TTA-A2 是一种选择性 T 型钙通道拮抗剂，是一种有效的抗惊厥药，可减少孕烷 X 受体的激活。它对 Cav3.1 (a1G) 和 Cav3.2 (a1H) 通道在 -80 mV 和- 100 mV 保持电位上具有同样的作用，IC50 值分别为 89 和 92 nM。它可用于多种人类神经系统疾病的研究，包括睡眠障碍和癫痫。

TTA-A2 is a selective T-type calcium channel antagonist as a potent anticonvulsant that the Cav3.1 isoform plays a prominent role in mediating. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

TTA-A2 (oral gavage; 10 mg/kg; once daily; 5 days) shows selective effect on recurrent thalamocortical network activity, it suppresses active wake and promotes slow-wave sleep in wild-type mice but not in mice lacking both Cav3.1 and Cav3.3[1].TTA-A2 (oral gavage;?3 mg/kg;?single dose) produces significant changes in sleep architecture in rats.?A reduction in active wake soon after dosing with a concurrent increase in delta sleep and decrease in REM sleep.?Additionally, these effects persists for up to 4 h post-dose in rats[2].

953778-63-7

C20H21F3N2O2

378.395

DMSO:10 mM
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