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Titolo:
COMPARISON OF BENZODIAZEPINE RECEPTOR LIGANDS WITH PARTIAL AGONISTIC,ANTAGONISTIC OR PARTIAL INVERSE AGONISTIC PROPERTIES IN PRECIPITATINGWITHDRAWAL IN SQUIRREL-MONKEYS
Autore:
MARTIN JR; JENCK F; MOREAU JL;
Indirizzi:
F HOFFMANN LA ROCHE & CO LTD,DIV PHARMA,BLDG 72-150,GRENZACHERSTR 124CH-4002 BASEL SWITZERLAND
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 275, anno: 1995,
pagine: 405 - 411
SICI:
0022-3565(1995)275:1<405:COBRLW>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
ABSTINENCE SYNDROME; RO 15-1788; DIAZEPAM; DEPENDENCE; RO-15-1788; CGS-8216; ABUSE; CATS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
19
Recensione:
Indirizzi per estratti:
Citazione:
J.R. Martin et al., "COMPARISON OF BENZODIAZEPINE RECEPTOR LIGANDS WITH PARTIAL AGONISTIC,ANTAGONISTIC OR PARTIAL INVERSE AGONISTIC PROPERTIES IN PRECIPITATINGWITHDRAWAL IN SQUIRREL-MONKEYS", The Journal of pharmacology and experimental therapeutics, 275(1), 1995, pp. 405-411

Abstract

Benzodiazepine receptor (BZR) ligands previously characterized as differing in intrinsic efficacy were evaluated first for potency in antagonizing flunitrazepam-induced sleep in monkeys. Data from these experiments were used to define approximately equieffective doses for subsequent use in precipitating withdrawal in diazepam-treated monkeys. It was shown that partial agonists with intermediate intrinsic efficacy (bretazenil, Ro 41-7812) were relatively ineffective in precipitating withdrawal reactions in diazepam-treated squirrel monkeys. The potent and specific BZR antagonist flumazenil, which possesses weak intrinsic efficacy, was more effective in precipitating a withdrawal reaction in diazepam-treated monkeys. In contrast, the highest dose of the BZR antagonist ZK 93426 that could be administered failed to precipitate withdrawal under the same experimental conditions. Finally, the BZR partial inverse agonist sarmazenil was the most effective of these BZR ligands in eliciting a precipitated withdrawal reaction. Thus, the results of the present investigation strongly suggest that BZR ligands differing in intrinsic efficacy differentially precipitate withdrawal in squirrel monkeys treated chronically with diazepam.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/20 alle ore 18:24:47