TTA-Q6 is a selective antagonist of T-type Ca2+ channel and can be used in neurological research[1].
TTA-Q6 displayed good overall profiles and were examined in several in vivo assays responsive to T-type calcium channel antagonists. It showed robust inhibition of seizures in the WAG/Rij epilepsy model after oral dosing at 3 mg/kg. A 10 mg/kg dose of TTA-Q6 to rats right before their sleep period produced a further suppression of active wake for 0.5-2 h after dosing[2]. TTA-Q6 dose-dependently reduced amphetamine-induced psychomotor activity[3].
References:
[1]: Schlegel KA, Yang ZQ, et,al.Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8. PMID: 20673719.
[2]: Barrow JC, Rittle KE, et,al. Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists. ACS Med Chem Lett. 2010 Feb 1;1(2):75-9. doi: 10.1021/ml100004r. PMID: 24900180; PMCID: PMC4007971.
[3]: Uslaner JM, Smith SM, et,al. T-type calcium channel antagonism produces antipsychotic-like effects and reduces stimulant-induced glutamate release in the nucleus accumbens of rats. Neuropharmacology. 2012 Mar;62(3):1413-21. doi: 10.1016/j.neuropharm.2010.11.015. Epub 2010 Nov 24. PMID: 21110986.
TTA-Q6是T型Ca2+通道的选择性拮抗剂，可用于神经学研究[1]。
TTA-Q6 显示出良好的整体特征，并在几种对 T 型钙通道拮抗剂有反应的体内试验中进行了检查。在 WAG/Rij 癫痫模型中，口服给药 3 mg/kg 后，它显示出对癫痫发作的强烈抑制作用。在大鼠睡眠期前给予 10 mg/kg 剂量的 TTA-Q6 会在给药后 0.5-2 小时进一步抑制主动觉醒[2]。 TTA-Q6 剂量依赖性地降低苯丙胺诱导的精神运动活动[3]。