Muscarinic M2 antagonists: anthranilamide derivatives with exceptional selectivity and in vivo activity

Bioorg Med Chem. 2004 Jan 15;12(2):319-26. doi: 10.1016/j.bmc.2003.11.005.

Abstract

Anthranilamide analogues such as 23 are potent and highly selective muscarinic M2 antagonists that also show good oral bioavailability and in vivo activity.

MeSH terms

  • Animals
  • Avoidance Learning / drug effects
  • Biochemistry / methods
  • Biological Availability
  • CHO Cells
  • Cricetinae
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical / methods
  • Muscarinic Antagonists / chemistry*
  • Muscarinic Antagonists / pharmacokinetics
  • Muscarinic Antagonists / pharmacology*
  • Piperidines / chemistry*
  • Piperidines / pharmacology*
  • Rats
  • Receptor, Muscarinic M2 / antagonists & inhibitors*
  • Structure-Activity Relationship
  • ortho-Aminobenzoates / chemistry*

Substances

  • 1'-(2-amino-3-methylbenzoyl)-4-(4-((3-chlorophenyl)sulfonyl)phenyl)methyl-1,4'-bipiperidine
  • Muscarinic Antagonists
  • Piperidines
  • Receptor, Muscarinic M2
  • ortho-Aminobenzoates
  • piperidine
  • anthranilamide