Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands

Bioorg Med Chem Lett. 2002 Mar 11;12(5):791-4. doi: 10.1016/s0960-894x(02)00023-9.

Abstract

A novel series of 2-(R)-methyl-substituted piperazines (e.g., 2) is described. They are potent M(2) selective ligands that have >100-fold selectivity versus the M(1) receptor. In the rat microdialysis assay, compound 14 showed significantly enchanced levels of acetylcholine after oral administration.

MeSH terms

  • Acetylcholine / metabolism
  • Administration, Oral
  • Animals
  • Binding Sites
  • Ligands
  • Microdialysis
  • Molecular Structure
  • Piperazines / chemical synthesis*
  • Piperazines / chemistry
  • Piperazines / metabolism*
  • Rats
  • Receptor, Muscarinic M1
  • Receptor, Muscarinic M2
  • Receptors, Muscarinic / metabolism*

Substances

  • Ligands
  • Piperazines
  • Receptor, Muscarinic M1
  • Receptor, Muscarinic M2
  • Receptors, Muscarinic
  • Acetylcholine