[(pF)Phe,Arg,Lys]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor
نویسندگان
چکیده
Department of Experimental and Clinical Medicine, Section of Pharmacology and Neuroscience Center (G.C., A.R., F.M., G.M., D.R., E.G., S.Z., D.R., M.M., G.C.) and Department of Pharmaceutical Sciences and Biotechnology Center (R.G., S.S.), University of Ferrara, 44100 Ferrara, Italy. Department of Cardiovascular Sciences, Pharmacology and Therapeutics Group (T.A.B., J.McD., C.P.H., D.G.L.) and Department of Health Sciences, Division of Anaesthesia, Critical Care and Pain Management (D.J.R.), Leicester Royal Infirmary, Leicester, LE1 5WW, UK. Department of Pharmacology (V.A.K., D.R.K.), Louisiana State University, Health Sciences Center, New Orleans, Louisiana, U.S. JPET Fast Forward. Published on October 27, 2004 as DOI:10.1124/jpet.104.077339
منابع مشابه
[(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.
A novel ligand for the nociceptin/orphanin FQ (N/OFQ) receptor (NOP), [(pF)Phe(4),Arg(14),Lys(15)]N/OFQ-NH(2) (UFP-102), has been generated by combining in the N/OFQ-NH(2) sequence two chemical modifications, [Arg(14),Lys(15)] and [(pF)Phe(4)], that have been previously demonstrated to increase potency. In vitro, UFP-102 bound with high affinity to the human NOP receptor, showed at least 200-fo...
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The advance of functional genomics revealed the superfamily of G-protein coupled receptors (GPCRs). Hundreds of GPCRs have been cloned but many of them are orphan GPCRs with unidentified ligands. The first identified orphan GPCR is the opioid receptor like orphan receptor, ORL1. It was cloned in 1994 during the identification of opioid receptor subtypes and was de-orphanized in 1995 by the disc...
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Nociceptin/orphanin FQ (N/OFQ) modulates various biological functions, including nociception, via selective stimulation of the N/OFQ peptide receptor (NOP). Here we used the NOP selective antagonist UFP-101 to characterize the receptor involved in the spinal antinociceptive effects of N/OFQ evaluated in the mouse tail withdrawal assay and to investigate the mechanism underlying this action by a...
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The pharmacology of G protein-coupled receptors can be influenced by factors such as constitutive receptor activation and Na(+) ions. In this study, we examined the coupling of natively and heterologously expressed nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptors with voltage-dependent Ca(2+) channels after exposure to four high-affinity NOP receptor blockers [[Nphe(1)Arg(14)Lys(15)]N/OFQ...
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Nociceptin/orphanin FQ (N/OFQ) has been demonstrated to modulate nociceptive transmission via selective activation of N/OFQ peptide (NOP) receptors. Despite huge research efforts, the role(s) of the endogenous N/OFQ-NOP receptor system in pain processing remains incompletely understood. In the present study, we investigated the role of endogenous N/OFQ in the processing of tonic nociceptive inp...
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