Discovery and Development of Triptans - Mechanism

Mechanism

Triptans are specific and selective agonists for the 5-HT1 receptors. Sumatriptan binds to 5-HT1D receptors, zolmitriptan, rizatriptan, naratriptan, almotriptan, and frovatriptan binds to 5-HT1B/1D and eletriptan binds to 5-HT1B/1D/1F receptors. Triptans supposed mechanism of action are vasoconstriction effect on carotid arterial circulation without affecting cerebral blood flow, peripheral neuronal inhibition and inhibition of transmission through second order neurons of the trigeminocervical complex.

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