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Titolo:
Structure-activity relationship of [Nphe(1)]-NC-(1-13)-NH2, a pure and selective nociceptin/orphanin FQ receptor antagonist
Autore:
Guerrini, R; Calo, G; Bigoni, R; Rizzi, D; Regoli, D; Salvadori, S;
Indirizzi:
Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy Univ Ferrara Ferrara Italy I-44100 Sci Farmaceut, I-44100 Ferrara, Italy Ctr Biotechnol, Ferrara, Italy Ctr Biotechnol Ferrara ItalyCtr Biotechnol, Ferrara, Italy Dept Expt & Clin Med, Pharmacol Sect, Ferrara, Italy Dept Expt & Clin MedFerrara Italy Med, Pharmacol Sect, Ferrara, Italy
Titolo Testata:
JOURNAL OF PEPTIDE RESEARCH
fascicolo: 3, volume: 57, anno: 2001,
pagine: 215 - 222
SICI:
1397-002X(200103)57:3<215:SRO[AP>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
ORPHAN OPIOID RECEPTOR; MOUSE VAS-DEFERENS; GENE FAMILY; PHARMACOLOGICAL CHARACTERIZATION; TISSUE DISTRIBUTION; MOLECULAR-CLONING; ORL1 RECEPTORS; IN-VITRO; AGONIST; DISCOVERY;
Keywords:
[Nphe(1)]-NC(1-13)-NH2; nociceptin/orphanin FQ; ORL1 antagonists; ORL1 receptor; structure-activity relationships;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
47
Recensione:
Indirizzi per estratti:
Indirizzo: Salvadori, S Univ Ferrara, Dipartimento Sci Farmaceut, Via Fossato di Mortara 17-19, I-44100 Ferrara, Italy Univ Ferrara Via Fossato di Mortara 17-19Ferrara Italy I-44100
Citazione:
R. Guerrini et al., "Structure-activity relationship of [Nphe(1)]-NC-(1-13)-NH2, a pure and selective nociceptin/orphanin FQ receptor antagonist", J PEPT RES, 57(3), 2001, pp. 215-222

Abstract

A series of analogs of the ORL1 receptor antagonist [Nphe(1)]-NC(1-13)-NH2was prepared and tested for agonistic and antagonistic activities in the mouse vas deferens, a preparation that shows high sensitivity to nociceptin and related peptides. The purpose of this study was to determine the role of the aromatic residue at the N-terminal for antagonism and eventually identify compounds with improved potency. Results indicated that all 23 compounds are inactive as agonists, and the antagonistic potency of the initial template [Nphe(1)]-NC(1-13)-NH2 is high (pK(B) 6.43) compared with those of all other compounds except [(S)(beta Me)Nphe(1)]NC(1 -13)-NH2 (pK(B) 6.48). The other 22 compounds can be divided into two groups: 10 show antagonisticpotencies (pK(B)) ranging from 5.30 to 5.86, whereas the other 12 compounds are inactive. This study clearly shows that the aromatic ring of Nphe is very critical for the interaction with the ORL1 receptor and can not be enlarged or sterically modified without significant loss of antagonistic potency.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 01:05:55