TTA-Q6 是 T 型 Ca2+ 通道的选择性拮抗剂，可用于神经学研究。
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].
参考文献:
[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]。
| Animal experiment [1]: | |
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Animal models |
WAG/Rij epilepsy model SD rat |
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Preparation Method |
To evaluate the effects of T-type antagonists on sleep and wake, telemetric recordings of electrocorticogram (ECoG) and electromyogram (EMG) signals were measured in rats. In a 7 day crossover design, vehicle or TTA-Q6 was dosed orally every day, 30 min before the inactive phase. The ECoG and EMG signals were collected and scored for the amount of time awake or each phase of sleep. |
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Dosage form |
10 mg/kg TTA-Q6 orally every day for 7 days |
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Applications |
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. |
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参考文献: [1]. 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. |
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