Genomes and Genes
Summary: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.
Publications172 found, 100 shown here
- The novel squamosamide derivative FLZ protects against 6-hydroxydopamine-induced apoptosis through inhibition of related signal transduction in SH-SY5Y cellsDan 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...
- Small molecule-based reversible reprogramming of cellular lifespanJaejoon 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...
- Squamosamide derivative FLZ protects dopaminergic neurons against inflammation-mediated neurodegeneration through the inhibition of NADPH oxidase activityDan 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...
- 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 studyRiccardo 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...
- A novel cyclic squamosamide analogue compound FLZ improves memory impairment in artificial senescence mice induced by chronic injection of D-galactose and NaNO2Fang 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....
- Ocular permeation and inhibition of retinal inflammation: an examination of data and expert opinion on the clinical utility of nepafenacRichard 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...
- Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2Taeweon Lee
Amgen Inc, South San Francisco, California 94080, USA
Mol Pharmacol 74:1599-609. 2008....
- A natural squamosamide derivative FLZ reduces amyloid-beta production by increasing non-amyloidogenic AbetaPP processingYan 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...
- Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapyElvira 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...
- 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 cellsDan 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...
- [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...
- Protective effects of compound FLZ on beta-amyloid peptide-(25-35)-induced mouse hippocampal injury and learning and memory impairmentFang 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...
- Pharmacological study of the novel compound FLZ against experimental Parkinson's models and its active mechanismWeihong 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...
- Novel squamosamide derivative (compound FLZ) attenuates Abeta25-35-induced toxicity in SH-SY5Y cellsFang 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....
- Region-dependent G-protein activation by kappa-opioid receptor agonists in the mouse brainHirokazu 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...
- delta-opioid receptor-mediated actions on rostral ventromedial medulla neuronsS Marinelli
Pain Management Research Institute, Kolling Institute, Northern Clinical School, University of Sydney, Sydney, NSW 2006, Australia
Neuroscience 132:239-44. 2005
- Both kappa and mu opioid agonists inhibit glutamatergic input to ventral tegmental area neuronsElyssa 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...
- Differential time course of effects of kappa-opioid agonist treatment on dynorphin A levels and kappa-opioid receptor densityClaudio 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...
- Discriminative stimulus effects of acute morphine followed by naltrexone in the squirrel monkeyDavid 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...
- Kappa opioid receptor activation in the nucleus accumbens inhibits glutamate and GABA release through different mechanismsGregory 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...
- Presynaptic mechanism for anti-analgesic and anti-hyperalgesic actions of kappa-opioid receptorsBihua Bie
Department of Symptom Research, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
J Neurosci 23:7262-8. 2003....
- 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 activityPeter 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...
- Activation of mu opioid receptors in the ventrolateral periaqueductal gray inhibits reflex micturition in anesthetized ratsSeiji 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...
- A single cocaine exposure enhances both opioid reward and aversion through a ventral tegmental area-dependent mechanismJoseph 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...
- Opioid interactions in rhesus monkeys: effects of delta + mu and delta + kappa agonists on schedule-controlled responding and thermal nociceptionGlenn 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...
- Kappa-opioid agonists directly inhibit midbrain dopaminergic neuronsElyssa 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...
- Peripheral selectivity and apparent efficacy of dynorphins: comparison to non-peptidic kappa-opioid agonists in rhesus monkeysEduardo 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...
- Naloxone and its quaternary derivative, naloxone methiodide, have differing affinities for mu, delta, and kappa opioid receptors in mouse brain homogenatesTanya 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...
- Mu and kappa opioid receptors activate ERK/MAPK via different protein kinase C isoforms and secondary messengers in astrocytesMariana 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...
- 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....
- Opioid regulation of spinal cord plasticity: evidence the kappa-2 opioid receptor agonist GR89696 inhibits learning within the rat spinal cordStephanie 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...
