Publication Date:
1982-06-11
Description:
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.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Bowling, A C -- DeLorenzo, R J -- NS 1352/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1982 Jun 11;216(4551):1247-50.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6281893" target="_blank"〉PubMed〈/a〉
Keywords:
Animals
;
Benzodiazepines/*metabolism/pharmacology
;
Benzodiazepinones/metabolism
;
Brain/*metabolism
;
Calmodulin/antagonists & inhibitors
;
Diazepam/metabolism
;
Kinetics
;
Ligands
;
Protein Kinase Inhibitors
;
Rats
;
Receptors, Drug/*metabolism
;
Receptors, GABA-A
;
Structure-Activity Relationship
Print ISSN:
0036-8075
Electronic ISSN:
1095-9203
Topics:
Biology
,
Chemistry and Pharmacology
,
Computer Science
,
Medicine
,
Natural Sciences in General
,
Physics
