Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist

Daniel P Becker; Daniel L Flynn; Clara I Villamil

doi:10.1016/j.bmcl.2004.04.021

Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3073-5. doi: 10.1016/j.bmcl.2004.04.021.

Authors

Daniel P Becker¹, Daniel L Flynn, Clara I Villamil

Affiliation

¹ Department of Medicinal Chemistry, Pfizer Research and Development, 4901 Searle Parkway, Skokie, IL 60077, USA. dbecke3@luc.edu

PMID: 15149647
DOI: 10.1016/j.bmcl.2004.04.021

Abstract

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.

MeSH terms

Animals
Benzamides / chemistry*
Benzamides / pharmacology
Pyrroles / chemistry*
Pyrroles / pharmacology
Rats
Receptors, Serotonin, 5-HT4 / physiology
Salmonella typhimurium / drug effects
Salmonella typhimurium / metabolism
Serotonin 5-HT4 Receptor Agonists*
Serotonin Receptor Agonists / chemistry*
Serotonin Receptor Agonists / pharmacology

Substances

Benzamides
Pyrroles
Serotonin 5-HT4 Receptor Agonists
Serotonin Receptor Agonists
SC 53116
Receptors, Serotonin, 5-HT4