Pharmacological activities of clobazam and diazepam in the rat: Relation to drug brain levels

S. Caccia, M. Carli, S. Garattini, E. Poggesi, R. Rech, R. Samanin

Research output: Contribution to journalArticle

Abstract

Brain distribution and various pharmacological effects of clobazam and diazepam were studied in rats. When given at 10 mg/kg i.p. the compounds reached peak brain levels 15 min after injection, and showed similar half lives. At peak time brain levels were proportional to the dose administered. Very little of the N-desmethylmetabolite of each compound was found in the brain. Clobazam was less effective than diazepam in protecting rats from pentetrazol convulsions, disrupting rota-rod performance and increasing punished responses in a 'conflict' test, the relative potencies ranging from 4 to 8 in the various tests. The results are discussed in relation to the importance of animal species selection for predicting favourable therapeutic effects in humans.

Original languageEnglish
Pages (from-to)275-283
Number of pages9
JournalArchives Internationales de Pharmacodynamie et de Therapie
Volume243
Issue number2
Publication statusPublished - 1980

ASJC Scopus subject areas

  • Pharmacology

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