Publication Date:
1982-06-11
Description:
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.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Braestrup, C -- Schmiechen, R -- Neef, G -- Nielsen, M -- Petersen, E N -- New York, N.Y. -- Science. 1982 Jun 11;216(4551):1241-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6281892" target="_blank"〉PubMed〈/a〉
Keywords:
Allosteric Regulation
;
Animals
;
Carbolines/*metabolism
;
Cerebellum/metabolism
;
*Convulsants
;
Indoles/*metabolism
;
Ligands
;
Macromolecular Substances
;
Neural Inhibition
;
Rats
;
Receptors, Cell Surface/*metabolism
;
Receptors, Drug/classification/*metabolism
;
Receptors, GABA-A
Print ISSN:
0036-8075
Electronic ISSN:
1095-9203
Topics:
Biology
,
Chemistry and Pharmacology
,
Computer Science
,
Medicine
,
Natural Sciences in General
,
Physics
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