N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.

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Xu YC, Johnson KW, Phebus LA, Cohen M, Nelson DL, Schenck K, Walker CD, Fritz JE, Kaldor SW, LeTourneau ME, Murff RE, Zgombick JM, Calligaro DO, Audia JE, Schaus JM

N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.

J Med Chem. 2001 Nov 22;44(24):4031-4.

PubMed ID

11708905 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sumatriptan	5-hydroxytryptamine receptor 1F	EC 50 (nM)	35	N/A	N/A	Details
Sumatriptan	5-hydroxytryptamine receptor 1F	Ki (nM)	25.7	N/A	N/A	Details