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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Dodd RH,Ouannès C,de Carvalho LP,Valin A,Venault P,Chapouthier G,Rossier J,Potier P

doi

10.1021/jm00383a024

subject

Has Abstract

pub_date

1985-06-01 00:00:00

pages

824-8

issue

6

eissn

0022-2623

issn

1520-4804

journal_volume

28

pub_type

杂志文章

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