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152317-89-0

中文名稱 152317-89-0
英文名稱 Alniditan
CAS 152317-89-0
分子式 C17H26N4O
分子量 302.41
MOL 文件 152317-89-0.mol
152317-89-0 結(jié)構(gòu)式 152317-89-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T14190
英文別名
Alnitidan
1,3-Propanediamine, N1-[[(2R)-3,4-dihydro-2H-1-benzopyran-2-yl]methyl]-N3-(1,4,5,6-tetrahydro-2-pyrimidinyl)-

物理化學性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜

常見問題列表

生物活性
Alnitidan是5-HT1B/1D受體的有效抑制劑,pKi值分別為8.96和9.40;在HEK?293細胞中,IC50值分別為1.7和1.3 nM。
靶點

5-HT 1B Receptor

1.7 nM (IC 50 , in HEK?293 cell)

5-HT 1D Receptor

1.3 nM (IC 50 , in HEK?293 cell)

體外研究

In vitro, alniditan exhibits little vasoconstrictive effects on the rat basilar artery, although at a very high concentration 1 mM, alniditan causes intensive constriction, most likely through a mechanism independent from 5-HT receptor activation. Alniditan is 10 times more potent than sumatriptan at the h5-HT1B receptor, and twice as potent at the h5-HT 1D receptor.

體內(nèi)研究

The intraperitoneal administration of alniditan ED 50 =9 μg/kg and sumatriptan ED 50 =70 μg kg dose dependly reduces [ 125 I]-BSA extravasation in the rat meninges when done 30 min before stimulation. The estimated ED values for alniditan are 9 μg/kg in the absence and 190 μg/kg in the presence of GR 127935. Alniditan (3, 10, 30 and 100 μg/kg) produces a dose-dependent increase in the arteriovenous oxygen saturation difference, which seems to be attenuated in animals treated with GR127935. Alniditan dose-dependently decreases total carotid and arteriovenous anastomotic blood flow and concomitant conductance values; nutrient blood flow and conductance increase. Alniditan also produces significant increases in vascular conductance to the skin, ear, bone, salivary gland, fat, tongue, brain and dura mater; no changes are observed in the muscles and eyes.

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