Alniditan

Alniditan (Alnitidan) is a potent 5-HT_1B and 5-HT_1D receptors agonist, with IC₅₀s of 1.7 nM and 1.3 nM for h5-HT_1B and h5-HT_1D receptors in HEK 293 cells, respectively. Alniditan has migraine-preventive effects^[1][2]. IC50 & Target: IC50: 1.7 nM (HT_1B, in HEK 293 cell), 1.3 nM (HT_1D, in HEK 293 cells)^[3] 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]. 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].