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TTA-Q6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TTA-Q6图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍

TTA-Q6 is a selective antagonist of T-type Ca2+ channel and can be used in neurological research.

Animal models

WAG/Rij epilepsy model SD rat

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.

Dosage form

10 mg/kg TTA-Q6 orally every day for 7 days

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.

产品描述

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.