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June 1, 1985Journal of Medicinal Chemistry

3-Amino-.beta.-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam

Robert H. Dodd C. Ouannés Lia Prado de Carvalho Anne Valin Patrice Venault Georges Chapouthier Jean Rossier Pierre Potìer

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Abstract

Seven 3-N-substituted derivatives of 3-amino-beta-carboline were synthesized and their affinities for the benzodiazepine receptor were assessed in vitro. Two compounds, 3-(ethylamino)-beta-carboline and 3-[(methoxycarbonyl)amino]-beta-carboline (beta-CMC), showing IC50 values of 460 and 71 nM, respectively, were selected for in vivo studies. The former compound showed long-lasting proconvulsant activity in Papio papio baboons while beta-CMC was shown in mice to selectively antagonize the sedative effects of diazepam without exhibiting convulsant, proconvulsant, or anxiogenic activity by itself.

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Dodd et al. (1985) studied this question.

synapsesocial.com/papers/6a998ecd0e148c09fcabaabd https://doi.org/10.1021/jm00383a024

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