627-33. 2005
    ..Such pharmacological differences among these kappa-opioids raise the possibility that the development of other diterpene-based opioids may yield important therapeutic compounds...
  77. ncbi Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18)
    Cecile Beguin
    Molecular Pharmacology Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 16:4679-85. 2006
    ..Our preliminary SAR study at C(18) suggested that this part of the molecule interacts with a tight lipophilic pocket of the kappa-receptor...
  78. ncbi The hallucinogenic herb Salvia divinorum and its active ingredient salvinorin A reduce inflammation-induced hypermotility in mice
    R Capasso
    Department of Experimental Pharmacology, University of Naples Federico II, Naples, Italy
    Neurogastroenterol Motil 20:142-8. 2008
    ..doses tested (3 and 10 mg kg(-1)) and this effect was not counteracted by naloxone or by the kappa-opioid receptor (KOR) antagonist nor-binaltorphimine...
  79. pmc Stress-induced p38 mitogen-activated protein kinase activation mediates kappa-opioid-dependent dysphoria
    Michael R Bruchas
    Department of Pharmacology, University of Washington, Seattle, Washington 98195 7280, USA
    J Neurosci 27:11614-23. 2007
    ..Here, we show that repeated swim stress caused activation of both kappa-opioid receptor (KOR) and p38 mitogen-activated protein kinase (MAPK) coexpressed in GABAergic neurons in the nucleus accumbens, cortex, ..
  80. doi Evidence that cardioprotection by postconditioning involves preservation of myocardial opioid content and selective opioid receptor activation
    Amanda J Zatta
    Department of Cardiothoracic Surgery, Carlyle Fraser Heart Center Crawford Long Hospital, Emory University School of Medicine, Atlanta, Georgia 30308 2225, USA
    Am J Physiol Heart Circ Physiol 294:H1444-51. 2008
    ..96 +/- 7; P < 0.05). Thus the infarct-sparing effect of postconditioning appeared to involve endogenously activated MORs and possibly DORs, and preservation of enkephalin precursor synthesis in the AAR...
  81. doi Methionine-enkephalin modulation of hydrogen peroxide (H2O2) release by rat peritoneal macrophages involves different types of opioid receptors
    Stanislava Stanojevic
    Institute of Virology, Vaccines and Sera Torlak, Immunology Research Centre Branislav Jankovic, Vojvode Stepe 458, 11152 Belgrade, Serbia
    Neuropeptides 42:147-58. 2008
    ..enhancement of H2O2 release was mediated via delta1 or delta2 opioid receptor subtypes, or by mu-kappa opioid receptor functional interactions, while MET-induced suppression involved functional interactions between delta1 and ..
  82. doi Chronic, but not acute, tricyclic antidepressant treatment alleviates neuropathic allodynia after sciatic nerve cuffing in mice
    Malika Benbouzid
    Institut des Neurosciences Cellulaires et Integratives, Département Nociception et Douleur, Centre National de la Recherche Scientifique, Universite Louis Pasteur, 21 rue René Descartes, F 67084 Strasbourg, France
    Eur J Pain 12:1008-17. 2008
    ..Our work provides a clinically relevant model to understand the mechanism by which chronic antidepressant treatment can alleviate neuropathic pain...
  83. pmc Novel pharmacology: asimadoline, a kappa-opioid agonist, and visceral sensation
    M Camilleri
    Clinical Enteric Neuroscience Translational and Epidemiological Research, Mayo Clinic, Rochester, MN 55905, USA
    Neurogastroenterol Motil 20:971-9. 2008
    ..The 1.0 mg dose was also efficacious in IBS-alternating. There were also weeks with significant reduction in bowel frequency and urgency. Asimadoline has been well tolerated in human trials to date...
  84. pmc A functional haplotype implicated in vulnerability to develop cocaine dependence is associated with reduced PDYN expression in human brain
    Vadim Yuferov
    Laboratory of the Biology of Addictive Diseases, The Rockefeller University, New York, NY 10065, USA
    Neuropsychopharmacology 34:1185-97. 2009
    ....
