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Hypotaurine is an endogenous inhibitory amino acid.1 It inhibits GABA uptake by mouse GABA transporter 1 (GAT1), GAT2, GAT3, and GAT4 (IC50s = 170, 240, 4.9, and 8.1 μM, respectively) and rat GAT1, GAT2, and GAT3 (IC50s = 1,010, 52, and 73 μM, respectively). Hypotaurine also inhibits GABA uptake by betaine/GABA transporter 1 (BGT1) in L-M(TK-) cells expressing the human transporter (IC50 = 380 μM).2 It inhibits sodium-stimulated GABA uptake by rabbit choroid plexus slices (IC50 = 21.9 μM).3 It scavenges hypochlorous acid (HOCl) and hydroxyl, but not superoxide, radicals in cell-free assays.4 Hypotaurine (1 mM) protects rat TR-TBT 18d-1 placental trophoblasts from hydrogen peroxide-induced cell death.5
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1. Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4. Eur. J. Pharmacol. 519(1-2), 43-47 (2005).
2. Cloning and expression of a betaine/GABA transporter from human brain. J. Neurochem. 64(3), 977-984 (1995).
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4. The antioxidant action of taurine, hypotaurine and their metabolic precursors. Biochem. J. 256(1), 251-255 (1988).
5. Protective effect of hypotaurine against oxidative stress-