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

S Bourrain; J G Neduvelil; M S Beer; J A Stanton; G A Showell; A M MacLeod

doi:10.1016/s0960-894x(99)00614-9

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

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3369-74. doi: 10.1016/s0960-894x(99)00614-9.

Authors

S Bourrain¹, J G Neduvelil, M S Beer, J A Stanton, G A Showell, A M MacLeod

Affiliation

¹ Merck, Sharp & Dohme Research Laboratories, Terlings Park, Harlow, UK. Sylvie Bourrain@Merck.com

PMID: 10612601
DOI: 10.1016/s0960-894x(99)00614-9

Abstract

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.

MeSH terms

Animals
CHO Cells
Cricetinae
Humans
Migraine Disorders / drug therapy*
Piperidines / pharmacology*
Piperidines / therapeutic use
Receptor, Serotonin, 5-HT1D
Receptors, Serotonin / drug effects*
Serotonin Receptor Agonists / pharmacology*
Serotonin Receptor Agonists / therapeutic use

Substances

Piperidines
Receptor, Serotonin, 5-HT1D
Receptors, Serotonin
Serotonin Receptor Agonists