N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: A Potent, Selective, and Orally Active 5-HT1F Receptor Agonist Potentially Useful for Migraine Therapy
Journal of Medicinal Chemistry2001Vol. 44(24), pp. 4031–4034
Citations Over TimeTop 25% of 2001 papers
Yao‐Chang Xu, Kirk W. Johnson, Lee A. Phebus, Marlene L. Cohen, David L. Nelson, Kathy W. Schenck, Clint Walker, James E. Fritz, Stephen W. Kaldor, Michael E. LeTourneau, Robert E. Murff, John M. Zgombick, David O. Calligaro, James E. Audia, John M. Schaus
Abstract
Recent studies have demonstrated that selective 5-HT(1F) 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-HT(1F) receptor relative to more than 40 other serotonergic and nonserotonergic receptors examined.
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