A GABA receptor modulator
(R)-4-Amino-3-hydroxybutyric acid is a GABA receptor modulator.1 It binds to GABAA and GABAB receptors (IC50s = 1 and 0.35 µM, respectively) and inhibits GABA uptake in rat brain synaptosomes (IC50 = 67 µM). (R)-4-amino-3-hydroxybutyric acid is also a GABAC receptor agonist that induces currents in a patch-clamp assay using Xenopus oocytes expressing the human receptor (EC50 = 19 µM).2 In vivo, (R)-4-amino-3-hydroxybutyric acid (20 mg/animal) inhibits electrical discharges in the amygdala in a cat model of N-amidinobenzamide-induced seizures.3
1.Falch, E., Hedegaard, A., Nielsen, L., et al.Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparationsJ. Neurochem.47(3)898-903(1986) 2.Hinton, T., Chebib, M., and Johnston, G.A.R.Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABAC receptorsBioorg. Med. Chem. Lett.18(1)402-404(2008) 3.Katayama, Y., and Mori, A.Inhibitory action of (3R)-(-)-4-amino-3-hydroxybutanoic acid on N-amidinobenzamide induced seizure activity in cat brainIRCS Med. Sci.5(9)437(1977)
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