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
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
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.