Impact of isometheptene enantiomers in human blood vessels in vitro and rat middle meningeal artery

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  • Isometheptene enantiomers do not constrict the human coronary artery in vitro and therefore have a relatively safe peripheral vascular profile in migraine.

Why this matters

  • Racemic isometheptene is an antimigraine drug that has previously been separated into its enantiomers, (R)- and (S)-isometheptene as a result of cardiovascular side-effect concerns but do not appear to modulate neurogenic calcitonin gene-related peptide (CGRP) release so the mechanism of anti-migraine activity remains unknown.

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