Stereospecificity of 2,4-diaminobutyric acid with respect to inhibition of 4-aminobutyric acid uptake and binding.
S(+)-2,4-Diaminobutyric acid is at least 20 times more potent than the R(-) stereoisomer as an inhibitor of the sodium-dependent uptake of 4-aminobutyric acid (GABA) in rat brain slices. Both isomers, however, are equipotent as inhibitors of sodium-independent binding of GABA to membranes from rat brain. The latter finding may be relevant to the reported neurotoxicity in rats of both isomers of 2,4-diaminobutyric acid after intracisternal injection.
D000613:Aminobutyrates / Q000378:metabolism* / Q000494:pharmacology*; D000818:Animals; D001692:Biological Transport; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D066298:In Vitro Techniques; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D000613:Aminobutyrates; D005680:gamma-Aminobutyric Acid