Involvement of gamma-amino butyric acid (GABA) in the anticonvulsant action of methaqualone.
The effects of methaqualone on isonicotinic acid hydrazide, 6-mercapto propionic acid, picrotoxin, and strychnine-induced convulsion were studied in mice and the results compared with diazepam. Methaqualone, like diazepam, was found to be a selective antagonist of isoniazid-induced convulsion and a much less effective inhibitor of strychnine convulsion. Methaqualone elicits muscle-relaxant, sedative, and anticonvulsant effects at different dose levels. At low, nonsedative doses the drug produces anticonvulsant effects, and at higher doses, muscle-relaxant and sedative effects. It appears that the mechanism(s) of action of methaqualone in on GABA deficiency or receptor blockade, rather than on glycine receptors.
D000613:Aminobutyrates / Q000502:physiology*; D000818:Animals; D000927:Anticonvulsants; D001923:Brain Chemistry; D002531:Cerebellum / Q000378:metabolism; D003975:Diazepam / Q000494:pharmacology; D006993:Hypnotics and Sedatives; D008297:Male; D008702:Methaqualone / Q000494:pharmacology*; D009126:Muscle Relaxation / Q000187:drug effects; D010634:Phenobarbital / Q000494:pharmacology; D051381:Rats; D012640:Seizures / Q000139:chemically induced; D005680:gamma-Aminobutyric Acid / Q000502:physiology*
D000613:Aminobutyrates; D000927:Anticonvulsants; D006993:Hypnotics and Sedatives; D005680:gamma-Aminobutyric Acid; D008702:Methaqualone; D003975:Diazepam; D010634:Phenobarbital