Evidence for the pharmacological relevance of benzodiazepine receptors to anticonvulsant activity.
Each of a series of benzodiazepines was found to be effective in preventing convulsions evoked by intermittent photic stimulation of epileptic chickens. There was a high correlation between the anticonvulsant potencies (mean effective dosages) and the affinity of the agents for the putative benzodiazepine receptor as measured by displacement of [3H]diazepam from binding sites on chicken synaptosomal membranes. This correlation in a genetic model of epilepsy provides further evidence that benzodiazepines exert their anticonvulsant effects by interacting with the benzodiazepine receptor.
Fisher
T E
TE
Johnson
D D
DD
Tuchek
J M
JM
Crawford
R D
RD
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D000927:Anticonvulsants / Q000494:pharmacology*; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D002645:Chickens; D003975:Diazepam / Q000378:metabolism; D066298:In Vitro Techniques; D011963:Receptors, GABA-A / Q000187:drug effects*; D013570:Synaptic Membranes / Q000378:metabolism; D013574:Synaptosomes / Q000378:metabolism
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D011963:Receptors, GABA-A; D003975:Diazepam