The picrotoxin-like action of a convulsant benzodiazepine, Ro5-3663.
The potency and site of action of Ro5-3663 as a GABA antagonist were investigated in the rat cuneate slice in vitro. A Schild plot for Ro5-3663 was clearly non-linear but enabled a pA2 value of 3.97 to be calculated. Combination studies using the 'classical' GABA antagonists bicuculline and picrotoxin indicated that Ro5-3663 acted at a separate site from bicuculline, but may share a common site with picrotoxin.
D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology*; D001640:Bicuculline / Q000494:pharmacology; D003292:Convulsants / Q000494:pharmacology*; D066298:In Vitro Techniques; D008526:Medulla Oblongata / Q000378:metabolism; D009118:Muscimol / Q000494:pharmacology; D009474:Neurons / Q000378:metabolism; D010852:Picrotoxin / Q000494:pharmacology*; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism; D011963:Receptors, GABA-A
D001570:Benzodiazepinones; D001640:Bicuculline; D003292:Convulsants; D009118:Muscimol; D010852:Picrotoxin; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; C022193:Ro 5-3663