N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: A Potent, Selective, and Orally Active 5-HT1FReceptor Agonist Potentially Useful for Migraine Therapy
JOURNAL OF MEDICINAL CHEMISTRY(2001)
Abstract
Recent studies have demonstrated that selective 5-HT1F receptor agonists inhibit neurogenic dural inflammation, a model of migraine headache, indicating that these compounds may be effective therapies for the treatment of migraine pain. This communication describes the synthesis and discovery of a novel compound, N-[3-(2-dimethylamino)ethyl)-2-methyl-1H-indol-5-yl]-4-fluorobenzamide (4), which possesses high binding affinity and selectivity at the 5-HT1F receptor relative to more than 40 other serotonergic and nonserotonergic receptors examined.
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