Inhibition of the Trigemino-Vascular System with 5-HT1D Agonist Drugs: Selectively Targeting Additional Sites of Action

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Abstract
Inappropriate activation of the trigemino-vascular system is thought to be important in the pathogenesis of a migraine attack. The 5-HTID 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-HTID 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.

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