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Titolo:
LACK OF CROSS-TOLERANCE BETWEEN U69,593 AND BREMAZOCINE SUGGESTS KAPPA-OPIOID RECEPTOR MULTIPLICITY IN MICE
Autore:
HORAN PJ; PORRECA F;
Indirizzi:
UNIV ARIZONA,HLTH SCI CTR,DEPT PHARMACOL TUCSON AZ 85721 UNIV ARIZONA,HLTH SCI CTR,DEPT PHARMACOL TUCSON AZ 85721
Titolo Testata:
European journal of pharmacology
fascicolo: 1-3, volume: 239, anno: 1993,
pagine: 93 - 98
SICI:
0014-2999(1993)239:1-3<93:LOCBUA>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; NALOXONE BENZOYLHYDRAZONE; NOR-BINALTORPHIMINE; DELTA-RECEPTOR; BINDING-SITES; SPINAL-CORD; OPIATE; SUBTYPES; AGONIST; LIGAND;
Keywords:
KAPPA-OPIOID RECEPTORS; ANTINOCICEPTION; ARYLACETAMIDES; BENZOMORPHANS; (MOUSE);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
P.J. Horan e F. Porreca, "LACK OF CROSS-TOLERANCE BETWEEN U69,593 AND BREMAZOCINE SUGGESTS KAPPA-OPIOID RECEPTOR MULTIPLICITY IN MICE", European journal of pharmacology, 239(1-3), 1993, pp. 93-98

Abstract

The development of tolerance, and the possibility of cross-tolerance,to the kappa-opioid receptor-mediated antinociceptive effects of U69,593 and bremazocine was studied in mice. U69,593 and bremazocine elicited dose-related and kappa-receptor-mediated antinociception followingi.c.v. administration to mice. After a 3 day treatment regimen (twicedaily injections) with an approximate antinociceptive A90 dose (90 nmol, i.c.v.) of U69,593, tolerance developed as demonstrated by a 5.6-fold rightward shift of the U69,593 dose-response line. The i.c.v. dose-response line for bremazocine was unaltered in U69,593-tolerant mice. Pretreatment with an approximate antinociceptive A90 dose of bremazocine (30 nmol, i.c.v.) for 3 days also produced tolerance as shown by agreater than 15-fold rightward shift in the bremazocine antinociceptive dose-response line. The i.c.v. dose-response line for U69,593 was unaltered in bremazocine-tolerant mice. These data demonstrate that while tolerance develops to the antinociceptive effects of both U69,593 and bremazocine, a two-way lack of cross-tolerance can be demonstrated between these kappa-agonists in this endpoint. These data suggest mechanistic differences in the antinociceptive effects of these kappa-agonists. Such suggestions are consistent with antinociceptive action of these agonists at subtypes of kappa-receptors.

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Documento generato il 14/08/20 alle ore 16:13:41