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

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...

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Veröffentlicht in:	Journal of medicinal chemistry 2001-11, Vol.44 (24), p.4031-4034
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzamides - chemical synthesis Benzamides - chemistry Benzamides - metabolism Benzamides - pharmacology Cell Line Dura Mater - drug effects Guinea Pigs Humans In Vitro Techniques Indoles - chemical synthesis Indoles - chemistry Indoles - metabolism Indoles - pharmacology Inflammation Migraine Disorders - drug therapy Muscle Contraction - drug effects Muscle, Smooth, Vascular - drug effects Muscle, Smooth, Vascular - physiology Rabbits Rats Receptor, Serotonin, 5-HT1F Receptors, Neurotransmitter - metabolism Receptors, Serotonin - drug effects Receptors, Serotonin - metabolism Saphenous Vein - drug effects Saphenous Vein - physiology Serotonin Receptor Agonists - chemical synthesis Serotonin Receptor Agonists - chemistry Serotonin Receptor Agonists - metabolism Serotonin Receptor Agonists - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0022-2623