- N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacyCecile Beguin
Department of Psychiatry, McLean Hospital, MRC 322A, 115 Mill Street, Belmont, MA 02478, USA
J Pharmacol Exp Ther 324:188-95. 2008....
- 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 cellsKENNETH 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....
- The hallucinogen derived from Salvia divinorum, salvinorin A, has kappa-opioid agonist discriminative stimulus effects in ratsCatherine 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...
- 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 ratsMelissa 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...
- Increased locomotor response to amphetamine induced by the repeated administration of the selective kappa-opioid receptor agonist U-69593José 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...
- Acute amphetamine exposure selectively desensitizes kappa-opioid receptors in the nucleus accumbensYan 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...
- The kappa-opioid receptor agonist U-69593 prevents cocaine-induced phosphorylation of DARPP-32 at Thr(34) in the rat brainManuela 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...
- Sensitivity of the five-choice serial reaction time task to the effects of various psychotropic drugs in Sprague-Dawley ratsTracie 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...
- Pharmacological and genetic manipulation of kappa opioid receptors: effects on cocaine- and pentylenetetrazol-induced convulsions and seizure kindlingRafal 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....
- Functional interaction between alpha2-adrenoceptors, mu- and kappa-opioid receptors in the guinea pig myenteric plexus: effect of chronic desipramine treatmentLuca 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....
- Role of serotonin in the regulation of the dynorphinergic system by a kappa-opioid agonist and cocaine treatment in rat CNSM Di Benedetto
Department of Pharmacology, University of Bologna, Irnerio 48, Bologna, 40126 Italy
Neuroscience 144:157-64. 2007....
- Repeated administration of the selective kappa-opioid receptor agonist U-69593 increases stimulated dopamine extracellular levels in the rat nucleus accumbensJosé 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...
- Increased opioid receptor binding and G protein coupling in the accumbens and ventral tegmental area of postnatal day 2 ratsYanning 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...
- Kappa-opioid agonist U69593 potentiates locomotor sensitization to the D2/D3 agonist quinpirole: pre- and postsynaptic mechanismsMelissa 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...
- Novel D-amino acid tetrapeptides produce potent antinociception by selectively acting at peripheral kappa-opioid receptorsTodd 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...
- Predominance of delta-opioid-binding sites in the porcine enteric nervous systemDeWayne 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...
- HS-599: a novel long acting opioid analgesic does not induce place-preference in ratsR 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...
- SoRI 9409, a non-peptide opioid mu receptor agonist/delta receptor antagonist, fails to stimulate [35S]-GTP-gamma-S binding at cloned opioid receptorsH 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...
- Kappa opioid receptor stimulation decreases amphetamine-induced behavior and neuropeptide mRNA expression in the striatumJ 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...
- Kappa-opioid receptor-mediated effects of the plant-derived hallucinogen, salvinorin A, on inverted screen performance in the mouseWilliam 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...
- The bovine mu-opioid receptor: cloning of cDNA and pharmacological characterization of the receptor expressed in mammalian cellsI 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...
- Cloning and pharmacological characterization of a rat kappa opioid receptorF 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...
- Evidence for transduction of mu but not kappa opioid modulation of extracellular signal-regulated kinase activity by G(z) and G(12) proteinsM 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...
- Kappa opioid agonists alter dopamine markers and cocaine-stimulated locomotor activityS 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...
- Opioids suppress basal and nicotine-induced catecholamine secretion via a stabilizing effect on actin filamentsE 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...
- Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeysS 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...
- kappa-Opioid agonist modulation of [3H]thymidine incorporation into DNA: evidence for the involvement of pertussis toxin-sensitive G protein-coupled phosphoinositide turnoverJ 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...
- Agonists and antagonists bind to different domains of the cloned kappa opioid receptorH 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...
- A cellular mechanism for the antinociceptive effect of a kappa opioid receptor agonistM A Ackley
Department of Anesthesia and Critical Care, University of Chicago, Chicago, IL 60637, USA
Pain 91:377-88. 2001....
