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Alniditan dihydrochloride

Names

[ CAS No. ]:
155428-00-5

[ Name ]:
Alniditan dihydrochloride

Biological Activity

[Description]:

Alniditan (Alnitidan) dihydrochloride 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 dihydrochloride has migraine-preventive effects[1][2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

human 5-HT1B Receptor:1.7 nM (IC50)

human 5-HT1D Receptor:1.3 nM (IC50)

5-HT1B Receptor:0.9 nM (Kd)

5-HT1D Receptor:1.2 nM (Kd)


[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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H28Cl2N4O

[ Molecular Weight ]:
375.34

Related Compounds