[Nphe1]Nociceptin(1-13)NH2 - CAS 267234-08-2
Category: Inhibitor
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Opioid Receptor
[Nphe1]Nociceptin(1-13)NH2 acts as the first truly selective and competitive nociceptin receptor antagonist and is devoid of any residual agonist activity. It binds selectively to recombinant nociceptin receptors (pKi = 8.4), and competitively antagonizes the actions of nociceptin in vitro and in vivo.
(Modifications: Gly-1 = N-Bn-Gly, Lys-13 = C-terminal amide)
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1.Involvement of nociceptin/orphanin FQ in release of hypothalamic GnRH mediated by ORL1 receptor in ovariectomized rats.
An XF1, Chen HP, Ma SL, Feng Y, Hao JW, Chen BY. Acta Pharmacol Sin. 2005 Sep;26(9):1039-44.
AIM: To investigate effect of the nociceptin/orphanin FQ (OFQ) on hypothalamus gonadotropin-releasing hormone (GnRH) release in ovariectomized (OVX) rats.
2.Novel potent agonist [(pF)Phe4,Aib7,Aib11,Arg14,Lys15]N/OFQ-NH2 and antagonist [Nphe1,(pF)Phe4,Aib7,Aib11,Arg14,Lys15]N/OFQ-NH2 of nociceptin/orphanin FQ receptor.
Peng YL1, Chang M, Dong SL, Li W, Han RW, Fu GX, Chen Q, Wang R. Regul Pept. 2006 May 15;134(2-3):75-81. Epub 2006 Mar 6.
Two novel ligands for the nociceptin/orphanin FQ (N/OFQ) receptor (NOP), [(pF)Phe4,Aib7, Aib11,Arg14,Lys15]N/OFQ-NH2 (peptide-1) and [Nphe1,(pF)Phe4,Aib7,Aib11,Arg14,Lys15]N/OFQ-NH2 (peptide-2), have been generated by combining different modifications of N/OFQ sequence. In the present study, we investigated the actions of two analogues and compared them with those of N/OFQ in four assays. Peptide-1 mimicked N/OFQ effects in mouse vas deferens and mouse colon and showed similar maximal effects but higher potency relative to N/OFQ. The effects of peptide-1 were sensitive to NOP receptor selective antagonist ([Nphe1]N/OFQ(1-13)-NH2) but not to naloxone in vitro. Peptide-1 (25 pmol, i.c.v.) mimicked the pronociceptive action of N/OFQ (2.5 nmol, i.c.v.) in mouse tail withdrawal assay, displaying higher potency and longer lasting effects. In anesthetized rats, peptide-1 (1 nmol/kg, i.v.) produced a marked decrease in mean arterial pressure, which was comparable to that evoked by i.
3.MT-7716, a novel selective nonpeptidergic NOP receptor agonist, effectively blocks ethanol-induced increase in GABAergic transmission in the rat central amygdala.
Kallupi M1, Oleata CS2, Luu G2, Teshima K3, Ciccocioppo R4, Roberto M2. Front Integr Neurosci. 2014 Feb 18;8:18. doi: 10.3389/fnint.2014.00018. eCollection 2014.
The GABAergic system in the central amygdala (CeA) plays a major role in ethanol dependence and the anxiogenic-like response to ethanol withdrawal. A large body of evidence shows that Nociceptin/Orphanin FQ (N/OFQ) regulates ethanol intake and anxiety-like behavior. In the rat, ethanol significantly augments CeA GABA release, whereas N/OFQ diminishes it. Using electrophysiological techniques in an in vitro slice preparation, in this study we investigated the effects of a nonpeptidergic NOP receptor agonist, MT-7716 [(R)-2-3-[1-(Acenaphthen-1-yl)piperidin-4-yl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl-N-methylacetamide hydrochloride hydrate], and its interaction with ethanol on GABAergic transmission in CeA slices of naïve rats. We found that MT-7716 dose-dependently (100-1000 nM) diminished evoked GABAA receptor-mediated inhibitory postsynaptic potentials (IPSPs) and increased paired-pulse facilitation (PPF) ratio of these evoked IPSPs, suggesting a presynaptic site of action of the MT-7716 by decreasing GABA release at CeA synapses.
4.Role of hypothalamus nociceptin/orphanin FQ in pre-ovulatory luteinizing hormone surge of estrogen and progesterone-primed, ovariectomized rats.
An XF1, Yu JY, Feng Y, Chen BY, Zhang SL. Acta Pharmacol Sin. 2007 Aug;28(8):1189-97.
AIM: To investigate the role of hypothalamus nociceptin/orphanin FQ (OFQ) and its endogenous receptor, the opioid receptor-like1 receptor (ORL1 receptor) in the estrus cycle of female rats.
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CAS 267234-08-2 [Nphe1]Nociceptin(1-13)NH2

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