Pharmacological studies on the NOP and opioid receptor agonist PWT2-[Dmt1]N/OFQ(1-13)
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چکیده
منابع مشابه
In vitro pharmacological characterization of a novel unbiased NOP receptor‐selective nonpeptide agonist AT‐403
Nociceptin/orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP), a member of the opioid receptor family. We recently identified a new high affinity and highly selective NOP agonist AT-403. In this study, we characterized the functional profile of AT-403 and compared it to other known nonpeptide NOP agonists Ro 65-6570, Ro 2q, SCH-221510...
متن کاملXWH - 07 - 1 - 0162 TITLE : Pharmacological studies of NOP receptor agonists as novel analgesics PRINCIPAL INVESTIGATOR :
Nociceptin/orphanin FQ (N/OFQ) is the endogenous peptide for the NOP receptors. Depending on the doses, intrathecal administration of N/OFQ has dual actions (ie, hyperalgesia and antinociception) in rodents. However, the pharmacological profile of intrathecal N/OFQ is not fully known in primates. The aim of this study was to investigate behavioral effects of intrathecal N/OFQ over a wide dose r...
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Suggestions to Contributors Tribute to Dr. Paul Lewis Munson 3 Agonist-induced Desensitization of the 3-Adrenergic Receptor-linked Adenylate Cyclase. T. KENDALL HARDEN 5 Behavioral and Pharmacological Aspects of Opioid Dependence: Mixed Agonist-Antagonists. WILLIAM L. WOOLVERTON AND CHARLES R. SCHUSTER 33 Pharmacology of Mesocortical Dopamine Neurons. MICHAEL J. BANNON AND ROBERT H. ROTH 53 Opi...
متن کامل[Dmt1]N/OFQ(1-13)-NH2: a potent nociceptin/orphanin FQ and opioid receptor universal agonist.
BACKGROUND AND PURPOSE Intrathecally (i.t.) administered nociceptin/orphanin FQ (N/OFQ) evokes antinociceptive effects in rodents. Recent studies in monkeys demonstrated that i.t. co-application of N/OFQ and morphine elicits synergistic antinociceptive actions suggesting mixed N/OFQ peptide (NOP) and μ opioid receptor agonists as innovative spinal analgesics. Thus, novel N/OFQ related peptides ...
متن کاملStudies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.
Salvinorin A (1), from the sage Salvia divinorum, is a potent and selective kappa opioid receptor (KOR) agonist. We screened other salvinorins and derivatives for binding affinity and functional activity at opioid receptors. Our results suggest that the methyl ester and furan ring are required for activity but that the lactone and ketone functionalities are not. Other salvinorins showed negligi...
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ژورنال
عنوان ژورنال: European Journal of Pharmacology
سال: 2017
ISSN: 0014-2999
DOI: 10.1016/j.ejphar.2016.11.026