152317-89-0
| 中文名称 | 152317-89-0 |
|---|---|
| 中文同义词 | 化合物 T14190;化合物 ALNIDITAN |
| 英文名称 | Alniditan |
| 英文同义词 | 1,3-Propanediamine, N1-[[(2R)-3,4-dihydro-2H-1-benzopyran-2-yl]methyl]-N3-(1,4,5,6-tetrahydro-2-pyrimidinyl)-;Alnitidan |
| CAS号 | 152317-89-0 |
| 分子式 | C17H26N4O |
| 分子量 | 302.41 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 152317-89-0.mol |
| 结构式 |  |
152317-89-0 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
|
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) |
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.
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.