Interaction of Convulsive Ligands with Benzodiazepine Receptors

作者：C. Bræstrup, Ralph Schmiechen, Günter Neef, Mogens Brøndsted Nielsen, Erling N. Petersen · 发表于：Science · 年份：1982 · DOI：10.1126/science.6281892 · 被引用次数：548 · 研究领域：Synthesis and pharmacology of benzodiazepine derivatives

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.