benzeneacetamides

Summary

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

Top Publications

  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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

Research Grants

  1. EFFECTS OF SYSTEMICALLY ADMINISTERED DYNORPHINS
    Eduardo Butelman; Fiscal Year: 2002
  2. kappa-agonist effects of the hallucinogen Salvinorin A
    Eduardo Butelman; Fiscal Year: 2007
  3. NOVEL DELTA OPIOIDS--ANALGESIC EFFECTS & ABUSE LIABILITY
    SIDNEY NEGUS; Fiscal Year: 2002
  4. Plasticity of Kappa Opioid Function in Reward Circuitry
    GREGORY HJELMSTAD; Fiscal Year: 2007
  5. Novel Delta Opioids: Analgesic Effects & Abuse Liability
    SIDNEY NEGUS; Fiscal Year: 2009
  6. Neurobiology and Treatment of Pain
    SIDNEY NEGUS; Fiscal Year: 2009
  7. Medications Development for Stimulant Abuse
    SIDNEY NEGUS; Fiscal Year: 2009
  8. Opioid Receptors in the Mechanisms of Opioid Tolerance
    Zhizhong Pan; Fiscal Year: 2005
  9. Trigeminal Mechanisms of Cannabinoid Analgesia
    Ian Meng; Fiscal Year: 2005
  10. "Post-partum steroid withdrawal-induced depression"
    REBECCA CRAFT; Fiscal Year: 2006

