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

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 n...

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Veröffentlicht in:Journal of medicinal chemistry 2001-11, Vol.44 (24), p.4031-4034
Hauptverfasser: Xu, Yao-Chang, Johnson, Kirk W, Phebus, Lee A, Cohen, Marlene, Nelson, David L, Schenck, Kathy, Walker, Clint D, Fritz, James E, Kaldor, Stephen W, LeTourneau, Michael E, Murff, Robert E, Zgombick, John M, Calligaro, David O, Audia, James E, Schaus, John M
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Sprache:eng
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Zusammenfassung: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0155190