Effect of elevated brain GABA concentrations on the actions of bicuculline and picrotoxin in mice.
gamma-Acetylenic GABA and gamma-vinyl GABA, two catalytic irreversible inhibitors of mammalian brain GABA transaminase that produce several-fold increases in brain GABA concentrations were tested for their effects on bicuculline and picrotoxin-induced seizures and mortality in mice. Neither inhibitor influenced the frequency of seizures or death produced by either bicuculline or picrotoxin. Both inhibitors, however, produced a dose-dependent prolongation of the time to onset of seizures and death induced by picrotoxin but by bicuculline. These results suggest differences in the antagonism by bicuculline and picrotoxin of GABA-mediated neural functions.
D000613:Aminobutyrates / Q000494:pharmacology*; D000818:Animals; D001640:Bicuculline / Q000008:administration & dosage / Q000037:antagonists & inhibitors*; D001921:Brain / Q000378:metabolism*; D007274:Injections, Intraperitoneal; D007546:Isoquinolines / Q000037:antagonists & inhibitors*; D008297:Male; D051379:Mice; D010852:Picrotoxin / Q000008:administration & dosage / Q000037:antagonists & inhibitors*; D009435:Synaptic Transmission / Q000187:drug effects; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology*
D000613:Aminobutyrates; D001640:Bicuculline; D007546:Isoquinolines; D010852:Picrotoxin; D005680:gamma-Aminobutyric Acid