Literature DB >> 11708905

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.

Y C Xu1, K W Johnson, L A Phebus, M Cohen, D L Nelson, K Schenck, C D Walker, J E Fritz, S W Kaldor, M E LeTourneau, R E Murff, J M Zgombick, D O Calligaro, J E Audia, J M Schaus.   

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.

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Year:  2001        PMID: 11708905     DOI: 10.1021/jm0155190

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Balancing focused combinatorial libraries based on multiple GPCR ligands.

Authors:  Farhad Soltanshahi; Tamsin E Mansley; Sun Choi; Robert D Clark
Journal:  J Comput Aided Mol Des       Date:  2006-10-13       Impact factor: 3.686

Review 2.  5-HT(1F) Receptor agonists: a new treatment option for migraine attacks?

Authors:  Lars Neeb; Jannis Meents; Uwe Reuter
Journal:  Neurotherapeutics       Date:  2010-04       Impact factor: 7.620

3.  Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships.

Authors:  Michael T Klein; Małgorzata Dukat; Richard A Glennon; Milt Teitler
Journal:  J Pharmacol Exp Ther       Date:  2011-03-21       Impact factor: 4.030

  3 in total

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