Research Area: Neurological Disease
Biological Activity:
SKF 89976A is a GABA transporter type 1 inhibitor with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. It is selective for GAT-1. It inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo. [1]References on SKF 89976A HCl[1] Acta Physiol Scand. , 152(2):173-9, 1994 Oct.