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

Autor: Xu, Y.-C., Johnson, K. W., Phebus, L. A., Cohen, M., Nelson, D. L., Schenck, K., Walker, C. D., Fritz, J. E., Kaldor, S. W., LeTourneau, M. E., Murff, R. E., Zgombick, J. M., Calligaro, D. O., Audia, J. E., Schaus, J. M.
Zdroj: Journal of Medicinal Chemistry; November 2001, Vol. 44 Issue: 24 p4031-4034, 4p
Abstrakt: 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.
Databáze: Supplemental Index