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Maxalt

Merck & Co., Inc.

Drug Names(s): rizatriptan benzoate, MK-0462

Description: Maxalt binds with high affinity to human cloned 5-HT1B and 5-HT1D receptors. Maxalt hasweak affinity for other 5-HT1 receptor subtypes (5-HT1A, 5-HT1E, 5-HT1F) and the 5-HT7 receptor, but hasno significant activity at 5-HT2, 5-HT3, alpha- and beta-adrenergic, dopaminergic, histaminergic,muscarinic or benzodiazepine receptors.

The therapeutic activity of Maxalt in migraine can most likely be attributed to agonist effects at 5-HT1B/1D receptors on the extracerebral, intracranial bloodvessels that become dilated during a migraine attack and on nerve terminals in the trigeminal system.Activation of these receptors results in cranial vessel constriction, inhibition of neuropeptide release andreduced transmission in trigeminal pain pathways.


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