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Titolo:
DIFFERENTIAL ANTAGONISM OF BREMAZOCINE-INDUCED AND U69,593-INDUCED ANTINOCICEPTION BY QUADAZOCINE - FURTHER FUNCTIONAL EVIDENCE OF OPIOD KAPPA-RECEPTOR MULTIPLICITY IN THE MOUSE
Autore:
HORAN PJ; DECOSTA BR; RICE K; HAASETH RC; HRUBY VJ; PORRECA F;
Indirizzi:
UNIV ARIZONA,ARIZONA MED CTR,DEPT PHARMACOL TUCSON AZ 85724 UNIV ARIZONA,ARIZONA MED CTR,DEPT PHARMACOL TUCSON AZ 85724 UNIV ARIZONA,ARIZONA MED CTR,DEPT CHEM TUCSON AZ 85724 NIADDKD,MED CHEM LAB BETHESDA MD 20892
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 2, volume: 266, anno: 1993,
pagine: 926 - 933
SICI:
0022-3565(1993)266:2<926:DAOBAU>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; BINDING-SITES; NALOXONE BENZOYLHYDRAZONE; BETA-FUNALTREXAMINE; SELECTIVE AGONIST; OPIATE RECEPTORS; RHESUS-MONKEYS; MU-OPIATE; LIGAND; DRUGS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
40
Recensione:
Indirizzi per estratti:
Citazione:
P.J. Horan et al., "DIFFERENTIAL ANTAGONISM OF BREMAZOCINE-INDUCED AND U69,593-INDUCED ANTINOCICEPTION BY QUADAZOCINE - FURTHER FUNCTIONAL EVIDENCE OF OPIOD KAPPA-RECEPTOR MULTIPLICITY IN THE MOUSE", The Journal of pharmacology and experimental therapeutics, 266(2), 1993, pp. 926-933

Abstract

In these studies, the antagonistic actions of methyl-2,6-methano-3-benzazocin-11-yl)-3-pentanone methanesulfonate (quadazocine) were evaluated against the kappa-receptor-mediated antinociceptive effects of i.c.v. rolidinylyl-oxaspiro(4,5)dec-8-yl)benzeneacetamide (U69,593) or bremazocine in the mouse warm water tail-flick test. Quadazocine produced no antinociceptive effects alone, and it selectively antagonized theactions of bremazocine, but not U69,593, in a dose- and time-related fashion, supporting previous suggestions of differences in kappa receptors mediating the antinociceptive effects of these agonists. Quadazocine, however, also antagonized the antinociceptive effects of both DAMGO (opioid mu agonist) and DPDPE (opioid delta agonist) at doses approximately 3-fold less than those needed to attenuate significantly the effects of bremazocine. The structurally diverse kappa opioids lidinyl)-cyclohexyl]benzo[b]-thiophene-4-acetamide (PD 117,302), ethylketocyclazocine (EKC) and tifluadom were studied under kappa-selective conditions, and the sensitivity of their effects to ro-N-[2(1-pyrrolidinyl)cyclohexyl]benzeneacetamide [(-)-UPHIT] (kappa1 antagonist) or quadazocine (kappa2 antagonist) was determined. On this basis PD 117,302, EKC and tifluadom were classified as acting at opioid kappa1, kappa1, and kappa2 receptors, respectively; EKC and tifluadom were also shown to have significant activity at opioid mu, but not delta, receptors. Thesedata demonstrating two-way differential antagonism of U69,593 and bremazocine by quadazocine and (-)-UPHIT provide strong functional evidence of opioid kappa receptor subtypes mediating supraspinal antinociception in the mouse. Additionally, the kappa-subtype classification of kappa agonists of different structures begins to provide a basis for structure-activity relationships of opioids acting at kappa1 and kappa2 receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 21:10:46