Detail Information

Publications125 found, 100 shown here

  1. 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...
  2. 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...
  3. 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...
  4. 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...
  5. 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...
  6. 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...
  7. 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
    ....
  8. 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...
  9. 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...
  10. 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...
  11. 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...
  12. 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...
  13. 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...
  14. 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
    ....
  15. 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...
  16. 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...
  17. 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
    ....
  18. 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...
  19. 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
    ....
  20. ncbi 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...
  21. ncbi 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...
  22. ncbi 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...
  23. 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
    ....
  24. 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...
  25. 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...
  26. ncbi 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...
  27. 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...
  28. 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...
  29. ncbi 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 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
    ....
  31. 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
  32. 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...
  33. 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...
  34. ncbi Differential time course of effects of kappa-opioid agonist treatment on dynorphin A levels and kappa-opioid receptor density
    Manuela Di Benedetto
    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...
  35. 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...
  36. 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...
  37. 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...
  38. 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...
  39. 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...
  40. 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...
  41. ncbi 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...
  42. 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...
  43. 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
    ....
  44. ncbi 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...
  45. 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...
  46. 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
    ....
  47. 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...
  48. 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...
  49. ncbi 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...
  50. 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...
  51. 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
    ....
  52. 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...
  53. 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...
  54. 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...
  55. ncbi 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...
  56. 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) ..
  57. ncbi Agonist-induced internalization of CC chemokine receptor 5 as a mechanism to inhibit HIV replication
    Thierry Ferain
    Euroscreen s a, Rue Adrienne Bolland, 47, B 6041 Gosselies, Belgium
    J Pharmacol Exp Ther 337:655-62. 2011
    ....
  58. 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...
  59. ncbi 2,3-Disubstituted acrylamides as potent glucokinase activators
    Achyutharao Sidduri
    Department of Discovery Chemistry, Roche Research Center, 340 Kingsland Street, Nutley, NJ 07110, USA
    Bioorg Med Chem Lett 20:5673-6. 2010
    ..In normal Wistar rats, the 2,3-disubstituted acrylamide analog 10 was well absorbed and demonstrated robust glucose lowering effects...
  60. ncbi The utility of in vitro data in making accurate predictions of human P-glycoprotein-mediated drug-drug interactions: a case study for AZD5672
    Robert Elsby
    Clinical Pharmacology and DMPK, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 39:275-82. 2011
    ..The observed dose-dependent clinically significant interaction was accurately predicted using calculated [I(2)] and in vitro P-gp inhibition data, confirming AZD5672 to be a P-gp inhibitor in vivo...
  61. ncbi FLZ, a novel HSP27 and HSP70 inducer, protects SH-SY5Y cells from apoptosis caused by MPP(+)
    Xiang Chen Kong
    Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, PR China
    Brain Res 1383:99-107. 2011
    ..These results provide new evidence for elucidating the mechanism of the neuroprotective effect of FLZ against PD...
  62. ncbi Blockade of the chemokine receptor CXCR2 ameliorates adjuvant-induced arthritis in rats
    M M Barsante
    Departamento de Bioquimica e Imunologia, Instituto Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil
    Br J Pharmacol 153:992-1002. 2008
    ..The potential benefits of oral administration of a CXCR1/2 inhibitor, DF 2162, in adjuvant-induced polyarthritis (AIA) were investigated...
  63. ncbi Repeated treatment with the κ-opioid agonist U-69593 increases K+-stimulated dopamine release in the rat medial prefrontal cortex
    José Antonio Fuentealba
    Millenium Science Nucleus in Stress and Addiction, Pontificia Universidad Catolica de Chile, Santiago, Chile
    Synapse 64:898-904. 2010
    ..The repeated treatment with U-69593 significantly augmented potassium-stimulated DA extracellular levels, without affecting potassium-stimulated 5HT extracellular levels, suggesting an increase in DA releasability...
  64. ncbi Differential expression and sensitivity of presynaptic and postsynaptic opioid receptors regulating hypothalamic proopiomelanocortin neurons
    Reagan L Pennock
    Department of Biomedical Sciences, Colorado State University, Fort Collins, Colorado 80523, USA
    J Neurosci 31:281-8. 2011
    ..The results may help explain why it has been difficult to clearly discern the role that opioids play in the regulation of food intake and other processes involving POMC neurons...
  65. ncbi The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, alvimopan, ADL 08-0011 and methylnaltrexone
    D T Beattie
    Department of Pharmacology, Theravance Inc, 901 Gateway Boulevard, South San Francisco, CA 94080, USA
    Naunyn Schmiedebergs Arch Pharmacol 375:205-20. 2007
    ..The clinical significance of the data from this study remains to be determined...
  66. ncbi Molecular dynamics of cis-1-(2-hydroxy-5- methylphenyl)ethanone oxime and N-(2-hydroxy-4-methylphenyl)acetamide in solution studied by NMR spectroscopy
    Ibrahim Garib Mamedov
    Chemical Faculty, NMR Laboratory, Baku State University, Baku, Azerbaijan
    Magn Reson Chem 48:671-7. 2010
    ..O, O-H...N and O...H-N type inter- and intramolecular hydrogen bonds. Spin-lattice relaxation times (T(1)), activation energy of molecular dynamics and energy of intramolecular hydrogen bonds have been determined...
  67. ncbi U-69593, a kappa opioid receptor agonist, decreases cocaine-induced behavioral sensitization in female rats
    Anabel Puig-Ramos
    Department of Physiology, University of Puerto Rico, School of Medicine, San Juan, Puerto Rico
    Behav Neurosci 122:151-60. 2008
    ..This decrease in cocaine-induced hyperlocomotion persisted after 1 week of cocaine withdrawal. These data indicate that the KOPr system participates in estradiol modulation of cocaine-induced behavioral sensitization in the female rat...
  68. ncbi Corneal melting after use of nepafenac in a patient with chronic cystoid macular edema after cataract surgery
    Mario A Di Pascuale
    Department of Ophthalmology, The University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX, 75390 9057, USA
    Eye Contact Lens 34:129-30. 2008
    ..To the authors' knowledge, this is the first case report of a corneal melt after the prolonged use of nepafenac to treat cystoid macular edema...
  69. 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
    ....
  70. ncbi Double-masked comparison of ketorolac tromethamine 0.4% versus nepafenac sodium 0.1% for postoperative healing rates and pain control in eyes undergoing surface ablation
    Rolando Toyos
    Cornea 27:384; author reply 384-5. 2008
  71. ncbi Depletion of serotonin decreases the effects of the kappa-opioid receptor agonist U-69593 on cocaine-stimulated activity
    Elena Zakharova
    University of Miami Miller School of Medicine, Department of Psychiatry and Behavioral Sciences, 1600 NW 10th Ave, Suite 4113A, D 80, Miami, FL 33136, USA
    Eur J Pharmacol 586:123-9. 2008
    ..These findings suggest that serotonin plays an important role in mediating the effects of kappa-opioid receptor agonists on the behavioral response to cocaine...
  72. ncbi Displacement of opioid receptor binding ligands from the rat brain by N3-(2',5'-dimethoxyphenacyl) arabinofuranosyluracil
    Tomomi Shimizu
    Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Ho-3, Kanagawa-machi, Kanazawa 920-1181, Japan
    Res Commun Mol Pathol Pharmacol 117:105-13. 2005
    ..These results indicate that N3-(2',5'-DiMeOPhAc)AraU interacts with mu- and delta-opioid receptors...
  73. ncbi Behavioral effects of acute stimulation of kappa-opioid receptors during lactation
    Elizabeth Teodorov
    Faculdade de Medicina Veterinaria e Zootecnia, Departamento de Patologia, Universidade de Sao Paulo, Brazil
    Pharmacol Biochem Behav 90:534-9. 2008
    ..The present results suggest that pre-mating repeated exposure to morphine produces a tolerance-like effect on behavioral responses to low-dose kappa-opioid receptor stimulation in active reproductive females...
  74. ncbi The kappa-opioid agonist U69,593 blocks cocaine-induced enhancement of brain stimulation reward
    Hilarie C Tomasiewicz
    Behavioral Genetics Laboratory, Department of Psychiatry, Harvard Medical School, McLean Hospital, Belmont, MA 02478, USA
    Biol Psychiatry 64:982-8. 2008
    ....
  75. ncbi The use of a cyclooxygenase-2 inhibitor (Nepafenac) in an ocular and metastatic animal model of uveal melanoma
    Jean Claude A Marshall
    The Henry C Witelson Ophthalmic Pathology Laboratory and Registry, McGill University Health Center, 3775 University Street, Lyman Duff Building, Room 216, Montreal, Quebec H3A 2B4, Canada
    Carcinogenesis 28:2053-8. 2007
