Anti-Migraine Drug Interactions with Cloned Human 5-Hydroxytryptamine 1 , Receptor Subtypes

Multiple 5‐hydroxytryptamine receptors have been identified in humans

Stephen J. Peroutka

2005

Scholarcy highlights

  • Multiple 5‐hydroxytryptamine receptors have been identified in humans
  • Recent molecular biological advances have allowed for the development of assays employing cloned human 5‐HT 1 receptors expressed in cells by DNA transfection
  • This study analyzed the ability of ergotamine, dihydroergotamine, 5‐HT and sumatriptan to interact with the four known human 5‐HT 1 receptor subtypes
  • Drug affinities for the human 5‐HT 1B and 5‐HT 1D receptors correlate most closely with the rank order of clinical dosages used to treat a migraine attack. These data indicate that human 5‐HT 1B and/or 5‐HT 1D receptors are likely to mediate the therapeutic efficacy of acute anti‐migraine drugs
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