SKF-89976A hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的 GABA 转运蛋白 1 (GAT1) 抑制剂，对 hGAT1 的 IC50 为 0.13 uM。

A potent, selective and GABA transporter 1 (GAT1) inhibitor with IC50 of 0.13 uM for hGAT1; shows little to no activity for rGAT-2, hGAT-3 and hBGT-1 (IC50>500 uM); blocks GABA uptake and uncoupled transmitter-gated current with Ki of 7 uM and 0.03 uM, respectively.

SKF89976A has a 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, with IC50 values of 3514 , 202.13, and 728.8, respectively. 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. 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).

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

SKF89976A hydrochloride

Membrane Transporter/Ion Channel

GAT

GAT

Neurological Disease

——

85375-15-1

371.9003

C22H26ClNO2

>98% (HPLC)

DMSO: ≥ 34 mg/mL

O=C(C1CN(CC/C=C(C2=CC=CC=C2)/C3=CC=CC=C3)CCC1)O

3-Piperidinecarboxylic acid, 1-(4,4-diphenyl-3-buten-1-yl)-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years