    ..These results indicate that the topical administration of a COX-2 inhibitor delayed the progression of this malignancy in our animal model. A clinical trail using an anti-COX-2 inhibitor for patients with UM should be considered...
  76. ncbi Midbrain dopamine neurons: projection target determines action potential duration and dopamine D(2) receptor inhibition
    Elyssa B Margolis
    Ernest Gallo Clinic and Research Center, University of California, San Francisco, Emeryville, California 94608, USA
    J Neurosci 28:8908-13. 2008
    ..Therefore, in the VTA, AP duration and inhibition by D(2)R agonists may be valid markers of DA content in neurons of known projection target...
  77. ncbi Compound FLZ inhibits lipopolysaccharide-induced inflammatory effects via down-regulation of the TAK-IKK and TAK-JNK/p38MAPK pathways in RAW264.7 macrophages
    Hong Yan Pang
    Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China
    Acta Pharmacol Sin 30:209-18. 2009
    ..7 macrophages...
  78. ncbi Effects of kappa opioids in an assay of pain-depressed intracranial self-stimulation in rats
    S Stevens Negus
    Department of Pharmacology and Toxicology, Virginia Commonwealth University, 410 North 12th Street, Richmond, VA 23298, USA
    Psychopharmacology (Berl) 210:149-59. 2010
    ..This discrepancy may be related to the behavioral depressant effects of kappa agonists. Kappa antagonists do not typically produce antinociception, but they produce antidepressant-like effects in some preclinical assays...
  79. ncbi Cystoid and diabetic macular edema treated with nepafenac 0.1%
    Seenu M Hariprasad
    Department of Ophthalmology and Visual Science, University of Chicago, Chicago, IL 60637, USA
    J Ocul Pharmacol Ther 23:585-90. 2007
    ..These clinical data strongly suggest that nepafenac 0.1% is a promising drug for the treatment of posterior segment inflammation, including CME, and warrants further investigation...
  80. ncbi Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [3H]deltorphin II
    B Buzas
    Isotope Laboratory, Biological Research Center, Hungarian Academy of Sciences, Szeged
    Life Sci 50:PL75-8. 1992
    ..The highly delta selective binding properties of this new radioligand suggest that it could serve as an excellent tool for investigating the delta opioid receptors in various species...
  81. ncbi N-phenethyl-2-phenylacetamide isolated from Xenorhabdus nematophilus induces apoptosis through caspase activation and calpain-mediated Bax cleavage in U937 cells
    Seok-Young Hwang
    Institute for Medical Science, Keimyung University, Daegu 700-712, Korea
    Int J Oncol 22:151-7. 2003
    ..Taken together, the apoptotic effects of NPPA may be related, in part to the caspase-3 activation, the down-regulation of XIAP, and Bax cleavage mediated by caspase-dependent calpain activation...
  82. ncbi Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities
    Kyoung Soon Kim
    Department of Oncology Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543 4000, USA
    J Med Chem 45:3905-27. 2002
    ....
  83. ncbi Differential antagonism of bremazocine- and U69,593-induced antinociception by quadazocine: further functional evidence of opioid kappa receptor multiplicity in the mouse
    P J Horan
    Department of Pharmacology, University of Arizona Health Sciences Center, Tucson
    J Pharmacol Exp Ther 266:926-33. 1993
    ..abstract truncated at 250 words)..
  84. ncbi L-type Ca2+ channel modulation by dihydropyridines potentiates kappa-opioid receptor agonist induced acute analgesia and inhibits development of tolerance in rats
    S Gullapalli
    Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research, Phase - X, Sector 67, S.A.S.Nagar (Mohali) - 160 062, Punjab, India
    Neuropharmacology 42:467-75. 2002
    ..These results strongly suggest a functional role of L-type Ca(2+) channels in the regulation of pain sensitivity, mechanism of kappa-opioid analgesia and expression of tolerance...
  85. ncbi Effects of kappa-opioid receptor agonists on long-term cocaine use and dopamine neurotransmission
    S L Collins
    Department of Neurology, University of Miami School of Medicine, 1501 NW 9th Avenue (D4-5, Miami, FL 33136, USA
    Eur J Pharmacol 426:25-34. 2001
    ..In addition, U-69593 can block cocaine-induced locomotor effects without major perturbation of the dopamine system...
  86. ncbi Chronic opioid treatment of the mouse thymoma cell lines R1.G1 and R1EGO leads to down-regulation of the kappa opioid receptor without desensitization of adenylyl cyclase activity
    I Martin-Kleiner
    Division of Molecular Medicine, Ruder Boskovic Institute, Bijenicka c 54, 10001 Zagreb, Croatia
    Int Immunopharmacol 1:13-20. 2001
    ..This study demonstrates that unlike some neuronal preparations, chronic opioid treatment of the thymoma cell lines resulted in receptor down-regulation without desensitization...
  87. ncbi Kappa-opioid receptor activation modifies dopamine uptake in the nucleus accumbens and opposes the effects of cocaine
    A C Thompson
    Behavioral Neuroscience Branch, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    J Neurosci 20:9333-40. 2000
    ..The action of kappa-agonists on DA uptake or DAT binding, or both, may be the mechanism(s) mediating the previously reported "cocaine-antagonist" effect of kappa-opioid receptor agonists...
  88. ncbi Effects of the inhibition of cyclo-oxygenase 1 or 2 or 5-lipoxygenase on the activation of the hypothalamic-pituitary-adrenal axis induced by interleukin-1beta in the male Rat
    S M Parsadaniantz
