Bioactivity | Alniditan (Alnitidan) is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK 293 cells, respectively. Alniditan has migraine-preventive effects[1][2]. |
Invitro | 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]. |
Name | Alniditan |
CAS | 152317-89-0 |
Formula | C17H26N4O |
Molar Mass | 302.41 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Limmroth V, et al. Effects of alniditan on neurogenic oedema in the rat dura mater and on contraction of rat basilar artery. Eur J Pharmacol. 1999 Oct 8;382(2):103-9. [2]. Lesage AS, et al. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65. |