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Titolo:
Pharmacological characterization of the nociceptin receptor, ORL1 - Insight from the inward rectifier activation in the periaqueductal gray
Autore:
Chiou, LC;
Indirizzi:
Natl Taiwan Univ, Coll Med, Dept Pharmacol, Taipei 100, Taiwan Natl TaiwanUniv Taipei Taiwan 100 d, Dept Pharmacol, Taipei 100, Taiwan
Titolo Testata:
JOURNAL OF BIOMEDICAL SCIENCE
fascicolo: 3, volume: 7, anno: 2000,
pagine: 232 - 240
SICI:
1021-7770(200005/06)7:3<232:PCOTNR>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
NEURONS IN-VITRO; RAT VAS-DEFERENS; ORPHANIN-FQ/NOCICEPTIN; NALOXONE BENZOYLHYDRAZONE; NORADRENALINE RELEASE; MEDIATED INHIBITION; SPINAL-CORD; MOUSE-BRAIN; NOCISTATIN REVERSES; NUCLEUS NEURONS;
Keywords:
nociceptin; ORL1; mu-opioid receptors; naloxone benzoylhydrazone; [Phe1 psi(CH2-NH)Gly(2)]nociceptin-(1-13)-NH2; K+ channels; periaqueductal gray; patch clamp; brain slices; nocistatin; acetyl-RYYRIK-NH2;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
61
Recensione:
Indirizzi per estratti:
Indirizzo: Chiou, LC Natl Taiwan Univ, Coll Med, Dept Pharmacol, 1 Jen Ai Rd,Sect 1, Taipei 100, Taiwan Natl Taiwan Univ 1 Jen Ai Rd,Sect 1 Taipei Taiwan 100 0, Taiwan
Citazione:
L.C. Chiou, "Pharmacological characterization of the nociceptin receptor, ORL1 - Insight from the inward rectifier activation in the periaqueductal gray", J BIOMED SC, 7(3), 2000, pp. 232-240

Abstract

A novel opioid receptor-like orphan receptor (ORL1) was cloned and identified to be homologous to classical opioid receptors but insensitive to traditional opioids. A heptadecapeptide, termed orphanin FQ or nociceptin (OFQ/N), was identified as its endogenous ligand. OFQ/N shares overlapping distribution sites in pain-processing areas and common cellular mechanisms with opioids but exerts diverse effects on nociceptive responses. Of the two reported ORL1 antagonists, [Phe(1)psi(CH2-NH)-Gly(2)] nociceptin-(1-1 3)-NH2 (Phe psi) and naloxone benzoylhydrazone (NBZ), antagonisms were validated in the activation of inward rectifying K channels induced by OFQ/N, using the patch clamp technique in ventrolateral periaqueductal gray slices. Results showed that Phe psi acted as a partial agonist and NBZ was a weak nonselective antagonist of ORL1. It is comparable with most but not all of the findings from other tissues. Comparing all the reports supports the above inference for these two antagonists. The possible causes for the discrepancy werediscussed. A brief review on the putative ORL1 antagonists, acetyl-RYYRIK-NH2, some sigma-ligands and the functional antagonist, nocistatin, is also included. It indicates that a potent and selective ORL1 antagonist is expecting to elucidate the physiological role of OFQ/N, Copyright (C) 2000 National Science Council. ROC and S. Karger AG, Basel.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 15:14:11