Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.
Pyrrolizidine benzamide (+/-)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT(4) agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (+/-)-2 has an EC(50) of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116.
Becker
Daniel P
DP
Department of Medicinal Chemistry, Pfizer Research and Development, 4901 Searle Parkway, Skokie, IL 60077, USA. dbecke3@luc.edu
Flynn
Daniel L
DL
Villamil
Clara I
CI
D000818:Animals; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D044422:Receptors, Serotonin, 5-HT4 / Q000502:physiology; D012486:Salmonella typhimurium / Q000187:drug effects / Q000378:metabolism; D058828:Serotonin 5-HT4 Receptor Agonists; D017366:Serotonin Receptor Agonists / Q000737:chemistry* / Q000494:pharmacology
D001549:Benzamides; D011758:Pyrroles; D058828:Serotonin 5-HT4 Receptor Agonists; D017366:Serotonin Receptor Agonists; C074211:SC 53116; D044422:Receptors, Serotonin, 5-HT4