    Laboratoire de Neurobiologie Cellulaire et Moleculaire, Faculte de Pharmacie, Paris, France
    J Neuroendocrinol 12:766-73. 2000
    ....
  89. ncbi Dissociable effects of the kappa-opioid receptor agonists bremazocine, U69593, and U50488H on locomotor activity and long-term behavioral sensitization induced by amphetamine and cocaine
    L J Vanderschuren
    Department of Pharmacology, Medical Faculty, Free University, Amsterdam, The Netherlands
    Psychopharmacology (Berl) 150:35-44. 2000
    ..By influencing dopaminergic neurotransmission, opioid drugs can alter the behavioral effects of psychostimulants...
  90. ncbi U-69,593 microinjection in the infralimbic cortex reduces anxiety and enhances spontaneous alternation memory in mice
    P M Wall
    School of Psychology, University of Ottawa, Vanier Room 215, Ottawa, Canada
    Brain Res 856:259-80. 2000
    ....
  91. ncbi [11C]-methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)-methyl]-1- piperazinecarboxylate ([11C]GR89696): synthesis and in vivo binding to kappa opiate receptors
    H T Ravert
    Department of Radiology, The Johns Hopkins Medical Institutions, Baltimore, Maryland 21287 0750, USA
    Nucl Med Biol 26:737-41. 1999
    ..8, 5.6, and 4.5 for the hypothalamus, olfactory tubercle, and striatum, respectively. The uptake of [11C]GR89696 correlated with known kappa opioid receptor densities and was inhibited by kappa opioid selective drugs...
  92. ncbi Inhibition of tumour growth by lipoxygenase inhibitors
    H J Hussey
    Pharmaceutical Sciences Institute, Aston University, Birmingham, UK
    Br J Cancer 74:683-7. 1996
    ..The inhibitory effect of these agents on cell growth may result from an imbalance of metabolism of arachidonic acid between the 5-, 12- and 15-lipoxygenase pathways...
  93. ncbi kappa-Opioid receptor recognition sites are not modulated by local anaesthetics
    G L Fraser
    Astra Pain Control AB, Preclinical R and D, Novum Unit, Huddinge, Sweden
    Biochem Pharmacol 49:883-91. 1995
    ..These studies demonstrate that effects of kappa-opioid receptor recognition site conformation are unlikely to explain the clinically observed synergy between local anaesthetics and opioids...
  94. ncbi Failure of the inhibition of rat gastric mucosal 5-lipoxygenase by novel acetohydroxamic acids to prevent ethanol-induced damage
    N K Boughton-Smith
    Department of Pharmacology, Wellcome Research Laboratories, Beckenham, Kent
    Br J Pharmacol 95:155-62. 1988
    ..9. These findings suggest that the leukotrienes, LTB4 and LTC4 are not the primary mediators of ethanol-induced acute mucosal damage, but do not exclude their role in more chronic gastric damage and inflammation...
  95. ncbi Pharmacological activities of optically pure enantiomers of the kappa opioid agonist, U50,488, and its cis diastereomer: evidence for three kappa receptor subtypes
    R B Rothman
    Unit on Receptor Studies, LCS, NIMH, Bethesda, MD 20892
    Eur J Pharmacol 167:345-53. 1989
    ..The order of potency was (-)-(1S,2S)-U50,488 greater than (+/-)-U50,488 greater than (+/-)-cis diastereomer of U50,488 greater than (+)-(1R,2R)-U50,488.(ABSTRACT TRUNCATED AT 250 WORDS)..
  96. ncbi Involvement of capsaicin-sensitive nerves in the bronchomotor effects of arachidonic acid and melittin: a possible role for lipoxin A4
    S Manzini
    Istituto Farmacobiologico Malesci, Research Laboratories, Firenze, Italy
    Br J Pharmacol 103:1027-32. 1991
    ..6. These findings indicate that lipoxin A4 but not leukotriene D4 or 15-HETE, might be one of the lipoxygenase mediators of excitatory effects of AA on capsaicin-sensitive sensory nerves...
  97. ncbi Phosphorylation- and stimulus-dependent inhibition of cellular 5-lipoxygenase activity by nonredox-type inhibitors
    Lutz Fischer
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie-Curie Strasse 9, D-60439 Frankfurt, Germany
    FASEB J 17:949-51. 2003
    ....
  98. ncbi Age-related differences in sensitivity to the antinociceptive effects of kappa opioids in adult male rats
    Mark A Smith
    Program in Neuroscience, Davidson College, Davidson, NC 28035 7037, USA
    Psychopharmacology (Berl) 162:255-64. 2002
    ..Although the relationship between aging and sensitivity to the antinociceptive effects of mu opioids has been examined extensively, relatively few studies have examined this relationship in kappa opioids...
  99. ncbi Investigation of substituent effect of 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides on CCR5 binding affinity using QSAR and virtual screening techniques
    Antreas Afantitis
    School of Chemical Engineering, National Technical University of Athens, Athens, Greece
    J Comput Aided Mol Des 20:83-95. 2006
    ..The study leads to a number of guanidine derivatives with significantly improved predicted activities...
  100. ncbi Comparison of the analgesic efficacy and safety of nepafenac ophthalmic suspension compared with diclofenac ophthalmic solution for ocular pain and photophobia after excimer laser surgery: a phase II, randomized, double-masked trial
    Joseph Colin
    University Hospital Complex of Bordeaux, Pellegrin Hospital, Bordeaux, France
    Clin Ther 28:527-36. 2006
    ..There was no difference in the proportion of patients who took rescue acetaminophen for pain. All treatments were well tolerated in these patients...
  101. ncbi Importance of mixture of minor determinants and benzylpenicilloyl poly-L-lysine skin testing in the diagnosis of beta-lactam allergy
    P J Bousquet
    J Allergy Clin Immunol 115:1314-6. 2005

