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Competitive Inhibition of γ‐Aminobutyric Acid Synaptosomal Uptake by 4‐(4′‐Azidobenzoimidylamino)butanoic Acid
Author(s) -
Tunnicliff Godfrey,
Ngo That T.
Publication year - 1982
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1982.tb11488.x
Subject(s) - nipecotic acid , aminobutyric acid , chemistry , biochemistry , non competitive inhibition , stereochemistry , neurotransmitter , enzyme , receptor
4‐(4′‐Azidobenzoimidylamino)butanoic acid (ABBA) is a potent inhibitor of rat brain synaptosomal [ 3 H]γ‐aminobutyric acid uptake. K 1 values were calculated to be 8 μM and 16 μM 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.