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

Joseph A Kozlowski; Guowei Zhou; Jayaram R Tagat; Sue Ing Lin; Stuart W McCombie; Vilma B Ruperto; Ruth A Duffy; Robert A McQuade; Gordon Crosby; Lisa A Taylor; William Billard; Herbert Binch; Jean E Lachowicz

doi:10.1016/s0960-894x(02)00023-9

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.

Authors

Joseph A Kozlowski¹, Guowei Zhou, Jayaram R Tagat, Sue Ing Lin, Stuart W McCombie, Vilma B Ruperto, Ruth A Duffy, Robert A McQuade, Gordon Crosby, Lisa A Taylor, William Billard, Herbert Binch, Jean E Lachowicz

Affiliation

¹ Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA. joseph.kozlowski@spcorp.com

PMID: 11859004
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