  85. pmc Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor
    Cecile Beguin
    Mailman Research Center, McLean Hospital, Belmont, MA 02478, USA
    Bioorg Med Chem 17:1370-80. 2009
    In an effort to find novel agents which selectively target the kappa opioid receptor (KOPR), we modified the furan ring of the highly potent and selective KOPR agonist salvinorin A...
  86. doi Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A
    Lu Yang
    Bio Organic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA
    Bioorg Med Chem Lett 19:1301-4. 2009
    ..These results suggest that electronic factors that may affect either the electron density of hydrogen bond acceptor at C-12 or hydrophobic interactions between C-12 moiety and KOPR are critical to C-12 analog's affinity for KOPR...
  87. doi The individual and combined effects of U50,488, and flurbiprofen axetil on visceral pain in conscious rats
    Takayuki Kitamura
    Department of Anesthesiology, Faculty of Medicine, The University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo, Japan 113 8655
    Anesth Analg 108:1964-6. 2009
    ....
  88. doi Effect of chronic intra-peritoneally administered chimeric peptide of met-enkephalin and FMRFa-[D-Ala2]YFa-on antinociception and opioid receptor regulation
    Ishwar Dutt Vats
    Peptide Synthesis Laboratory, Institute of Genomics and Integrative Biology, Delhi, India
    Eur J Pain 14:295.e1-9. 2010
    ..dose dependent antinociception which was mainly mediated by delta (DOR) and partially by mu (MOR) and kappa (KOR) opioid receptors...
  89. doi Myocardial apoptosis and infarction after ischemia/reperfusion are attenuated by kappa-opioid receptor agonist
    Fan Rong
    Department of Physiology, National Key Discipline of Cell Biology, Xijing Hospital, Fourth Military Medical University, Shaanxi Province, PR China
    Arch Med Res 40:227-34. 2009
    ..Therefore, the effect of U50488H on myocardial apoptosis was investigated in the present study...
  90. doi Salvinorin A inhibits colonic transit and neurogenic ion transport in mice by activating kappa-opioid and cannabinoid receptors
    J Fichna
    Division of Gastroenterology, Department of Medicine, Snyder Institute of Infection, Immunity and Inflammation III, Alberta, Canada
    Neurogastroenterol Motil 21:1326-e128. 2009
    ..receptors (KORs) and cannabinoid (CB) receptors, as they were inhibited by the antagonists nor-binaltorphimine (KOR), AM 251 (CB(1) receptor) and AM 630 (CB(2) receptor)...
  91. pmc Blockade of ethanol reward by the kappa opioid receptor agonist U50,488H
    Marian L Logrip
    The Ernest Gallo Research Center, Suite 200, Emeryville, CA 94608, USA
    Alcohol 43:359-65. 2009
    ..One putative regulatory system includes the kappa opioid receptor (KOR) and its endogenous ligand, dynorphin...
  92. pmc Endothelin-A receptor antagonism attenuates carcinoma-induced pain through opioids in mice
    Phuong N Quang
    UCSF School of Dentistry, Oral and Craniofacial Sciences Graduate Program, University of California, San Francisco, San Francisco, CA 94143 0440, USA
    J Pain 11:663-71. 2010
    ..These results demonstrate that antagonism of peripheral ET-A receptor attenuates carcinoma pain by modulating release of endogenous opioids to act on opioid receptors in the cancer microenvironment...
  93. doi A comparative study of morphine stimulation and biphalin inhibition of human glioblastoma T98G cell proliferation in vitro
    Marzena Lazarczyk
    Department of Experimental and Clinical Neuropathology, M Mossakowski Medical Research Centre, Polish Academy of Sciences, 5 Pawinskiego Str, 02 106 Warsaw, Poland
    Peptides 31:1606-12. 2010
    ..Earlier data implicating involvement of opioid receptors, particularly MOR (mu opioid receptor) and KOR (kappa opioid receptor), in cell cycle regulation prompted us to investigate the effect of biphalin and morphine on human glioma ..
