Micromolar Affinity Benzodiazepine Receptors: Identification and Characterization in Central Nervous System
- 11 June 1982
- journal article
- research article
- Published by American Association for the Advancement of Science (AAAS) in Science
- Vol. 216 (4551), 1247-1250
- https://doi.org/10.1126/science.6281893
Abstract
Receptors that selectively bind micromolar concentrations of benzodiazepines are present in rat brain membrane. These micromolar receptors exhibit saturable, stereospecific binding, and the potency of benzodiazepine binding to these receptors is correlated with the ability of the benzodiazepines to inhibit maximum electric shock-induced convulsions. Benzodiazepine receptors with nanomolar affinity differ from the micromolar receptors in their binding, kinetic, and pharmacologic characteristics. The micromolar receptors also bind phenytoin, a non-benzodiazepine anticonvulsant. These results provide evidence for a distinct class of clinically relevant benzodiazepine receptors that may regulate neuronal excitability and anticonvulsant activity.This publication has 22 references indexed in Scilit:
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