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Alniditan

CAS No. : 152317-89-0

MCE 站：Alniditan

产品活性：Alnitidan是5-HT_1B/1D受体的有效抑制剂，pK_i值分别为8.96和9.40；在HEK?293细胞中，IC₅₀值分别为1.7和1.3 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

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. Alniditan is 10 times more potent than sumatriptan at the h5-HT1B receptor, and twice as potent at the h5-HT_1D receptor.

In Vivo: The intraperitoneal administration of alniditan ED₅₀=9 μg/kg and sumatriptan ED₅₀=70 μg kg dose dependly reduces [¹²⁵I]-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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