  94. doi Progesterone prevents allodynia after experimental spinal cord injury
    María F Coronel
    Laboratorio de Bioquimica Neuroendocrina, Instituto de Biologia y Medicina Experimental, CONICET, Buenos Aires, Argentina
    J Pain 12:71-83. 2011
    ..N-methyl-D-aspartate receptor (NMDAR) subunits, protein kinase C gamma (PKCγ), preprodynorphin (ppD), and kappa opioid receptor (KOR), key players in chronic pain mechanisms, was determined in the dorsal spinal cord...
  95. pmc Cholesterol modulates the membrane effects and spatial organization of membrane-penetrating ligands for G-protein coupled receptors
    George Khelashvili
    Department of Physiology and Biophysics, Weill Cornell Medical College of Cornell University, New York, New York, USA
    J Phys Chem B 114:12046-57. 2010
    ..and dynamics of such a lipid-bilayer-penetrating ligand, the endogenous ligand for the κ-opioid receptor (KOR) dynorphin A (1-17) (DynA), using molecular dynamics (MD) simulations of DynA in cholesterol-depleted and ..
  96. ncbi [The study of effects and mechanism of U50, 488H on electrical coupling during ischemia in the perfused isolated rat heart]
    Hong Jiao Mao
    Department of Physiology, Shaoxing University School of Medicine, Shaoxing 312000, China
    Zhongguo Ying Yong Sheng Li Xue Za Zhi 26:261-5. 2010
    ..To determine the effect of activation of lambda-opioid receptor with U50, 488H, a selective kappa-opioid receptor agonist, on the changes in electrical coupling during prolonged ischemia and to explore the possible mechanism...
  97. doi Endogenous κ-opioid peptide mediates the cardioprotection induced by ischemic postconditioning
    Hai Tao Guo
    Department of Emergency Medicine, Xijing Hospital, Xi an 710032, China
    J Cardiovasc Pharmacol 58:207-15. 2011
    The aim of this study was to investigate the underlying mechanism that dynorphin, an endogenous kappa opioid receptor (κ-OR) agonist, triggers antiapoptotic effect of postconditioning (Postcon)...
  98. ncbi [Effects of electroacupuncture on pain reactions, expression of spinal kappa-opioid receptor and contents of enkephalin and beta-endorphin in periaqueductal gray of midbrain in dysmenorrhea model rats]
    Xiao Xuan Ren
    School of Acu Moxibustion and Tuina, Beijing University of Chinese Medicine, Beijing 100029, China
    Zhen Ci Yan Jiu 37:1-7. 2012
    ....
  99. pmc Antinociceptive effects of two deltorphins analogs in the tail-immersion test in rats
    J H Kotlinska
    Department of Pharmacology and Pharmacodynamics, Medical University, Lublin, Poland
    Peptides 39:103-10. 2013
    ..The contribution of the MOR, δ-(DOR) and κ-opioid receptors (KOR) in antinociceptive effects of the deltorphins analogs was studies using selective antagonists of these receptors...
  100. pmc Stress produces aversion and potentiates cocaine reward by releasing endogenous dynorphins in the ventral striatum to locally stimulate serotonin reuptake
    Abigail G Schindler
    Department of Pharmacology, University of Washington, School of Medicine, Seattle, Washington 98195, USA
    J Neurosci 32:17582-96. 2012
    Activation of the dynorphin/κ-opioid receptor (KOR) system by repeated stress exposure or agonist treatment produces place aversion, social avoidance, and reinstatement of extinguished cocaine place preference behaviors by stimulation ..
