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Science 11 June 1982:
Vol. 216. no. 4551, pp. 1247 - 1250
DOI: 10.1126/science.6281893
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Articles

Science, Vol 216, Issue 4551, 1247-1250
Copyright © 1982 by American Association for the Advancement of Science

articles

Micromolar affinity benzodiazepine receptors: identification and characterization in central nervous system

AC Bowling and RJ DeLorenzo

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.


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