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.
|
Authors | G R Martin |
Journal | European neurology
(Eur Neurol)
Vol. 36 Suppl 2
Pg. 13-8
( 1996)
ISSN: 0014-3022 [Print] Switzerland |
PMID | 8791027
(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
|