  101. pmc The macrocyclic tetrapeptide [D-Trp]CJ-15,208 produces short-acting κ opioid receptor antagonism in the CNS after oral administration
    Shainnel O Eans
    Torrey Pines Institute for Molecular Studies, Port St Lucie, FL, USA
    Br J Pharmacol 169:426-36. 2013
    ..We hypothesized that the macrocyclic κ opioid receptor (KOR)-selective antagonist [D-Trp]CJ-15,208 would demonstrate antagonist activity after systemic, that is, s.c...

Research Grants72

  1. Charles Chavkin; Fiscal Year: 2016
    ..advances in molecular and behavioral pharmacology suggest that novel opioid analgesics selective for the kappa opioid receptor system may provide effective pain relief without having the addiction risk common to mu-selective opioid ..
  2. Jane V Aldrich; Fiscal Year: 2016
    ..Thus there is considerable interest in identifying analgesics with reduced liabilities for clinical use. Kappa opioid receptor (KOPr) ligands have shown therapeutic value in the treatment of pain, and potential for the treatment of ..
  3. Evan D Morris; Fiscal Year: 2016
    ..The specific objective is to bring together experts to determine if Kappa opioid receptors (KOR) are affected by heavy drinking and if they have a role in mediating variability in efficacy of NTX...
  4. Novel Glycosylated Delta Opioid Receptor Agonists for Chronic Inflammatory Pain
    Mark S Kleven; Fiscal Year: 2012
    ..potency in vitro, and are at least 1000x functionally selective for DOR over MOR and kappa opioid receptors (KOR)...
  5. Yan Zhang; Fiscal Year: 2016
    ..amino acid residues in the binding pocket compared with corresponding (or conserved) loci in the delta and kappa opioid receptor antagonist binding sites...
  6. JOHN ELLIOTT ROBINSON; Fiscal Year: 2016
    ..The proposed training plan will provide a solid educational and professional foundation on which to pursue a career as a physician-scientist in the field of addiction medicine. ..
  7. The Role of Kappa Opioid Receptor-induced Activation of Astrocytes in the Reinsta
    Charles Chavkin; Fiscal Year: 2009
    ..We previously found that stress-induced dynorphin release activates kappa opioid receptors (KOR) that stimulate phosphorylation of p38 MAPK expressed by both astroglial cells and GABAergic neurons in brain...
  8. Michael R Bruchas; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): Activation of kappa opioid receptors (KOR) in humans elicits dysphoria, and KOR activation by agonists or by stress-induced dynorphin release in rodents produces reinstatement of drug seeking...
  9. Susan M Lunte; Fiscal Year: 2014
    ..Kappa opioid receptors (KOR) and their endogenous peptide agonists the dynorphins prominently modulate dopaminergic function...
  10. NAIJIANG LIU; Fiscal Year: 2014
    ..sexual dimorphic relationships among spinal ?-opioid receptors (MOR), endomorphin 2 (EM2), ?-opioid receptors (KOR) and dynorphin 1-17 (Dyn) are supported by substantial preliminary data, which is undergirded by our previous ..
  11. Analgesic Mechanism of Action of Endogenous Opioid Peptides Enkephalins with a Fo
    Gregory Scherrer; Fiscal Year: 2011
    ..composed of several peptide agonists (including enkephalins) and of the delta, kappa and mu opioid receptors (DOR, KOR and MOR, respectively)...
  12. Gregory Scherrer; Fiscal Year: 2014
    ..composed of several peptide agonists (including enkephalins) and of the delta, kappa and mu opioid receptors (DOR, KOR and MOR, respectively)...
  13. Endogenous Opioid Mechanisms Modulating Stress
    JAY MCLAUGHLIN; Fiscal Year: 2006
    ..released opioid peptide, G-protein receptor kinase phosphorylates the serine-369 residue on the kappa opioid receptor to initiate the desensitization process...
  14. William A Carlezon; Fiscal Year: 2016
    ..Its purpose is to understand how interactions of CREB and kappa-opioid receptor (KOR) systems in the nucleus accumbens shell (NAs) affect behavior in the context of mood and anxiety disorders...
  15. Charles Chavkin; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): Pharmacological activation of kappa opioid receptors (KOR) in humans elicits reports of dysphoria, and KOR activation by agonists or by stress-evoked dynorphin release in rodents produces aversion...
  16. Novel Mechanisms Underlying Depression: PET Imaging of the Kappa Opioid Receptor
    Jeffrey M Miller; Fiscal Year: 2012
    ..The kappa opioid receptor (KOR) is stimulated by the endogenous kappa opioids, dynorphins, in response to stress...
  17. Elena H Chartoff; Fiscal Year: 2014
    ..If gonadectomy abolishes the sex difference in the depressive-like effects of KOR activation, then it is likely that activational effects of gonadal steroid hormones are required...
  18. THOMAS EDWARD PRISINZANO; Fiscal Year: 2016
    ..of this proposal is that structural modification of salvinorin A will lead to identification of novel kappa opioid receptor ligands with the potential to treat drug dependence and its relapse...
  19. Cellular mechanisms underlying kappa opioid regulation of stress responses
    Julia C Lemos; Fiscal Year: 2010
    ..Using animal models, recent studies have posited a role for the dynorphin- kappa opioid receptor (KOR) neuropeptide system in mediating the aversive and pro-depressive components of repeated stress...
  20. John R Traynor; Fiscal Year: 2016
    ..Efficacy as treatment agents will come from the compounds kappa opioid receptor antagonist activity, coupled with agonism at NOP (nociceptin) receptors...
  21. Dopaminergic Mechanisms of Kappa Opioid Receptor-Induced Potentiation of Cocaine
    Jonathan M Ehrich; Fiscal Year: 2012
    DESCRIPTION (provided by applicant): Pharmacological activation of kappa opioid receptors (KOR) in humans elicits reports of dysphoria, and KOR activation by agonists or by stress-evoked dynorphin release in rodents produces aversion...
  22. Kappa-opioid Receptor Modulation of the Stress Response
    Richard M Gustin; Fiscal Year: 2012
    ..Pretreatment with kappa opioid receptor antagonists or genetic disruption of the dynorphin/? -opioid receptor system (Dyn/KOR) effectively ..
  23. Delta-kappa opioid receptor interactions: Ligand-dependent effects
    KELLY ANN BERG; Fiscal Year: 2010
    ..data suggest that the affinity and/or efficacy of DOR agonists can be regulated by the k opioid receptor (KOR) antagonist, nor-BNI...
  24. SARAH ELIZABETH ROSS; Fiscal Year: 2016
    ..This finding is important because dynorphin is a kappa opioid receptor (KOR) agonist, and KOR agonists have recently been shown to relieve itch in rodents and man...
  25. Brendan M Walker; Fiscal Year: 2016
    ..The hypothesis will be tested by pursuing the following specific aims: Aim #1 will evaluate kappa opioid receptor antagonism within specific sites of the extended amygdala during acute withdrawal...
  26. Opioid and Noradrenergic Mechanisms in Stress and Drug Seeking
    Michael R Bruchas; Fiscal Year: 2013
    ..Specifically, it concerns Kappa opioid receptor (KOR) signaling and noradrenergic mechanims in stress and drug seeking...
  27. Charles Chavkin; Fiscal Year: 2015
    ..Second, that kappa opioid receptor activation of p38 MAPK initiates signaling events responsible for the dysphoric and anxiogenic effects of ..
  28. Ontogenetic changes in ethanol's motivational properties: Involvement of the kapp
    Michael E Nizhnikov; Fiscal Year: 2010
    ..The endogenous dynorphin/kappa opioid receptor system is of great interest due to its possible involvement in diminishing ethanol intake through ..
  29. Jane V Aldrich; Fiscal Year: 2016
    ..Notably, activation of kappa opioid receptors (KOR) inhibits dopamine signaling, and thus may counteract the effects of cocaine...
  30. Irwin Lucki; Fiscal Year: 2016
    ..As a mu-opioid receptor (MOR) partial agonist and kappa-opioid receptor (KOR) antagonist, buprenorphine has been studied extensively in models of drug reward, physical dependence, and ..
  31. Kappa Opioid Receptor Activation Underlies Compulsive Methamphetamine Intake
    TIMOTHY WAYNE WHITFIELD; Fiscal Year: 2013
    ..Kitamura et. al, 2006, Wee et. al, 2007, Wee et. al, unpublished results). The kappa opioid receptor (KOR) and its ligand, prodynorphin, are known to be involved in the central nervous system effects of ..
  32. Sukhbir S Mokha; Fiscal Year: 2014
    ..We will test the hypothesis that estrogen differentially regulates the antinociceptive function of KOR and ORL1 receptors via both genomic mechanisms, involving transcription of receptors and signaling machinery, as ..
  33. Alexander Neumeister; Fiscal Year: 2014
    ..weight matched controls (HCs) to participate in a PET study using a novel PET tracer for the Kappa-opioid receptor (KOR). Subjects will complete laboratory measures of food avoidance and a food-reward based reversal learning task...
  34. Behavioral Pharmacology of Itch
    Mei Chuan Ko; Fiscal Year: 2013
    ..other experimental itch models using different pruritogenic agents and to determine the effectiveness of kappa opioid receptor agonists as antipruritics in a broader context in behaving monkeys...
  35. Role of opioid receptors in transmission of itch by spinothalamic tract neuron
    HANNAH ROSE MOSER; Fiscal Year: 2013
    ..will test the hypothesis that MOR agonists which cause itch excite STT neurons which carry itch information, while KOR agonists which have been used to treat itch inhibit these same neurons...
  36. Central Kappa Opioid Neural Regulation of Cardiovascular and Renal Function
    Helmut B Gottlieb; Fiscal Year: 2012
    ..Western Blot analysis will determine the kappa opioid receptor and peptide protein levels in these regions...
  37. Control of Nociception in the Spinal Cord
    Sukhbir S Mokha; Fiscal Year: 2010
    ..The present proposal is, therefore, designed to test the hypotheses that (!) selective activation of the kappa opioid receptor (KOR) in the dorsal horn of the spinal cord produces enhanced antinociception in the female as compared to ..
  38. Sex differences in mesolimbic dopamine responses to social stress
    Brian C Trainor; Fiscal Year: 2013
    ..Kappa opioid receptors (KOR) function at the intersection of stress and depression-like behavior because they are activated during stress and ..
  39. Sammanda Ramamoorthy; Fiscal Year: 2014
    ..opioid receptors (KOR) are enriched in brain circuits that subserve mood and motivation and regulate the basal activity of DA neurons ..
  40. RESEARCH PROJECT 1
    James L Howard; Fiscal Year: 2011
    During the last few years, we have been conducting research directed toward the development of selective kappa opioid receptor antagonists. The major overall goal was to discover and develop pharmacotherapies to treat cocaine relapse...
  41. Characterization of the Response to the Kappa Opiate Agonist Salvinorin A in Heal
    Mohini Ranganathan; Fiscal Year: 2012
    ..SA is unique in being a highly selective agonist solely at the kappa opioid receptor (KOR) and presumably produces its psychotomimetic effects by agonism at this receptor...
  42. PACAP signaling in stress and anxiety
    William A Carlezon; Fiscal Year: 2012
    ..highly selective for PACAP (PAC1) receptors but not previously tested in stress studies, and kappa-opioid receptor (KOR) antagonists, which have been shown to block the long-term effects of stress...
  43. Role of dopamine signaling in the mood-related effects of salvinorin A
    Elena H Chartoff; Fiscal Year: 2013
    ..is the main active ingredient of the hallucinogenic plant Salvia divinorum and is a potent and selective kappa opioid receptor (KOR) agonist (Roth et al., 2002)...
  44. Analytical Methods for Investigating Peptide Transport
    SUSAN LUNTE; Fiscal Year: 2007
    ..Dyn A is a natural ligand of the kappa opioid receptor. Analogs of dynorphin and its metabolites have been investigated for the treatment of peripheral pain, ..
  45. William A Carlezon; Fiscal Year: 2016
    ..VPAC1) receptors, neither of which has been previously tested in stress studies, as well as kappa-opioid receptor (KOR) antagonists, which have been shown to block stress effects...
  46. YIYUN HENRY HUANG; Fiscal Year: 2014
    ..The availability of validated PET imaging agents will provide non-invasive biomarker to investigate the KOR and gain insights into the function and dysfunction of this receptor in these disorders...
  47. Studies of mouse kappa opioid receptor gene regulation
    Li na Wei; Fiscal Year: 2011
    ..of this project is to understand "when, where, and how much" of opioid receptor protein, specifically the kappaOR (KOR), is expressed in neurons under a physiological condition, and how is it regulated...
  48. Kappa opioid antagonists: synthesis, potency, selectivity, and time-course
    William A Carlezon; Fiscal Year: 2011
    ..The kappa opioid receptor (KOR) has recently been validated as a highly promising target for this purpose...
  49. Kappa Opioid Regulation of Ethanol Withdrawal and
    Glenn R Valdez; Fiscal Year: 2010
    ..in the regulation of stress-related behavior, using the elevated plus maze model of anxiety in rats, via kappa opioid receptor activation and exposure to external stressors...
  50. Laura M Bohn; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): We are proposing to develop new kappa opioid receptor (KOR) targeted drugs for the treatment of drug addiction...
  51. Novel agonist tracers for PET imaging of kappa opioid receptors
    YIYUN HENRY HUANG; Fiscal Year: 2012
    ..The availability of PET imaging agents will provide non-invasive biomarkers to interrogate the KOR and gain insights into the function and dysfunction of this receptor system in the aforementioned disorders...
  52. YIYUN HENRY HUANG; Fiscal Year: 2015
    ..The availability of PET imaging agents will provide non-invasive biomarkers to interrogate the KOR and gain insights into the function and dysfunction of this receptor system in the aforementioned disorders...
  53. Pawhuskins: Potential Treatments for Stimulant Abuse.
    Jeffrey D Neighbors; Fiscal Year: 2010
    ..Novel therapeutics that could help with the relapse effect or otherwise improve treatment outcomes should be of high priority. ..
  54. Buprenorphine effects on oligodendrocyte development and axonal growth
    Carmen Sato Bigbee; Fiscal Year: 2010
    ..Clear understanding of these effects is crucial to the design and management strategies for pregnant opioid addicts minimizing harmful effects in the maturing CNS. ..
  55. DYNORPHIN ANALOGS AS KAPPA OPIOID RECEPTOR ANTAGONISTS
    Andrew Coop; Fiscal Year: 2000
    ..Such derivatives could be valuable pharmacological tools in increasing our understanding of how opioid ligands interact with their receptors at a molecular level. ..
  56. Opioid and Noradrenergic Mechanisms in Stress and Drug Seeking
    Michael R Bruchas; Fiscal Year: 2010
    ..The research training proposal concerns Kappa opioid receptor (KOR) signaling and noradrenergic mechanisms in stress and drug seeking...
  57. Prefrontal control of kappa-opioid receptor mediated stress-induced relapse.
    Peter A Groblewski; Fiscal Year: 2013
    ..Interestingly, the DRN possesses a number of direct inputs from KOR-expressing regions of the prefrontal cortex (PFC)-an area previously found to play an important role in stress and ..
  58. Heroin withdrawal: modulation of aversive states by kappa opioid receptors
    KATHARINE M CAMMACK; Fiscal Year: 2013
    ..Ultimately, this research will broaden our understanding of how endogenous opioid-receptor systems may be modulated as an approach to addiction therapy. ..
  59. MONICA G RIVERA-MINDT; Fiscal Year: 2016
    ..Buprenorphine, a partial mu opioid receptor agonist and kappa opioid receptor antagonist, may have favorable NC effects compared to methadone...
  60. Selectively Targeting Opioid Receptor Heterodimers
    Jennifer L Whistler; Fiscal Year: 2012
    ..system is comprised of three highly related receptors: the mu, delta, and kappa opioid receptors (MOR, DOR, and KOR respectively)...
  61. Role of corticostriatal dopamine signaling in response strategy selection.
    Jacqueline M Barker; Fiscal Year: 2012
    ..Additionally, we expect that enhanced kappa opioid receptor activity in the dorsolateral striatum will promote goal-directed behavior by decreasing dopamine signaling ..
  62. Bryan L Roth; Fiscal Year: 2014
    ..In 2002, my lab discovered that salvinorin A potently and specifically targets ?-opioid receptors (KOR) (Roth et al., PNAS 2002);these findings have been widely replicated...
  63. OPIOID RECEPTOR SPECIFIC PEPTIDES
    Victor Hruby; Fiscal Year: 1999
    ..vitro and in vivo pharmacological, biochemical and physiological studies including use of the cloned human kappa opioid receptor(s)...
  64. Opioid mediation of stress-potentiated cocaine response
    Charles Chavkin; Fiscal Year: 2007
    ..The application is based on the hypothesis that kappa opioid receptor activation by repeated stress induces release of endogenous dynorphin peptides that underlie a significant ..
  65. REGULATION OF KAPPA OPIOID RECEPTORS
    Lee Yuan Liu Chen; Fiscal Year: 2002
    ..The following are the hypotheses for proposed studies. Following chronic exposure to an agonist, the human KOR undergoes desensitization, sequestration and down-regulation...
  66. Mu Opioid Receptor Regulation in Neonatal Brainstem
    GEORGE OLSEN; Fiscal Year: 2006
    ..Guinea pig kappa opioid receptor has been cloned, but only partial sequences of MOR and delta opioid receptors have been available...
  67. K OPIOIDS AND DOPAMINE--MECHANISMS OF STIMULANT ABUSE
    Sari Izenwasser; Fiscal Year: 2001
    ..Hence, the ability to regulate dopaminergic transmission via alterations of the dopamine transporter would be useful in the treatment of such syndromes. ..
  68. Cocaine behavior: Regulation by k-opioids and serotonin
    Sari Izenwasser; Fiscal Year: 2009
    ..abstract_text> ..
  69. Opioid Binding to U51: A Human herpes Virus Protein
    Jean Bidlack; Fiscal Year: 2002
    ..identified as an opioid receptor homologue, sharing greater than 50 percent sequence similarity with the Kappa opioid receptor. HHV-6 and -7 U51 share greater sequence similarity with the Kappa, mu and delta opioid receptors than ..
  70. PHYSIOLOGY AND PHARMACOLOGY OF OPIOIDS IN BRAIN
    EDWARD FRENCH; Fiscal Year: 2001
    ....
  71. MOLECULAR STUDIES OF A KAPPA OPIOID RECEPTOR
    David Grandy; Fiscal Year: 2000
    ..Having demonstrated that R21 encodes a rat kappa opioid receptor, we are now ready to proceed with the molecular studies of this receptor...
  72. Control of Nociception in the Spinal Cord
    SUKHBIR MOKHA; Fiscal Year: 2007
    ..present application is, therefore, designed to test the hypotheses that (1) selective activation of the kappa opioid receptor (KOR) in the dorsal horn of the spinal cord produces enhanced antinociception in the female as compared to ..