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

Citation
Yc. Xu et al., 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, J MED CHEM, 44(24), 2001, pp. 4031-4034
Citations number
43
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
44
Issue
24
Year of publication
2001
Pages
4031 - 4034
Database
ISI
SICI code
0022-2623(20011122)44:24<4031:NAP>2.0.ZU;2-0
Abstract
Recent studies have demonstrated that selective 5-HT1F receptor agonists in hibit neurogenic dural inflammation, a model of migraine headache, indicati ng that these compounds may be effective therapies for the treatment of mig raine pain. This communication describes the synthesis and discovery of a n ovel compound, N-[3-(2-dimethylamino)ethyl)-2-methyl-1H-indol-5-yl]-4-fluor obenzamide (4), which possesses high binding affinity and selectivity at th e 5-HT1F receptor relative to more than 40 other serotonergic and nonseroto nergic receptors examined.