Alniditan

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Alniditan

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。

CAS NO:

152317-89-0

Alnitidan

Alniditan (Alnitidan) 是一种有效的5-HT_1B和5-HT_1D受体激动剂，在 HEK 293 细胞中，对人5-HT_1B和人5-HT_1D受体的IC₅₀分别为 1.7 nM 和 1.3 nM。Alniditan 具有预防偏头痛的作用。

生物活性

Alniditan (Alnitidan) is a potent5-HT_1Band5-HT_1Dreceptorsagonist, withIC₅₀s of 1.7 nM and 1.3 nM forh5-HT_1Bandh5-HT_1Dreceptorsin HEK 293 cells, respectively. Alniditan has migraine-preventive effects^[1]^[2].

IC₅₀& Target^[2]

human 5-HT_1BReceptor

1.7 nM (IC₅₀, in HEK 293 cell)

human 5-HT_1DReceptor

1.3 nM (IC₅₀, in HEK 293 cell)

5-HT_1BReceptor

0.9 nM (Kd)

5-HT_1DReceptor

1.2 nM (Kd)

体外研究
(In Vitro)

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^[1].

体内研究
(In Vivo)

The intraperitoneal administration of Alniditan ED₅₀=9 μg/kg dose dependly reduces [¹²⁵I]-BSA extravasation in the rat meninges when done 30 min before stimulation. Alniditan dose dependently attenuateds the neurogenic inflammation in vivo model of neurogenic inflammation^[1].

分子量

302.41

Formula

C₁₇H₂₆N₄O

CAS 号

152317-89-0

中文名称

阿尼地坦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.