Tasipimidine

Chemical Structure : Tasipimidine

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货号: PC-47093Not For Human Use, Lab Use Only.

Tasipimidine is a potent, selective and orally active human α2A-adrenoceptor agonist with pEC50 of 7.57, >100-fold selectivity over α2B-and α2C-adrenoceptors and the rodent α2D-adrenoceptor.

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生物&药学活性

Tasipimidine is a potent, selective and orally active human α2A-adrenoceptor agonist with pEC50 of 7.57, >100-fold selectivity over α2B-and α2C-adrenoceptors and the rodent α2D-adrenoceptor.
Tasipimidine had no functional effects in the LNCaP cells expressing endogenously the human α1A-adrenoceptors but was a weak agonist in the Chem-1 cells coexpressing Gα15 protein and α1A-adrenoceptors.
Tasipimidine was a full agonist in the intracellular [Ca2+] assay, and a weak partial agonist in the inositol monophosphate accumulation assay.
Tasipimidine prolonged ejaculation latency and the interintromission interval at the dose of 200 µg/kg in the control of ejaculation and sexual incentive motivation in rats.

物理化学性质&存储条件

分子量	232.283
分子式	C13H16N2O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(5-methoxy-3,4-dihydro-1H-isochromen-1-yl)-4,5-dihydro-1H-imidazole

参考文献

1. Lehtimäki J, et al. Eur J Pharmacol. 2022 May 15;923:174949.

2. Lehtimäki J, et al. J Sex Med. 2021 Oct;18(10):1677-1689.

Tasipimidine

生物&药学活性

物理化学性质&存储条件

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Tasipimidine

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