SKF89976A hydrochloride 是GABA转运蛋白GAT-1的选择性抑制剂，抑制 CHO 细胞中的 GAT-1，GAT-2 和 GAT-3，IC50分别为 0.28 μM，137.34 μM 和 202.8 μM。

SKF89976A hydrochloride is a selective inhibitor GABA transporter such as GAT-1 (IC50s = 0.28 μM), GAT-2 (IC50s = 137.34 μM) and GAT-3(IC50s = 202.8 μM) in CHO cells.

SKF89976A with weak antiallodynic action. SKF89976A weakly inhibits serotonin transporter (SERT), noradrenaline transporter (NET), and dopamine transporter (DAT) in chinese hamster ovary (CHO) cells stably expressing each transporter using a substrate uptake assay(IC50 values of 3514 , 202.13, and 728.8, respectively)[1]. SKF89976A is a GABA-transport blocker. GABA (1 mM) elicited an inward current that is completely suppressed by the GABA transport inhibitors tiagabine (10 μM) and SKF89976A (100 μM), but is unaffected by 100 μM picrotoxin. 100 μM SKF 89976-A is known to block the transport of GABA into cells, completely eliminated the GABA-elicited current in a reversible fashion[2]. SKF89976A is a nontransportable blockers of GAT-1. SKF89976-A also suppresses baseline inward currents that likely result from tonic GAT activation by background GABA. SKF89976A (100 μM) reversibly reduces GAT currents in every studied cell by 67.9±4.4% (n=19). Intracellular perfusion of 20 μM SKF89976-A progressively reduced and blocked GABA-induced GAT currents without blocking GABAAR-mediated currents (n=4)[3].

When administered i.v. (0.3 mg/kg), SKF89976A produces a weak antiallodynic response . The i.t. injection of SKF89976A dose-dependently ameliorates the reduction in the withdrawal threshold in PSL model mice[1].

85375-15-1

C22H26ClNO2

371.9

d,l-SKF89976A hydrochloride

H2O:20 mg/mL (53.78 mM),Need ultrasonic
DMSO:100 mg/mL (268.89 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years