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Science 11 June 1982:
Vol. 216. no. 4551, pp. 1241 - 1243
DOI: 10.1126/science.6281892
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Articles

Science, Vol 216, Issue 4551, 1241-1243
Copyright © 1982 by American Association for the Advancement of Science

articles

Interaction of convulsive ligands with benzodiazepine receptors

C Braestrup, R Schmiechen, G Neef, M Nielsen, and EN Petersen

The gamma-aminobutyric acid (GABA)-benzodiazepine receptor complex, which is composed of distinct proteins embedded in the neuronal plasma membrane, is important for several effects of benzodiazepines, including protection afforded against convulsions. During structural modification of ethyl beta-carboline-3-carboxylate an agent was discovered which has high affinity for brain benzodiazepine receptors but which is a potent convulsant. Also in contrast to benzodiazepines, this type of benzodiazepine receptor ligand favors benzodiazepine receptors in the non-GABA-stimulated conformation, which may explain the convulsive properties.


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