Competitive inhibition of gamma-aminobutyric acid synaptosomal uptake by 4-(4'-azidobenzoimidylamino)butanoic acid.
4-(4'-Azidobenzoimidylamino)butanoic acid (ABBA) is a potent inhibitor of rat brain synaptosomal [3H]gamma-aminobutyric acid uptake. Ki values were calculated to be 8 microM and 16 microM with respect to the high-affinity and the low-affinity uptake processes. These values are of the same order as those reported for nipecotic acid and guvacine, which until now have been the most potent uptake inhibitors available. Since ABBA contains a phenyl group, it might be capable of penetrating the blood-brain barrier, thus becoming a useful GABA mimetic.
D000818:Animals; D001386:Azides / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D018756:GABA Antagonists; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism*
C035781:4-(4'-azidobenzoimidylamino)butanoic acid; D001386:Azides; D018756:GABA Antagonists