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Titolo:
Characterization of [Nphe(1)]nociceptin(1-13)NH2, a new selective nociceptin receptor antagonist
Autore:
Calo, G; Guerrini, R; Bigoni, R; Rizzi, A; Marzola, G; Okawa, H; Bianchi, C; Lambert, DG; Salvadori, S; Regoli, D;
Indirizzi:
Univ Ferrara, Pharmacol Sect, Dept Expt & Clin Med, I-44100 Ferrara, ItalyUniv Ferrara Ferrara Italy I-44100 pt & Clin Med, I-44100 Ferrara, Italy Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy Univ Ferrara Ferrara Italy I-44100 harmaceut Sci, I-44100 Ferrara, Italy Univ Ferrara, Ctr Biotechnol, I-44100 Ferrara, Italy Univ Ferrara Ferrara Italy I-44100 tr Biotechnol, I-44100 Ferrara, Italy Univ Leicester, Leicester Royal Infirm, Dept Anaesthesia, Leicester LE1 5WW, Leics, England Univ Leicester Leicester Leics England LE1 5WW er LE1 5WW, Leics, England
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 6, volume: 129, anno: 2000,
pagine: 1183 - 1193
SICI:
0007-1188(200003)129:6<1183:CO[ANS>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
KAPPA-OPIOID RECEPTOR; ENDOGENOUS ORPHANIN FQ; ADENYLYL-CYCLASE; MICE LACKING; NALOXONE BENZOYLHYDRAZONE; MORPHINE ANALGESIA; PHOSPHOLIPASE-C; ORL1 RECEPTOR; IN-VITRO; RAT;
Keywords:
nociceptin; [Nphe(1)]nociceptin(1-13)NH2; nociceptin receptor antagonist; native and recombinant receptors; isolated tissues; mouse tail withdrawal assay; morphine, analgesia;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
48
Recensione:
Indirizzi per estratti:
Indirizzo: Calo', G Univ Ferrara, Pharmacol Sect, Dept Expt & Clin Med, Via Fossato Mortara 17, I-44100 Ferrara, Italy Univ Ferrara Via Fossato Mortara 17 Ferrara Italy I-44100 Italy
Citazione:
G. Calo' et al., "Characterization of [Nphe(1)]nociceptin(1-13)NH2, a new selective nociceptin receptor antagonist", BR J PHARM, 129(6), 2000, pp. 1183-1193

Abstract

1 Nociceptin (orphanin FQ) is a novel neuropeptide capable of inducing a variety of biological actions via activation of a specific G-protein coupledreceptor. However, the lack of a selective nociceptin receptor antagonist has hampered our understanding of nociceptin actions and the role of this peptide in pathophysiological states. As part of a broader programme of research, geared to the identification and characterization of nociceptin receptor ligands, we report that the novel peptide [Nphe(1)]nociceptin(1-13)NH2 acts as the first truly selective and competitive nociceptin receptor antagonist and is devoid of any residual agonist activity.2 [Nphe(1)]nociceptin(1-13)NH2 binds selectively to recombinant nociceptinreceptors expressed in Chinese hamster ovary (CHO) cells (pK(i) 8.4) and competitively antagonizes the inhibitory effects of nociceptin (i) on cyclicAMP accumulation in CHO cells (pA(2) 6.0) and (ii) on electrically evoked contractions in isolated tissues of the mouse, rat and guinea-pig with pA(2) values ranging from 6.0 to 6.4.3 [Nphe(1)]nociceptin(1-13)NH2 is also active in vivo, where it prevents the pronociceptive and antimorphine actions of intracerebroventricularly applied nociceptin, measured in the mouse tail withdrawal assay. Moreover, [Nphe(1)]nociceptin(1-13)NH2 produces per se a dose dependent, naloxone resistant antinociceptive action and, at relatively low doses, potentiates morphine-induced analgesia.4 Collectively our data indicate that [Nphe(1)]nociceptin(1-13)NH2, actingas a nociceptin receptor antagonist, may be the prototype of a new class of analgesics.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 19:27:59