Abstract

A method for intravenous infusion of reverse agonists of the GABA-receptor complex (bicuculline, pentylentetrazol, and others) was used to examine the pharmacodynamics and pharmacokinetics of GABA-receptor complex agonists (benzodiazepines and barbiturates) and aliphatic alcohols in mice. A correlation was observed between the recorded indicators of convulsive seizures in intact mice and those administered ethanol or phenazepam. The dose—effect relationship and concentration ratios of the labeled analogs of the studied compounds were estimated in the brain and blood plasma to assess their distribution in the body. Examples of tests for the pharmacokinetics of ethanol, phenazepam, and their14C-analogs in mice are given.

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