Substituted 2-(R)-Methyl piperazines as muscarinic M2 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

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

A novel series of 2-(R)-methyl-substituted piperazines (e.g., 2) is described. They are potent M2 selective ligands that have >100-fold selectivity versus the M1 receptor. In the rat microdialysis assay, compound 14 showed significantly enchanced levels of acetylcholine after oral administration.

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muscarinic m2 selective ligands,cheminform abstract

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