Research Grants87

  1. EFFECTS OF SYSTEMICALLY ADMINISTERED DYNORPHINS
    Eduardo Butelman; Fiscal Year: 2002
    ....
  2. kappa-agonist effects of the hallucinogen Salvinorin A
    Eduardo Butelman; Fiscal Year: 2007
    ....
  3. NOVEL DELTA OPIOIDS--ANALGESIC EFFECTS & ABUSE LIABILITY
    SIDNEY NEGUS; Fiscal Year: 2002
    ....
  4. 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. ..
  5. Novel Delta Opioids: Analgesic Effects & Abuse Liability
    SIDNEY NEGUS; Fiscal Year: 2009
    ....
  6. Neurobiology and Treatment of Pain
    SIDNEY NEGUS; Fiscal Year: 2009
    ....
  7. Medications Development for Stimulant Abuse
    SIDNEY NEGUS; Fiscal Year: 2009
    ..These studies may contribute to both (a) more effective implementation of existing monoamine releasers as agonist medications, and (b) the development of safer medications with reduced abuse liability. ..
  8. 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. ..
  9. Trigeminal Mechanisms of Cannabinoid Analgesia
    Ian Meng; Fiscal Year: 2005
    ..abstract_text> ..
  10. "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. ..
  11. 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). ..
  12. 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 ..
  13. Identification and Pre-Clinical Evaluation of Measles Virus Inhibitors
    RICHARD PLEMPER; Fiscal Year: 2007
    ..Characteristic viral escape patterns will be identified for efficacious compounds that warrant future clinical development, and cross-resistance between structurally distinct therapeutic leads will be assessed. ..
  14. Development of Pharmacotherapies for Nicotine Addiction
    Frank Carroll; Fiscal Year: 2005
    ....
  15. DIABETIC RETINOPATHY
    Timothy Kern; Fiscal Year: 1999
    ....
  16. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 1991
    ....
  17. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2003
    ..abstract_text> ..
  18. Synaptic mechanisms for interactions of chronic pain and opioid addiction
    Zhizhong Pan; Fiscal Year: 2009
    ..The goal of this project is to identify pharmacological targets to reduce the abuse potential of opioids taken for pain control while maintaining their analgesic effects. ..
  19. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..
  20. MECHANISMS OF HUMAN BASOPHIL & MAST CELL DESENSITIZATION
    Donald MacGlashan; Fiscal Year: 1992
    ..Phosphorylation of 5'- phosphomonoesterase will be directly examined as will its activity in desensitized basophils and mast cells...
  21. Social and Enviromental Influences on Opioid Sensitivity
    Mark Smith; Fiscal Year: 2006
    ..These studies should identify the critical biological, pharmacological and environmental factors contributing to differences in drug-seeking behavior across subject populations. ..
  22. REGULATION OF SECRETION FROM HUMAN BASOPHILS
    Donald MacGlashan; Fiscal Year: 2007
    ..A population of subjects will be examined for this relationship. ..
  23. MECHANISMS OF HUMAN BASOPHIL & MAST CELL DESENSITIZATION
    Donald MacGlashan; Fiscal Year: 1993
    ..Since cytokine release appears dependent on mRNA accumulation, initial studies will focus on the mechanisms of mRNA accumulation...
  24. Neural Substrates of Stimulus-Induced Drug Seeking
    KRISTEN KEEFE; Fiscal Year: 2007
    ....
  25. Chronic morphine-induced sensitization of trigeminal dura sensitive neurons
    Ian Meng; Fiscal Year: 2007
    ..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. ..
  26. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2007
    ..Compounds that are potent delta selective opioid receptor inverse agonists will be evaluated by Dr. Chris Evans (UCLA) in a chronic antinociception rat model. ..