The Sound of Evolution
Eletriptan
Mechanism of action:
Eletriptan is a serotonin 5-HT1B/5-HT1D receptor agonist and belongs to the triptan class. Its action is concentrated in the trigeminovascular system. It stimulates 5-HT1B receptors on intracranial vascular smooth muscle, especially in meningeal vessels, increasing vascular tone and causing vasoconstriction. It also stimulates 5-HT1D receptors at trigeminal nerve endings, reducing the release of pro-inflammatory and pain-related neuropeptides such as calcitonin gene-related peptide and substance P, thereby decreasing neurogenic inflammation and pain transmission.
Reference(s):
1. Napier C et al. (1999). Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [³H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol.
2. van den Broek RW et al. (2000). Pharmacological analysis of contractile effects of eletriptan and sumatriptan on human isolated blood vessels. Eur J Pharmacol.