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SKF89976A hydrochloride

CAS No. : 85375-15-1

MCE 站：SKF89976A hydrochloride

产品活性：SKF89976A hydrochloride 是一种选择性 GABA 转运蛋白 GAT-1 抑制剂，作用于 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。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：GABA Receptor

In Vitro: 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).

In Vivo: 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.

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