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 selectivity over the h5-HT1B receptor.
Bourrain
S
S
Merck, Sharp & Dohme Research Laboratories, Terlings Park, Harlow, UK. Sylvie Bourrain@Merck.com
Neduvelil
J G
JG
Beer
M S
MS
Stanton
J A
JA
Showell
G A
GA
MacLeod
A M
AM
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy*; D010880:Piperidines / Q000494:pharmacology* / Q000627:therapeutic use; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin / Q000187:drug effects*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology* / Q000627:therapeutic use
D010880:Piperidines; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists