benzeneacetamides

Summary

Summary: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.

Top Publications

  1. ncbi The novel squamosamide derivative FLZ protects against 6-hydroxydopamine-induced apoptosis through inhibition of related signal transduction in SH-SY5Y cells
    Dan Zhang
    Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    Eur J Pharmacol 561:1-6. 2007
  2. ncbi Small molecule-based reversible reprogramming of cellular lifespan
    Jaejoon Won
    Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon 305 701, Korea
    Nat Chem Biol 2:369-74. 2006
  3. pmc Squamosamide derivative FLZ protects dopaminergic neurons against inflammation-mediated neurodegeneration through the inhibition of NADPH oxidase activity
    Dan Zhang
    Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, NC 27709, USA
    J Neuroinflammation 5:21. 2008
  4. ncbi Piragliatin (RO4389620), a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus: a mechanistic study
    Riccardo C Bonadonna
    Division of Endocrinology and Metabolism, Department of Medicine, University of Verona School of Medicine, Verona, Italy
    J Clin Endocrinol Metab 95:5028-36. 2010
  5. ncbi A novel cyclic squamosamide analogue compound FLZ improves memory impairment in artificial senescence mice induced by chronic injection of D-galactose and NaNO2
    Fang Fang
    Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, China
    Basic Clin Pharmacol Toxicol 101:447-54. 2007
  6. ncbi Ocular permeation and inhibition of retinal inflammation: an examination of data and expert opinion on the clinical utility of nepafenac
    Richard Lindstrom
    Minnesota Eye Consultants, Minneapolis, MN 55904, USA
    Curr Med Res Opin 22:397-404. 2006
  7. ncbi Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2
    Taeweon Lee
    Amgen Inc, South San Francisco, California 94080, USA
    Mol Pharmacol 74:1599-609. 2008
  8. ncbi A natural squamosamide derivative FLZ reduces amyloid-beta production by increasing non-amyloidogenic AbetaPP processing
    Yan Hou
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USA
    J Alzheimers Dis 18:153-65. 2009
  9. ncbi Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy
    Elvira Crescenzi
    Dipartimento di Biologia e Patologia Cellulare e Molecolare L Califano, Universita di Napoli Federico II, Naples, Italy
    Clin Cancer Res 14:1877-87. 2008
  10. ncbi The novel squamosamide derivative (compound FLZ) attenuated 1-methyl, 4-phenyl-pyridinium ion (MPP+)-induced apoptosis and alternations of related signal transduction in SH-SY5Y cells
    Dan Zhang
    Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, China
    Neuropharmacology 52:423-9. 2007

Detail Information

Publications172 found, 100 shown here

  1. ncbi The novel squamosamide derivative FLZ protects against 6-hydroxydopamine-induced apoptosis through inhibition of related signal transduction in SH-SY5Y cells
    Dan Zhang
    Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    Eur J Pharmacol 561:1-6. 2007
    ..The results suggested that FLZ has potential neuroprotective effect on 6-OHDA-induced apoptosis of SH-SY5Y cells through regulating related signal-transduction...
  2. ncbi Small molecule-based reversible reprogramming of cellular lifespan
    Jaejoon Won
    Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon 305 701, Korea
    Nat Chem Biol 2:369-74. 2006
    ..These results might reflect the specific targeting of the kinase activities of ATM and ATR by CGK733 without affecting any other domains required for cell proliferation...
  3. pmc Squamosamide derivative FLZ protects dopaminergic neurons against inflammation-mediated neurodegeneration through the inhibition of NADPH oxidase activity
    Dan Zhang
    Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, NC 27709, USA
    J Neuroinflammation 5:21. 2008
    ..Hence, prevention of microglial over-activation has been shown to be a prime target for the development of therapeutic agents for inflammation-mediated neurodegenerative diseases...
  4. ncbi Piragliatin (RO4389620), a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus: a mechanistic study
    Riccardo C Bonadonna
    Division of Endocrinology and Metabolism, Department of Medicine, University of Verona School of Medicine, Verona, Italy
    J Clin Endocrinol Metab 95:5028-36. 2010
    ..Glucokinase plays a key role in glucose homeostasis. Glucokinase activators can lower glucose levels in both animal and human type 2 diabetes, but their mechanism of action has never been explored in humans...
  5. ncbi A novel cyclic squamosamide analogue compound FLZ improves memory impairment in artificial senescence mice induced by chronic injection of D-galactose and NaNO2
    Fang Fang
    Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, China
    Basic Clin Pharmacol Toxicol 101:447-54. 2007
    ....
  6. ncbi Ocular permeation and inhibition of retinal inflammation: an examination of data and expert opinion on the clinical utility of nepafenac
    Richard Lindstrom
    Minnesota Eye Consultants, Minneapolis, MN 55904, USA
    Curr Med Res Opin 22:397-404. 2006
    ..Preclinical data suggest nepafenac may also provide unique efficacy in the posterior segment...
  7. ncbi Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2
    Taeweon Lee
    Amgen Inc, South San Francisco, California 94080, USA
    Mol Pharmacol 74:1599-609. 2008
    ....
  8. ncbi A natural squamosamide derivative FLZ reduces amyloid-beta production by increasing non-amyloidogenic AbetaPP processing
    Yan Hou
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USA
    J Alzheimers Dis 18:153-65. 2009
    ..These findings suggest that FLZ reduces Abeta production by promoting AbetaPP non-amyloidogenic alpha-secretase processing. As such, FLZ may have therapeutic potential for the treatment of AD...
  9. ncbi Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy
    Elvira Crescenzi
    Dipartimento di Biologia e Patologia Cellulare e Molecolare L Califano, Universita di Napoli Federico II, Naples, Italy
    Clin Cancer Res 14:1877-87. 2008
    ..We set out to find a means to specifically induce senescent tumor cells to undergo cell death and not to reenter the cell cycle that may have general application in cancer therapy...
  10. ncbi The novel squamosamide derivative (compound FLZ) attenuated 1-methyl, 4-phenyl-pyridinium ion (MPP+)-induced apoptosis and alternations of related signal transduction in SH-SY5Y cells
    Dan Zhang
    Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, China
    Neuropharmacology 52:423-9. 2007
    ..The results suggest that cFLZ possesses potent neuroprotective activity and may be a potential anti-Parkinson's disease drug worthy for further study...
  11. ncbi [Synthesis and antioxiactivity of squamosamide cyclic analogs]
    Ping Xie
    Department of Drug Synthesis, Institute of Materia Medica, CAMS and PUMC, Beijing 100050, China
    Zhongguo Yi Xue Ke Xue Yuan Xue Bao 26:372-8. 2004
    ..To design and synthesize a series of squamosamide cyclic analogues and to test their antioxidation activity...
  12. ncbi Protective effects of compound FLZ on beta-amyloid peptide-(25-35)-induced mouse hippocampal injury and learning and memory impairment
    Fang Fang
    Department of Pharmacology, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China
    Acta Pharmacol Sin 27:651-8. 2006
    ..To study the protective effects of compound FLZ, a novel synthetic analogue of natural squamosamide, on learning and memory impairment and lesions of the hippocampus caused by icv injection of beta-amyloid(25-35)(Abeta(25-35)) in mice...
  13. ncbi Pharmacological study of the novel compound FLZ against experimental Parkinson's models and its active mechanism
    Weihong Feng
    Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China
    Mol Neurobiol 31:295-300. 2005
    ..Additionally, FLZ inhibited cytochrome-c release from mitochondria and caspase-3 activation by dopamine in PC-12 cells. The above results suggest that compound FLZ possesses anti-PD activity through neuroprotection...
  14. ncbi Novel squamosamide derivative (compound FLZ) attenuates Abeta25-35-induced toxicity in SH-SY5Y cells
    Fang Fang
    Department of Pharmacology, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China
    Acta Pharmacol Sin 29:152-60. 2008
    ....
  15. ncbi Region-dependent G-protein activation by kappa-opioid receptor agonists in the mouse brain
    Hirokazu Mizoguchi
    Department of Anesthesiology, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226, USA
    Neurosci Lett 356:145-7. 2004
    ..The present results suggest that the catalytic efficiency of kappa-opioid receptor-G-protein coupling may be variable in different brain regions...
  16. ncbi delta-opioid receptor-mediated actions on rostral ventromedial medulla neurons
    S Marinelli
    Pain Management Research Institute, Kolling Institute, Northern Clinical School, University of Sydney, Sydney, NSW 2006, Australia
    Neuroscience 132:239-44. 2005
  17. ncbi Both kappa and mu opioid agonists inhibit glutamatergic input to ventral tegmental area neurons
    Elyssa B Margolis
    Ernest Gallo Clinic and Research Center, 5858 Horton St, Suite 200, Emeryville, CA 94608, USA
    J Neurophysiol 93:3086-93. 2005
    ..These findings show that MOP-R and KOP-R agonists regulate excitatory input onto each VTA cell type...
  18. ncbi Differential time course of effects of kappa-opioid agonist treatment on dynorphin A levels and kappa-opioid receptor density
    Claudio D'Addario
    Department of Pharmacology, University of Bologna, 40126 Bologna, Italy
    J Mol Neurosci 24:307-14. 2004
    ..These findings suggest that kappa-opioid receptor agonist treatment has long-term, continually changing effects on the kappa-opioid system...
  19. ncbi Discriminative stimulus effects of acute morphine followed by naltrexone in the squirrel monkey
    David A White
    Department of Pharmacology, Emory University School of Medicine, Rollins Research Center, 1510 Clifton Road NE, Suite 5074, Atlanta, GA 30322, USA
    Psychopharmacology (Berl) 167:203-10. 2003
    ..The discriminative stimulus effects of a combination of acute morphine followed by naltrexone have been described in rats. OBJECTIVE. The purpose of this study was to extend observations to a non-human primate...
  20. ncbi Kappa opioid receptor activation in the nucleus accumbens inhibits glutamate and GABA release through different mechanisms
    Gregory O Hjelmstad
    Department of Neurology, Ernest Gallo Clinic and Research Center, Emeryville, California 94143, USA
    J Neurophysiol 89:2389-95. 2003
    ..These results indicate that KOP receptor activation inhibits GABA release by reducing Ca(2+) influx, but inhibits glutamate release at a step downstream of Ca(2+) entry...
  21. ncbi Presynaptic mechanism for anti-analgesic and anti-hyperalgesic actions of kappa-opioid receptors
    Bihua Bie
    Department of Symptom Research, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
    J Neurosci 23:7262-8. 2003
    ....
  22. ncbi DPI-3290 [(+)-3-((alpha-R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide]. I. A mixed opioid agonist with potent antinociceptive activity
    Peter J Gengo
    Ardent Pharmaceuticals, Inc, 631 United Dr, Suite 200, Durham, NC 27713, USA
    J Pharmacol Exp Ther 307:1221-6. 2003
    ..The marked antinociceptive activity of DPI-3290 will likely provide a means for relieving severe pain in patients that require analgesic treatment...
  23. ncbi Activation of mu opioid receptors in the ventrolateral periaqueductal gray inhibits reflex micturition in anesthetized rats
    Seiji Matsumoto
    Department of Basic and Pharmaceutical Sciences, Albany College of Pharmacy, Union University, 106 New Scotland Avenue, Albany, NY 12208 3492, USA
    Neurosci Lett 363:116-9. 2004
    ..These data support the hypothesis that mu and kappa receptors in the vlPAG participate in the micturition reflex...
  24. pmc A single cocaine exposure enhances both opioid reward and aversion through a ventral tegmental area-dependent mechanism
    Joseph A Kim
    Ernest Gallo Clinic and Research Center, Wheeler Center for the Neurobiology of Addiction and Department of Neurology, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 101:5664-9. 2004
    ..Thus, through a circuit involving the ventral tegmental area, a single cocaine exposure enhanced both micro-opioid receptor reward and kappa-opioid receptor aversion...
  25. ncbi Opioid interactions in rhesus monkeys: effects of delta + mu and delta + kappa agonists on schedule-controlled responding and thermal nociception
    Glenn W Stevenson
    Alcohol and Drug Abuse Research Center, Harvard Medical School, McLean Hospital, 115 Mill St, Belmont, MA 02478 9106, USA
    J Pharmacol Exp Ther 307:1054-64. 2003
    ..These results also confirm that opioid agonist interactions may depend on the receptor selectivity and relative doses of the agonists and on the experimental endpoint...
  26. ncbi Kappa-opioid agonists directly inhibit midbrain dopaminergic neurons
    Elyssa B Margolis
    Joint University of California San Francisco University of California, Berkeley Bioengineering Graduate Group, San Francisco, California 94143 0775, USA
    J Neurosci 23:9981-6. 2003
    ..These results provide a cellular mechanism for the opposing behavioral effects of KOR and MOR agonists and shed light on how KORs might regulate the motivational effects of both natural rewards and addictive drugs...
  27. ncbi Peripheral selectivity and apparent efficacy of dynorphins: comparison to non-peptidic kappa-opioid agonists in rhesus monkeys
    Eduardo R Butelman
    Laboratory on the Biology of Addictive Diseases, Rockefeller University Box 171, 1230 York Avenue, New York, NY 10021, USA
    Psychoneuroendocrinology 29:307-26. 2004
    ..0032 mg/kg, s.c. and i.v., respectively). Overall, these findings are consistent with the hypothesis that the dynorphins act as high efficacy, peripherally selective kappa-agonists following systemic administration in primates...
  28. ncbi Naloxone and its quaternary derivative, naloxone methiodide, have differing affinities for mu, delta, and kappa opioid receptors in mouse brain homogenates
    Tanya Lewanowitsch
    Department of Clinical and Experimental Pharmacology, 5th Floor, Medical School North, University of Adelaide, South Australia 5005, Adelaide, Australia
    Brain Res 964:302-5. 2003
    ..Therefore, naloxone methiodide does have a lower affinity for opioid receptors than naloxone in mouse brain tissue, which must be taken into consideration in experimental designs...
  29. pmc Mu and kappa opioid receptors activate ERK/MAPK via different protein kinase C isoforms and secondary messengers in astrocytes
    Mariana M Belcheva
    E A Doisy Department of Biochemistry and Molecular Biology, St Louis University School of Medicine, St Louis, Missouri 63104, USA
    J Biol Chem 280:27662-9. 2005
    ..Collectively, our findings on acute opioid effects suggest that differences in their mechanism of signaling may contribute to the distinct outcomes on ERK modulation induced by chronic mu and kappa opioids...
  30. 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
    ....
  31. pmc Opioid regulation of spinal cord plasticity: evidence the kappa-2 opioid receptor agonist GR89696 inhibits learning within the rat spinal cord
    Stephanie N Washburn
    Texas A and M University, Psychology Department, Mailstop 4235, College Station, TX 77843 4235, USA
    Neurobiol Learn Mem 89:1-16. 2008
    ..The results suggest that a kappa-2 opioid agonist inhibits neural modifications within the spinal cord...
  32. ncbi N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacy
    Cecile Beguin
    Department of Psychiatry, McLean Hospital, MRC 322A, 115 Mill Street, Belmont, MA 02478, USA
    J Pharmacol Exp Ther 324:188-95. 2008
    ....
  33. 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
    ....
  34. ncbi The hallucinogen derived from Salvia divinorum, salvinorin A, has kappa-opioid agonist discriminative stimulus effects in rats
    Catherine B Willmore-Fordham
    Ohio Northern University, Department of Pharmaceutical and Biomedical Sciences, Raabe College of Pharmacy, 525 S Main Street, Ada, OH 45810, USA
    Neuropharmacology 53:481-6. 2007
    ..The discussion section of this article highlights public concern over salvinorin A misuse and emphasizes several potential pharmacotherapeutic applications for salvinorin A or analogue compounds...
  35. ncbi Cotreatment with the kappa opioid agonist U69593 enhances locomotor sensitization to the D2/D3 dopamine agonist quinpirole and alters dopamine D2 receptor and prodynorphin mRNA expression in rats
    Melissa L Perreault
    Department of Psychiatry and Behavioural Neurosciences, Health Science Centre, Room 4N7, McMaster University, Hamilton, ON, Canada
    Psychopharmacology (Berl) 194:485-96. 2007
    ..Behavioral evidence has implicated both pre- and postsynaptic changes as being involved in this augmentation...
  36. ncbi Increased locomotor response to amphetamine induced by the repeated administration of the selective kappa-opioid receptor agonist U-69593
    José Antonio Fuentealba
    Department of Pharmacy, Faculty of Chemistry, Pontificia Universidad Catolica de Chile, Alameda, Santiago, Chile
    Synapse 61:771-7. 2007
    ..These results suggest that long-term effect of KOR activation results in facilitation of amphetamine-induced DA extracellular levels in the NAc accompanied by sensitization of amphetamine-induced increase in locomotor activity...
  37. pmc Acute amphetamine exposure selectively desensitizes kappa-opioid receptors in the nucleus accumbens
    Yan fang Xia
    Ernest Gallo Clinic and Research Center, University of California, San Francisco, CA 94608, USA
    Neuropsychopharmacology 33:892-900. 2008
    ..This study demonstrates that amphetamine can produce regionally selective adaptations in KOP receptor signaling, which may, in turn, alter the effects of subsequent drug exposure...
  38. ncbi The kappa-opioid receptor agonist U-69593 prevents cocaine-induced phosphorylation of DARPP-32 at Thr(34) in the rat brain
    Manuela Di Benedetto
    Department of Pharmacology, University of Bologna, Irnerio 48, Bologna 40126, Italy
    Brain Res Bull 73:34-9. 2007
    ..These data could be considered consistent with the ability of kappa opioid agonists to attenuate many behavioural and neurochemical effects of cocaine...
  39. ncbi Sensitivity of the five-choice serial reaction time task to the effects of various psychotropic drugs in Sprague-Dawley rats
    Tracie A Paine
    Behavioral Genetics Laboratory, Department of Psychiatry, Harvard Medical School, McLean Hospital, 115 Mill Street, Belmont, MA 02478, USA
    Biol Psychiatry 62:687-93. 2007
    ..The five-choice serial reaction time task (5CSRTT) is one such model. Here, we characterized the effects of four standard psychotropic agents on performance in the 5CSRTT...
  40. ncbi Pharmacological and genetic manipulation of kappa opioid receptors: effects on cocaine- and pentylenetetrazol-induced convulsions and seizure kindling
    Rafal M Kaminski
    Integrative Neuroscience Section, Behavioral Neuroscience Branch, NIH NIDA Intramural Research Program, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Neuropharmacology 52:895-903. 2007
    ....
  41. ncbi Functional interaction between alpha2-adrenoceptors, mu- and kappa-opioid receptors in the guinea pig myenteric plexus: effect of chronic desipramine treatment
    Luca Canciani
    Clinical and Applied Pharmacology Centre, University of Insubria and University of Pavia, via O Rossi 9, I 21100 Varese, Italy
    Eur J Pharmacol 553:269-79. 2006
    ....
  42. ncbi Role of serotonin in the regulation of the dynorphinergic system by a kappa-opioid agonist and cocaine treatment in rat CNS
    M Di Benedetto
    Department of Pharmacology, University of Bologna, Irnerio 48, Bologna, 40126 Italy
    Neuroscience 144:157-64. 2007
    ....
  43. ncbi Repeated administration of the selective kappa-opioid receptor agonist U-69593 increases stimulated dopamine extracellular levels in the rat nucleus accumbens
    José Antonio Fuentealba
    Department of Cellular and Molecular Biology, Faculty of Biological Sciences, Catholic University of Chile, Santiago, Chile
    J Neurosci Res 84:450-9. 2006
    ..It is suggested that repeated activation of KOR changes the response status of dopaminergic neurons in the NAc...
  44. pmc Increased opioid receptor binding and G protein coupling in the accumbens and ventral tegmental area of postnatal day 2 rats
    Yanning Hou
    Department of Biochemistry and Molecular Biology, St Louis University School of Medicine, MO 63104, USA
    Neurosci Lett 395:244-8. 2006
    ..It may be of significance that these brain regions, Acb and VTA, are undergoing maturation on P2...
  45. ncbi Kappa-opioid agonist U69593 potentiates locomotor sensitization to the D2/D3 agonist quinpirole: pre- and postsynaptic mechanisms
    Melissa L Perreault
    Department of Psychiatry and Behavioural Neurosciences, McMaster University, Hamilton, ON, Canada
    Neuropsychopharmacology 31:1967-81. 2006
    ..Together, findings suggest that sensitization to QNP is not a unitary phenomenon but has components that are relatively independent, mediated by distinct pre- and postsynaptic mechanisms and modulated by kappa receptor activity...
  46. ncbi Novel D-amino acid tetrapeptides produce potent antinociception by selectively acting at peripheral kappa-opioid receptors
    Todd W Vanderah
    Department of Pharmacology, University of Arizona Health Sciences Center, Tucson, AZ 85724, USA
    Eur J Pharmacol 583:62-72. 2008
    ..Furthermore, FE 200665 has entered into clinical trials with great promise as a novel analgesic lacking unwanted side effects seen with current therapeutics...
  47. ncbi Predominance of delta-opioid-binding sites in the porcine enteric nervous system
    DeWayne Townsend
    Department of Veterinary Pathobiology, College of Veterinary Medicine, University of Minnesota, St Paul, Minnesota 55108 6010, USA
    J Pharmacol Exp Ther 300:900-9. 2002
    ..These results indicate that delta-OPRs predominate in the porcine enteric nervous system with a more circumscribed expression of kappa- and mu-OPRs...
  48. pmc HS-599: a novel long acting opioid analgesic does not induce place-preference in rats
    R Lattanzi
    Department of Human Physiology and Pharmacology, University 'La Sapienza, P.le Aldo Moro, I-00185 Rome, Italy
    Br J Pharmacol 134:441-7. 2001
    ..It produces intense and long-lasting antinociception and does not induce place-preference in rats...
  49. ncbi SoRI 9409, a non-peptide opioid mu receptor agonist/delta receptor antagonist, fails to stimulate [35S]-GTP-gamma-S binding at cloned opioid receptors
    H Xu
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    Brain Res Bull 55:507-11. 2001
    ..Viewed collectively, the in vitro data reported here predict that SoRI 9409 should be a mu antagonist in vivo, which is not observed. Resolving these discrepant findings will require additional research...
  50. ncbi Kappa opioid receptor stimulation decreases amphetamine-induced behavior and neuropeptide mRNA expression in the striatum
    J A Tzaferis
    Department of Physiology and Neuroscience, Medical University of South Carolina, 173 Ashley Avenue, BSB 403, Charleston, SC 29425, USA
    Brain Res Mol Brain Res 93:27-35. 2001
    ..16 mg/kg. These data suggest that stimulation of kappa receptors decreases acute amphetamine-induced behavior and mRNA expression of neuropeptides in the rat striatum...
  51. 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...
  52. ncbi The bovine mu-opioid receptor: cloning of cDNA and pharmacological characterization of the receptor expressed in mammalian cells
    I Onoprishvili
    Department of Psychiatry, NYU School of Medicine, New York, NY 10016, USA
    Brain Res Mol Brain Res 73:129-37. 1999
    ..Evidence is presented indicating that the cloned receptor is the same as the bovine mu receptor previously purified to homogeneity in our laboratory. No evidence was found for genes for multiple mu-type opioid receptors...
  53. pmc Cloning and pharmacological characterization of a rat kappa opioid receptor
    F Meng
    Mental Health Research Institute, University of Michigan, Ann Arbor 48109
    Proc Natl Acad Sci U S A 90:9954-8. 1993
    ..These observations indicate that we have cloned a cDNA encoding a rat kappa receptor of the kappa 1 subtype...
  54. ncbi Evidence for transduction of mu but not kappa opioid modulation of extracellular signal-regulated kinase activity by G(z) and G(12) proteins
    M M Belcheva
    Department of Biochemistry and Molecular Biology, St. Louis University School of Medicine, 1402 S. Grand Blvd, St. Louis, MO, USA
    Cell Signal 12:481-9. 2000
    ..In this and prior studies, Galpha(z) and Galpha(12) immunoreactivity were detected in untransfected COS-7 cells, suggesting that these G proteins may be endogenous mediators of chronic mu inhibitory actions on ERK...
  55. ncbi Kappa opioid agonists alter dopamine markers and cocaine-stimulated locomotor activity
    S L Collins
    Department of Neurology, University of Miami School of Medicine, Florida 33136, USA
    Behav Pharmacol 12:237-45. 2001
    ..In addition, treatment with the kappa-opioid agonist U-69593 (0.32 mg/kg) over a 5-day period decreased dopamine transporter densities in the caudate putamen, and this was also blocked by co-administration of naltrexone...
  56. ncbi Opioids suppress basal and nicotine-induced catecholamine secretion via a stabilizing effect on actin filaments
    E Dermitzaki
    Department of Clinical Chemistry, University of Crete School of Medicine, Heraklion GR-711 10, Crete, Greece
    Endocrinology 142:2022-31. 2001
    ..It also appears that basal catecholamine secretion is associated with opioid-sensitive machinery regulating the continuous formation of short-lived areas of cortical actin filament disassembly...
  57. ncbi Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys
    S Stevens Negus
    Alcohol and Drug Abuse Research Center, Harvard Medical School, McLean Hospital, 115 Mill Street, Belmont, MA 02478, USA
    Psychopharmacology (Berl) 163:412-9. 2002
    ..Receptor-selective antagonists are useful experimental tools for evaluation of opioid receptor-mediated processes. 5'-Guanidinonaltrindole (GNTI) was recently developed as a novel kappa-selective antagonist...
  58. pmc kappa-Opioid agonist modulation of [3H]thymidine incorporation into DNA: evidence for the involvement of pertussis toxin-sensitive G protein-coupled phosphoinositide turnover
    J Barg
    E. A. Doisy Department of Biochemistry and Molecular Biology, St. Louis University School of Medicine, Missouri 63104-1079
    J Neurochem 60:1505-11. 1993
    ..In mixed glial cell aggregates, U50488 increased thymidine incorporation into DNA 3.1-fold, and this stimulation was reversed by the opioid antagonist naltrexone...
  59. pmc Agonists and antagonists bind to different domains of the cloned kappa opioid receptor
    H Kong
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104
    Proc Natl Acad Sci U S A 91:8042-6. 1994
    ..The ability to dissociate agonist- and antagonist-binding sites will facilitate the development of more specific kappa agonists, which could have analgesic properties devoid of side effects...
  60. ncbi A cellular mechanism for the antinociceptive effect of a kappa opioid receptor agonist
    M A Ackley
    Department of Anesthesia and Critical Care, University of Chicago, Chicago, IL 60637, USA
    Pain 91:377-88. 2001
    ....
  61. ncbi Synthesis and structure-opioid activity relationships of trans-(+/-)-3,4-dichloro-N-methyl-N-[4- or 5-hydroxy-2-(1-pyrrolidiny)cyclohexyl]benzeneacetamides
    C Y Cheng
    School of Pharmacy, College of Medicine, National Taiwan University, Taipei, R O C
    J Pharm Pharmacol 49:835-42. 1997
    ..a hydroxy function to the cyclohexane ring of kappa-selective opioid N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamides, trans-(+/-)-3,4-dichloro-N-methyl-N-[4- or 5-hydroxy-2-(1-pyrrolidiny)cyclohexyl]benzeneacetamides (1-4) ..
  62. ncbi Role of the chemokine receptor CXCR2 in bleomycin-induced pulmonary inflammation and fibrosis
    Remo C Russo
    Laboratorio de Imunofarmacologia, Departamento de Bioquimica e Imunologia, Instituto de Ciencias Biologicas, Universidade Federal de Minas Gerais, Avenida Antonio Carlos 6627, CEP 30882 650 Pampulha, Belo Horizonte, MG, Brazil
    Am J Respir Cell Mol Biol 40:410-21. 2009
    ..An effect on neutrophils does not appear to account for the major effects of the blockade of CXCR2 in the system...
  63. ncbi Double-masked study of the effects of nepafenac 0.1% and ketorolac 0.4% on corneal epithelial wound healing and pain after photorefractive keratectomy
    Eric D Donnenfeld
    Ophthalmic Consultants of Long Island, Rockville Centre, New York 11570, USA
    Adv Ther 24:852-62. 2007
    ..4% provide postoperative pain relief after PRK surgery without associated adverse effects on corneal epithelial healing. Nepafenac 0.1% treatment may offer greater comfort upon instillation in patients who have undergone PRK...
  64. ncbi Kappa opioid receptor inhibition of glutamatergic transmission in the nucleus accumbens shell
    G O Hjelmstad
    Department of Neurology, The W M Keck Center for Integrative Neuroscience and The Wheeler Center for the Neurobiology of Addiction, University of California, San Francisco, California 94143, USA
    J Neurophysiol 85:1153-8. 2001
    ..This presynaptic inhibition of excitatory synaptic transmission in the nucleus accumbens shell provides a novel mechanism that may contribute to the kappa-receptor-mediated aversion observed in intact animals...
  65. ncbi Vagus nerve stimulation modulates visceral pain-related affective memory
    Xu Zhang
    Neuroscience Laboratory, Department of Biology and Chemistry, City University of Hong Kong, Kowloon, Hong Kong, China
    Behav Brain Res 236:8-15. 2013
    ....
  66. pmc Cholecystokinin enhances visceral pain-related affective memory via vagal afferent pathway in rats
    Bing Cao
    Neuroscience Laboratory, Department of Biology and Chemistry, City University of Hong Kong, Kowloon, Hong Kong, China
    Mol Brain 5:19. 2012
    ..It has been well demonstrated that CCK acting on vagal afferent fibers mediates various physiological functions. We hypothesize that CCK activation of vagal afferent enhances visceral pain-related affective memory...
  67. ncbi Paradoxical effects of prodynorphin gene deletion on basal and cocaine-evoked dopaminergic neurotransmission in the nucleus accumbens
    V I Chefer
    Integrative Neuroscience Section, Behavioral Neuroscience Branch, DHHS NIH NIDA IRP BNRB INS, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Eur J Neurosci 23:229-38. 2006
    ..These findings suggest that the phenotype of DYN KO mice is not solely due to loss of endogenous opioid peptide but also reflects developmental compensations that occur at the level of the opioid receptor...
  68. pmc TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats
    Joseph F Cotten
    Department of Anesthesia, Critical Care, and Pain Medicine, Massachusetts General Hospital, GRB 444, 55 Fruit St, Boston, MA 02114, USA
    Anesth Analg 116:810-6. 2013
    ..PK-THPP and A1899 are potent and selective TASK-1 and TASK-3 antagonists. I hypothesized PK-THPP and A1899 are, like doxapram, breathing stimulants...
  69. ncbi Treatment with exendin-4 improves the antidiabetic efficacy and reverses hepatic steatosis in glucokinase activator treated db/db mice
    Nirav Dhanesha
    Department of Pharmacology and Toxicology, Zydus Research Centre, Cadila Healthcare Limited, Sarkhej Bavla N H No 8A, Moraiya, Ahmedabad 382210, India
    Eur J Pharmacol 714:188-92. 2013
    ..Overall, our data indicate that combination of GKA and GLP-1 receptor agonist Ex-4 improves glucose homeostasis, shows antiobesity activity, without causing harmful side effects like fatty liver. ..
  70. ncbi Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors
    Taiji Goto
    R and D Division, Daiichi Sankyo Co, Ltd, 1 2 58 Hiromachi, Tokyo 140 8710, Japan
    Bioorg Med Chem Lett 23:3325-8. 2013
    ..The binding mode of the new inhibitor (31e) in the catalytic site of PDE4B is presented based on an X-ray crystal structure of the ligand-enzyme complex...
  71. pmc Ablation of kappa-opioid receptors from brain dopamine neurons has anxiolytic-like effects and enhances cocaine-induced plasticity
    Ashlee Van't Veer
    Department of Psychiatry, Harvard Medical School, McLean Hospital, Belmont, MA 02478, USA
    Neuropsychopharmacology 38:1585-97. 2013
    ..These mouse lines may be useful in future studies of KOR function...
  72. ncbi Sensitization to the conditioned rewarding effects of morphine and cocaine: differential effects of the kappa-opioid receptor agonist U69593
    T S Shippenberg
    Integrative Neuroscience Unit, Behavioral Neuroscience Branch, NIDA Division of Intramural Research, Baltimore, MD 21224, USA
    Eur J Pharmacol 345:27-34. 1998
    ..U69593 prevents sensitization and cross-sensitization induced by cocaine, but does not modify morphine-induced sensitization or the cross-sensitization which develops to cocaine after morphine administration...
  73. ncbi Analgesic, respiratory and heart rate effects of cannabinoid and opioid agonists in rhesus monkeys: antagonist effects of SR 141716A
    J A Vivian
    Department of Psychology, University of Michigan Medical School, Ann Arbor, Michigan 48109 0632, USA
    J Pharmacol Exp Ther 286:697-703. 1998
    ..These results demonstrate selective and reversible antagonism of cannabinoid behavioral effects by SR 141716A in rhesus monkeys...
  74. ncbi The effect of a novel thromboxane A2 (TXA2) receptor antagonist (S-1452) on the antigen-induced bronchoconstriction and airway hyperresponsiveness in guinea pigs
    H Nagai
    Department of Pharmacology, Gifu Pharmaceutical University, Japan
    Prostaglandins Leukot Essent Fatty Acids 48:343-9. 1993
    ..These results indicate the efficacy of S-1452 on antigen-induced bronchoconstriction and antigen-induced airway hyperresponsiveness in guinea pigs...
  75. ncbi ATR controls cellular adaptation to hypoxia through positive regulation of hypoxia-inducible factor 1 (HIF-1) expression
    F Fallone
    1 CNRS, IPBS Institut de Pharmacologie et de Biologie Structurale, Toulouse, France 2 Université de Toulouse, UPS, IPBS, Toulouse, France
    Oncogene 32:4387-96. 2013
    ..Our work offers new prospect for cancer therapy using ATR inhibitors with the potential to decrease cellular adaptation in hypoxic tumors. ..
  76. ncbi Nepafenac dosing frequency for ocular pain and inflammation associated with cataract surgery
    W Andrew Maxwell
    California Eye Institute, Fresno, CA 93720, USA
    J Ocul Pharmacol Ther 24:593-9. 2008
    ..Nepafenac ophthalmic suspension 0.1% was dosed topically once (QD), twice (BID), or three-times (TID) daily to assess the resolution of ocular pain and anterior-segment inflammation following cataract surgery...
  77. 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...
  78. ncbi Immunoregulatory properties of novel specific inhibitors of 5-lipoxygenase
    D S Liu
    Department of Experimental Immunobiology, Wellcome Research Laboratories, Kent, U K
    Immunopharmacology 17:1-9. 1989
    ..The immunosuppressive action of the 5-LO inhibitors described here seems to be a novel secondary property of the compounds...
  79. pmc The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation
    John P Alao
    Department of Cell and Molecular Biology, Lundberg Laboratory University of Gothenburg, P, O, Box 462, S 405 30 Goteborg, Sweden
    Radiat Oncol 4:51. 2009
    ..The differential effects of caffeine/CGK733 and KU55933 on cyclin D1 protein levels suggest that these agents will exhibit dissimilar molecular pharmacological profiles...
  80. ncbi mu/delta Cooperativity and opposing kappa-opioid effects in nucleus accumbens-mediated antinociception in the rat
    Brian L Schmidt
    Graduate Program in Oral Biology, University of California at San Francisco, San Francisco, CA 94143 0440, USA
    Eur J Neurosci 15:861-8. 2002
    ....
  81. ncbi Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides
    John G Cumming
    Respiratory and Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 15:5012-5. 2005
    ..SAR and DMPK studies led to the identification of substituted N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides as potent and orally bioavailable ligands for the human CCR5 chemokine receptor...
  82. ncbi Muscarinic receptor antagonist-induced lenticular opacity in rats
    Genevieve Durand
    Laboratoires Merck Sharp and Dohme Chibret, Route de Marsat, Riom, 63963 Clermont Ferrand Cedex 9, France
    Toxicol Sci 66:166-72. 2002
    ..No such lenticular opacities have been reported in other animal species, including man, after treatment with muscarinic receptor antagonists...
  83. ncbi A randomized comparison of to-aqueous penetration of ketorolac 0.45%, bromfenac 0.09% and nepafenac 0.1% in cataract patients undergoing phacoemulsification
    Frank A Bucci
    Bucci Laser Vision Institute, Wilkes Barre, PA 18702, USA
    Curr Med Res Opin 27:2235-9. 2011
    ..45%, bromfenac 0.09%, nepafenac 0.1%, and amfenac (the active metabolite of nepafenac) in patients undergoing phacoemulsification...
  84. ncbi Comparative effects of procainamide, tocainide and lorcainide on Na(+)-K(+)-ATPase in guinea pig heart preparations
    N Dzimiri
    Biological and Medical Research Department, King Faisal Specialist Hospital and Research Centre, Riyadh, Saudi Arabia
    Gen Pharmacol 22:403-6. 1991
    ..6. These interactions may be pertinent to the proarrhythmic or arrhythmogenic effects of the class 1 type of antiarrhythmic drugs...
  85. pmc The effects of beta 2-adrenoceptor agonists and a corticosteroid, budesonide, on the secretion of inflammatory mediators from monocytes
    M Linden
    Research and Development Department, Astra Draco AB, Lund, Sweden
    Br J Pharmacol 107:156-60. 1992
    ..Furthermore, the anti-secretory action of beta2-agonists was distinct from that of corticosteroids...
  86. ncbi Preclinical evaluation and molecular docking of 4-phenyl-1-Napthyl phenyl acetamide (4P1NPA) from Streptomyces sp. DPTB16 as a potent antifungal compound
    Subhasish Saha
    Department of Microbiology, School of Life Sciences, Bharathidasan University, Tamil Nadu, India
    Comput Biol Med 42:542-7. 2012
    ..On the whole, we highlight the findings of this research will be helpful to design 4P1NPA as novel antifungal drug to defend the emerging antifungal resistance...
  87. pmc Involvement of glutamate and gamma-amino-butyric acid receptor systems on gastric acid secretion induced by activation of kappa-opioid receptors in the central nervous system in rats
    Sachie Minowa
    Laboratory of Chemical Pharmacology, Graduate School of Pharmaceutical Sciences, Chiba University, Chiba 263 8522, Japan
    Br J Pharmacol 138:1049-58. 2003
    ..The present findings show pharmacological evidence for kappa-opioid receptor subtypes that regulate gastric acid secretion in the rat brain...
  88. ncbi The acceptability of a four-part protocol for penicillin allergy testing by practicing allergists
    Alyson B Simpson
    Division of Allergy and Immunology, Alfred I duPont Hospital for Children, Nemours Children s Clinic, Wilmington, Delaware, USA
    Allergy Asthma Proc 30:192-201. 2009
    ..Forty-five percent of the fellows of the AAAAI would apply the proposed protocol to test for PCN allergy. Sixty-two percent said they may apply the protocol if a larger study was performed...
  89. ncbi Preclinical and clinical investigation of a CCR5 antagonist, AZD5672, in patients with rheumatoid arthritis receiving methotrexate
    Danielle M Gerlag
    Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands
    Arthritis Rheum 62:3154-60. 2010
    ..To investigate both the preclinical effects of blocking the chemokine receptor CCR5 and the clinical effects of this approach on the signs and symptoms of rheumatoid arthritis (RA) in patients with active disease...
  90. pmc The role of prostanoid TP- and DP-receptors in the bronchoconstrictor effect of inhaled PGD2 in anaesthetized guinea-pigs: effect of the DP-antagonist BW A868C
    S Hamid-Bloomfield
    Department of Pharmacology, Wellcome Research Laboratories, Beckenham, Kent
    Br J Pharmacol 100:761-6. 1990
    ..8. These findings indicate that the bronchoconstrictor effect of inhaled PGD2 in guinea-pigs in vivo is mediated primarily through direct TP-receptor activation and not through actions on DP-receptors...
  91. 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...
  92. ncbi [3H]U-69593 labels a subtype of kappa opiate receptor with characteristics different from that labeled by [3H]ethylketocyclazocine
    B Nock
    Department of Psychiatry, Washington University School of Medicine, St Louis, MO 63110
    Life Sci 42:2403-12. 1988
    ..Based on these findings, we propose that [3H]U-69593 (and U-50488H) labels a kappa receptor subtype which differs from that labeled by [3H]EKC at 4 degrees C...
  93. pmc Molecular imaging of the ATM kinase activity
    Terence M Williams
    Department of Radiation Oncology, Ohio State University, Columbus, Ohio, USA
    Int J Radiat Oncol Biol Phys 86:969-77. 2013
    ..We sought to create a bioluminescent reporter that dynamically and noninvasively measures ATM kinase activity in living cells and subjects...
  94. ncbi The chemokine receptors CXCR1/CXCR2 modulate antigen-induced arthritis by regulating adhesion of neutrophils to the synovial microvasculature
    Fernanda M Coelho
    Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais, Brazil
    Arthritis Rheum 58:2329-37. 2008
    ..We undertook this study to investigate the role of these receptors in mediating neutrophil adhesion, subsequent migration, and neutrophil-dependent hypernociception in a murine model of monarticular antigen-induced arthritis (AIA)...
  95. ncbi Comparison of liquid chromatography-mass spectrometry and radioimmunoassay for measurement of fentanyl and determination of pharmacokinetics in equine plasma
    Sara M Thomasy
    K L Maddy Equine Analytical Chemistry Laboratory, California Animal Health and Food Safety Laboratory, School of Veterinary Medicine, University of California, Davis, California 95616, USA
    J Anal Toxicol 32:754-9. 2008
    ..In conclusion, when compared with LC-MS, fentanyl concentrations determined by RIA in equine plasma are misleading, especially for the calculation of fentanyl pharmacokinetics...
  96. ncbi Preparation of benzylpenicilloyl-polylysine: a preliminary study
    Preeti Vemuri
    Division of Allergy Immunology, Department of Medicine, Northwestern University Feinberg School of Medicine, Chicago, Illinois 60611, USA
    Allergy Asthma Proc 25:165-8. 2004
    ..Our benzylpenicilloyl-polylysine production methodology could prove useful to those who do not have access to PrePen or another similar reagent...
  97. ncbi Kappa-opioid receptor stimulation quickens pathogenesis of compulsive checking in the quinpirole sensitization model of obsessive-compulsive disorder (OCD)
    Melissa L Perreault
    Department of Psychiatry and Behavioural Neurosciences, McMaster University, Hamilton, ON, Canada
    Behav Neurosci 121:976-91. 2007
    ..The animal model findings point to a potential role of kappa opioid systems in hastening the pathogenesis of OCD and to the possibility that distinct brain regions may mediate the development and the expression of compulsive checking...
  98. ncbi Retrograde opioid signaling regulates glutamatergic transmission in the hypothalamus
    Karl J Iremonger
    Hotchkiss Brain Institute and Department of Physiology and Pharmacology, University of Calgary, Calgary, Alberta T2N 4N1, Canada
    J Neurosci 29:7349-58. 2009
    ..These findings demonstrate that neurons may self-regulate their excitability through the dendritic release of opioids to inhibit excitatory synaptic transmission...
  99. ncbi Topical capsaicin-induced allodynia in unanesthetized primates: pharmacological modulation
    Eduardo R Butelman
    Rockefeller University, New York, NY 10021, USA
    J Pharmacol Exp Ther 306:1106-14. 2003
    ....
  100. pmc Regulation of arcuate neurons coexpressing kisspeptin, neurokinin B, and dynorphin by modulators of neurokinin 3 and κ-opioid receptors in adult male mice
    Kristen A Ruka
    Department of Molecular and Integrative Physiology, University of Michigan, Ann Arbor, MI 48109, USA
    Endocrinology 154:2761-71. 2013
    ..Together, these observations support the hypotheses that activation of NK3R and KOR, respectively, excites and inhibits KNDy neurons and that gonadal steroids modulate these effects. ..
  101. ncbi [The role of structural protein Gag and related gene (protein) in late stages of the HIV-1 replication cycle and the inhibitors]
    Yan Jiang
    Institute of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China
    Yao Xue Xue Bao 45:205-14. 2010
    ..In this article, the role of structural protein Gag and related gene (protein) in late stages of the HIV-1 replication cycle and related inhibitors is reviewed...

Research Grants24

  1. EFFECTS OF SYSTEMICALLY ADMINISTERED DYNORPHINS
    Eduardo Butelman; Fiscal Year: 2002
    ....
  2. kappa-agonist effects of the hallucinogen Salvinorin A
    Eduardo Butelman; Fiscal Year: 2008
    ....
  3. Plasticity of Kappa Opioid Function in Reward Circuitry
    GREGORY HJELMSTAD; Fiscal Year: 2007
    ..Specific aims will test both the extracellular and intracellular mechanisms underlying this effect, as well as testing the specificity of the effect on glutamate release. ..
  4. Novel Delta Opioids: Analgesic Effects & Abuse Liability
    SIDNEY NEGUS; Fiscal Year: 2009
    ....
  5. High Throughput Screening-Based Identification of Measles Virus Probes
    RICHARD PLEMPER; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  6. Chronic drug exposures in monkeys: serial MRI studies
    Marc Kaufman; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  7. Magnetic Resonance, EEG, and Behavior After Cocaine
    Marc Kaufman; Fiscal Year: 2008
    ..This work will facilitate the direct comparison of neurochemical data across species. ..
  8. REGULATION OF SECRETION FROM HUMAN BASOPHILS
    Donald MacGlashan; Fiscal Year: 2009
    ..A population of subjects will be examined for this relationship. ..
  9. Chronic morphine-induced sensitization of trigeminal dura sensitive neurons
    Ian D Meng; Fiscal Year: 2010
    ..Understanding the neuro-adaptive changes that occur with chronic morphine exposure will lead the way to new therapeutic strategies to treat headache patients while reducing the risk of developing MOH. ..
  10. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 2001
    ..An ideal candidate compound would not only have efficacy in the preclinical models but would be safe, orally active, and potent, would not show tolerance or sensitization, and if abusable, would be less so than cocaine. ..
  11. Design and Development of Pharmacotherapies for Treating Stimulant Abuse
    Frank Ivy Carroll; Fiscal Year: 2010
    ..3) To continue on a limited basis our development of selected 3-phenyltropane analogs as second-generation pharmacotherapies to treat cocaine addiction. ..
  12. HIV-1 entry inhibitors targeting Phe43 cavity in gp120
    Asim Debnath; Fiscal Year: 2003
    ..The long-term goal of this proposal is to optimize the lead compounds through chemical synthesis and structure activity analyses and select 3-4 best compounds for further preclinical studies as novel ianti-HIV-1 chemotherapeutic agents. ..
  13. Rational Design of CCR5 Antagonists as Anti-HIV-1 Drugs
    Asim Debnath; Fiscal Year: 2006
    ..The long term goal is to optimize the lead compounds through chemical syntheses and structure activity relationship (SAR) analyses and select the 3-4 best compounds for further preclinical studies. ..
  14. Ultra High Field 9.4T Animal Magnetic Resonance Scanner
    Marc Kaufman; Fiscal Year: 2004
    ..4 Tesla animal scanner. ..
  15. Cocaine & Steroids: Brain Vascular & Behavioral Effects
    Marc Kaufman; Fiscal Year: 2005
    ..Thus, if our hypotheses regarding hormonal effects on cocaine-induced vasoconstriction are validated, the potential for identifying effective therapeutics for investigation in chronic treatment trials will be enhanced. ..
  16. GHB: Discrimination and effects on learning
    Lisa Baker; Fiscal Year: 2003
    ..Behavior under these assays is sensitive to other abused drugs. Therefore, these assays may be of value in characterizing the effects of GHB. ..
  17. "Post-partum steroid withdrawal-induced depression"
    REBECCA CRAFT; Fiscal Year: 2006
    ..Findings from the proposed model will enhance our understanding of the etiology of PPD and possibly lead to improved treatment options. ..
  18. Opioid Receptors in the Mechanisms of Opioid Tolerance
    Zhizhong Pan; Fiscal Year: 2005
    ..This research will significantly expand our knowledge of the neural mechanisms for opioid tolerance and contribute to our efforts to improve the treatment for chronic pain and other chronic opioid-related problems. ..
  19. Trigeminal Mechanisms of Cannabinoid Analgesia
    Ian Meng; Fiscal Year: 2005
    ..abstract_text> ..
  20. Effects of self-administered MDMA on brain and behavior in rhesus monkeys
    William Fantegrossi; Fiscal Year: 2007
    ..Thus, these studies are likely to be more relevant to the potential human condition of MDMA-induced lasting neurochemical alterations and behavioral changes [unreadable] [unreadable]..
  21. Structure-Based Design of Nipah Virus Entry Inhibitors
    RICHARD PLEMPER; Fiscal Year: 2006
    ..These will be characterized for their activity against live Nipah (aim 3). ..
  22. NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTION
    Frank Carroll; Fiscal Year: 2008
    ..abstract_text> ..
  23. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..