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Titolo:
Orphanin FQ/nociceptin and naloxone benzoylhydrazone activate distinct receptors in BE(2)-C human neuroblastoma cells
Autore:
Mathis, JP; Mandyam, CD; Altememi, GF; Pasternak, GW; Standifer, KM;
Indirizzi:
Univ Houston, Dept Pharmacol & Pharmaceut Sci, Houston, TX 77204 USA Univ Houston Houston TX USA 77204 & Pharmaceut Sci, Houston, TX 77204 USA Mem Sloan Kettering Canc Ctr, Dept Neurol, Cotzias Lab Neurooncol, New York, NY 10021 USA Mem Sloan Kettering Canc Ctr New York NY USA 10021 New York, NY 10021 USA
Titolo Testata:
NEUROSCIENCE LETTERS
fascicolo: 3, volume: 299, anno: 2001,
pagine: 173 - 176
SICI:
0304-3940(20010223)299:3<173:OFANBA>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
OPIOID RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; KAPPA(3)-OPIOID RECEPTORS; NOCICEPTIN; BINDING; BRAIN; FQ;
Keywords:
orphan opioid receptor-like receptor; cAMP; homologous desensitization; kappa(3) opioid receptor;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Standifer, KM Univ Houston, Dept Pharmacol & Pharmaceut Sci, Houston, TX 77204 USA Univ Houston Houston TX USA 77204 ci, Houston, TX 77204 USA
Citazione:
J.P. Mathis et al., "Orphanin FQ/nociceptin and naloxone benzoylhydrazone activate distinct receptors in BE(2)-C human neuroblastoma cells", NEUROSCI L, 299(3), 2001, pp. 173-176

Abstract

kappa (3) opioid receptors have a unique binding and analgesic profile, asoriginally defined by naloxone benzoylhydrazone (NalBzoH). Although antisense studies demonstrated the close relationship between kappa (3) opioid and Orphan opioid receptor-like receptor (ORL1) and implied they were generated from the same gene, these studies also revealed differences in the sensitivity profiles of NalBzoH and orphanin FQ/nociceptin (OFQ/N), indicating that they were not identical. To help define the relationship between kappa (3) and ORL1 receptors, we utilized BE(2)-C human neuroblastoma cells that natively express functional ORL1 and kappa (3) opioid receptors. I-125-[Tyr(14)]OFQ/N binds to a single population of receptors in BE(2)-C cells. Competition binding and adenylyl cyclase studies clearly illustrated marked selectivity differences between the ORL1 and the kappa (3) sites. Furthermore,antisense DNA targeting ORL1 blocked the inhibition of cAMP by OFQ/N, but not by NalBzoH. Thus, the receptor mechanisms mediating the activity of OFQ/N and NalBzoH in BE(2)-C cells are distinct. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/07/20 alle ore 06:24:36