SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo. References: Stringer JL, Aribi AM. Modulation of the in vivo effects of gabapentin by vigabatrin and SKF89976A. Epilepsy Res. 2002 Dec;52(2):129-37. PubMed PMID: 12458029.
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CAS:85375-15-1