- Synthesis and structure-opioid activity relationships of trans-(+/-)-3,4-dichloro-N-methyl-N-[4- or 5-hydroxy-2-(1-pyrrolidiny)cyclohexyl]benzeneacetamidesC 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) ..
- Role of the chemokine receptor CXCR2 in bleomycin-induced pulmonary inflammation and fibrosisRemo 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...
- Double-masked study of the effects of nepafenac 0.1% and ketorolac 0.4% on corneal epithelial wound healing and pain after photorefractive keratectomyEric 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...
- Kappa opioid receptor inhibition of glutamatergic transmission in the nucleus accumbens shellG 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...
- Vagus nerve stimulation modulates visceral pain-related affective memoryXu Zhang
Neuroscience Laboratory, Department of Biology and Chemistry, City University of Hong Kong, Kowloon, Hong Kong, China
Behav Brain Res 236:8-15. 2013....
- Cholecystokinin enhances visceral pain-related affective memory via vagal afferent pathway in ratsBing 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...
- Paradoxical effects of prodynorphin gene deletion on basal and cocaine-evoked dopaminergic neurotransmission in the nucleus accumbensV 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...
- TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized ratsJoseph 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...
- Treatment with exendin-4 improves the antidiabetic efficacy and reverses hepatic steatosis in glucokinase activator treated db/db miceNirav 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. ..
- Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitorsTaiji 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...
- Ablation of kappa-opioid receptors from brain dopamine neurons has anxiolytic-like effects and enhances cocaine-induced plasticityAshlee 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...
- Sensitization to the conditioned rewarding effects of morphine and cocaine: differential effects of the kappa-opioid receptor agonist U69593T 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...
- Analgesic, respiratory and heart rate effects of cannabinoid and opioid agonists in rhesus monkeys: antagonist effects of SR 141716AJ 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...
- The effect of a novel thromboxane A2 (TXA2) receptor antagonist (S-1452) on the antigen-induced bronchoconstriction and airway hyperresponsiveness in guinea pigsH 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...
- ATR controls cellular adaptation to hypoxia through positive regulation of hypoxia-inducible factor 1 (HIF-1) expressionF 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. ..
- Nepafenac dosing frequency for ocular pain and inflammation associated with cataract surgeryW 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...
- U69593, a kappa-opioid agonist, decreases cocaine self-administration and decreases cocaine-produced drug-seekingS 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...
- Immunoregulatory properties of novel specific inhibitors of 5-lipoxygenaseD 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...
- The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferationJohn 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...
- mu/delta Cooperativity and opposing kappa-opioid effects in nucleus accumbens-mediated antinociception in the ratBrian 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....
- Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamidesJohn 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...
- Muscarinic receptor antagonist-induced lenticular opacity in ratsGenevieve 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...
- A randomized comparison of to-aqueous penetration of ketorolac 0.45%, bromfenac 0.09% and nepafenac 0.1% in cataract patients undergoing phacoemulsificationFrank 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...
- Comparative effects of procainamide, tocainide and lorcainide on Na(+)-K(+)-ATPase in guinea pig heart preparationsN 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...
- The effects of beta 2-adrenoceptor agonists and a corticosteroid, budesonide, on the secretion of inflammatory mediators from monocytesM 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...
- Preclinical evaluation and molecular docking of 4-phenyl-1-Napthyl phenyl acetamide (4P1NPA) from Streptomyces sp. DPTB16 as a potent antifungal compoundSubhasish 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...
- 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 ratsSachie 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...
- The acceptability of a four-part protocol for penicillin allergy testing by practicing allergistsAlyson 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...
- Preclinical and clinical investigation of a CCR5 antagonist, AZD5672, in patients with rheumatoid arthritis receiving methotrexateDanielle 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...
- 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 A868CS 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...
- Lack of effect of kappa-opioid receptor agonism on long-term methamphetamine-induced neurotoxicity in ratsKamisha 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...
