A partial agonist at the anticonvulsant benzodiazepine receptor: reversal of the anticonvulsant effects of Ro 15-1788 with CGS-8216.
A benzodiazepine antagonist (Ro 15-1788) prevents the development of kindled seizures. CGS-8216, another benzodiazepine antagonist, prevents DMCM-induced seizures (indicating that CGS-8216 acts at a benzodiazepine receptor) but has no effect on kindling or kindled seizures. CGS-8216 prevents the anticonvulsant actions of Ro 15-1788 suggesting that Ro 15-1788 is a partial agonist at an anticonvulsant benzodiazepine receptor. These results support that idea of of distinct, separate receptors for anticonvulsant and sedative effects of benzodiazepines.
D000679:Amygdala / Q000187:drug effects*; D000818:Animals; D001570:Benzodiazepinones / Q000037:antagonists & inhibitors*; D003292:Convulsants / Q000494:pharmacology*; D005442:Flumazenil; D007696:Kindling, Neurologic / Q000187:drug effects*; D008297:Male; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000187:drug effects*; D011963:Receptors, GABA-A
D001570:Benzodiazepinones; D003292:Convulsants; D011720:Pyrazoles; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D005442:Flumazenil; C033830:2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one