4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines : Selective h5-HT1D agonists for the treatment of migraine

A series of 4-hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl] piperidines was investigated as potential selective h5-HT1D agonists for the treatment of migraine. The 4-[(N-benzyl-N-methyl)amino]methyl analog 12a was found to be a full agonist at the h5-HT1D receptor with good binding sele...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-12, Vol.9 (23), p.3369-3374
Hauptverfasser:	BOURRAIN, S, NEDUVELIL, J. G, BEER, M. S, STANTON, J. A, SHOWELL, G. A, MACLEOD, A. M
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences CHO Cells Cricetinae Humans Medical sciences Migraine Disorders - drug therapy Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperidines - pharmacology Piperidines - therapeutic use Receptor, Serotonin, 5-HT1D Receptors, Serotonin - drug effects Serotonin Receptor Agonists - pharmacology Serotonin Receptor Agonists - therapeutic use Serotoninergic system
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Zusammenfassung:	A series of 4-hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl] piperidines was investigated as potential selective h5-HT1D agonists for the treatment of migraine. The 4-[(N-benzyl-N-methyl)amino]methyl analog 12a was found to be a full agonist at the h5-HT1D receptor with good binding selectivity over the h5-HT1B receptor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00614-9