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Inhibition of the trigemino-vascular system with 5-HT1D agonist drugs: selectively targeting additional sites of action.

Abstract
Inappropriate activation of the trigemino-vascular system is thought to be important in the pathogenesis of a migraine attack. The 5-HT1D agonist sumatriptan, which is highly effective in the acute treatment of migraine, inhibits trigemino-vascular activation in animals, although its actions are normally limited to peripheral components of the trigemino-vascular system. 311C90, a novel 5-HT1D agonist drug, which is also highly effective in the acute treatment of migraine, acts not only at these sites, but, additionally within the brainstem, inhibiting trigemino-vascular activation centrally as well as peripherally. This article describes the pre-clinical development of 311C90 and considers, specifically, the approaches taken in the design of a molecule with attributes which facilitate access to brainstem components of the trigeminal pathway and combine this with good oral bioavailability.
AuthorsG R Martin
JournalEuropean neurology (Eur Neurol) Vol. 36 Suppl 2 Pg. 13-8 ( 1996) ISSN: 0014-3022 [Print] Switzerland
PMID8791027 (Publication Type: Journal Article, Review)
Chemical References
  • Oxazoles
  • Oxazolidinones
  • Serotonin Receptor Agonists
  • Tryptamines
  • zolmitriptan
Topics
  • Administration, Oral
  • Biological Availability
  • Cerebrovascular Circulation (drug effects)
  • Humans
  • Migraine Disorders (drug therapy)
  • Oxazoles (therapeutic use)
  • Oxazolidinones
  • Serotonin Receptor Agonists (pharmacokinetics, therapeutic use)
  • Trigeminal Nerve (drug effects)
  • Tryptamines

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