Pharmacokinetics and in vitro effects of a 4-aminobutyric acid derivative with anticonvulsant action.
N-trimethyl-acetyl-4-aminobutyric acid, called PG2, is a new anticonvulsant acting as a 4-aminobutyric acid (GABA) pro-drug. The stimulatory effect of PG2 on synaptosomal 14C-GABA release and its inhibitory effect of synaptosomal 14C-GABA uptake were studied together with its pharmacokinetics after intracardiac and oral administration to rat. PG2 is a weak inhibitor of the GABAse system in vitro with an apparent Ki value of 0.83 mmol/l.
D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism* / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013574:Synaptosomes / Q000378:metabolism; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology
D000927:Anticonvulsants; D005680:gamma-Aminobutyric Acid; C038979:pivagabine