- [3H]U-69593 labels a subtype of kappa opiate receptor with characteristics different from that labeled by [3H]ethylketocyclazocineB 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...
- Molecular imaging of the ATM kinase activityTerence 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...
- The chemokine receptors CXCR1/CXCR2 modulate antigen-induced arthritis by regulating adhesion of neutrophils to the synovial microvasculatureFernanda 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)...
- Comparison of liquid chromatography-mass spectrometry and radioimmunoassay for measurement of fentanyl and determination of pharmacokinetics in equine plasmaSara 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...
- Preparation of benzylpenicilloyl-polylysine: a preliminary studyPreeti 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...
- 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...
- Retrograde opioid signaling regulates glutamatergic transmission in the hypothalamusKarl 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...
- Topical capsaicin-induced allodynia in unanesthetized primates: pharmacological modulationEduardo R Butelman
Rockefeller University, New York, NY 10021, USA
J Pharmacol Exp Ther 306:1106-14. 2003....
- Regulation of arcuate neurons coexpressing kisspeptin, neurokinin B, and dynorphin by modulators of neurokinin 3 and κ-opioid receptors in adult male miceKristen 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. ..
- [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...
- EFFECTS OF SYSTEMICALLY ADMINISTERED DYNORPHINSEduardo Butelman; Fiscal Year: 2002....
- kappa-agonist effects of the hallucinogen Salvinorin AEduardo Butelman; Fiscal Year: 2008....
- Plasticity of Kappa Opioid Function in Reward CircuitryGREGORY 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. ..
- Novel Delta Opioids: Analgesic Effects & Abuse LiabilitySIDNEY NEGUS; Fiscal Year: 2009....
- High Throughput Screening-Based Identification of Measles Virus ProbesRICHARD PLEMPER; Fiscal Year: 2007..unreadable] [unreadable] [unreadable]..
- Chronic drug exposures in monkeys: serial MRI studiesMarc Kaufman; Fiscal Year: 2008..unreadable] [unreadable] [unreadable] [unreadable]..
- Magnetic Resonance, EEG, and Behavior After CocaineMarc Kaufman; Fiscal Year: 2008..This work will facilitate the direct comparison of neurochemical data across species. ..
- REGULATION OF SECRETION FROM HUMAN BASOPHILSDonald MacGlashan; Fiscal Year: 2009..A population of subjects will be examined for this relationship. ..
- Chronic morphine-induced sensitization of trigeminal dura sensitive neuronsIan 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. ..
- NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCEFrank 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. ..
- Design and Development of Pharmacotherapies for Treating Stimulant AbuseFrank 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. ..
- HIV-1 entry inhibitors targeting Phe43 cavity in gp120Asim 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. ..
- Rational Design of CCR5 Antagonists as Anti-HIV-1 DrugsAsim 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. ..
- Ultra High Field 9.4T Animal Magnetic Resonance ScannerMarc Kaufman; Fiscal Year: 2004..4 Tesla animal scanner. ..
- Cocaine & Steroids: Brain Vascular & Behavioral EffectsMarc 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. ..
- GHB: Discrimination and effects on learningLisa 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. ..
- "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. ..
- Opioid Receptors in the Mechanisms of Opioid ToleranceZhizhong 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. ..
- Trigeminal Mechanisms of Cannabinoid AnalgesiaIan Meng; Fiscal Year: 2005..abstract_text> ..
- Effects of self-administered MDMA on brain and behavior in rhesus monkeysWilliam 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]..
- Structure-Based Design of Nipah Virus Entry InhibitorsRICHARD PLEMPER; Fiscal Year: 2006..These will be characterized for their activity against live Nipah (aim 3). ..
- NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTIONFrank Carroll; Fiscal Year: 2008..abstract_text> ..
- COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTIONFrank Carroll; Fiscal Year: 2007..abstract_text> ..