PHARMACOLOGICAL ACTIVITIES OF CLOBAZAM AND DIAZEPAM IN THE RAT - RELATION TO DRUG BRAIN LEVELS

  • 1 January 1980
    • journal article
    • research article
    • Vol. 243  (2) , 275-283
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-demethylmetabolite 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 4-8 in the various tests. The results are discussed in relation to the importance of animal species selection for predicting favorable therapeutic effects in humans.

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