203180-28-3Relevant academic research and scientific papers
Synthesis and structure-Activity relationships of M2-Selective muscarinic receptor ligands in the 1-[4-(4-Arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family
McCombie, Stuart W.,Lin, Sue-Ing,Tagat, Jayaram R.,Nazareno, Dennis,Vice, Susan,Ford, Jennifer,Asberom, Theodros,Leone, Daria,Kozlowski, Joseph A.,Zhou, Guowei,Ruperto, Vilma B.,Duffy, Ruth A.,Lachowicz, Jean E.
, p. 795 - 798 (2007/10/03)
The synthesis and muscarinic binding properties of compounds based on the 1-[4-(4-arylsulfonyl)phenylmethyl]-4-(1-aroyl-4-piperidinyl)-piperazine skeleton are described. For compounds, substituted with appropriately configured methyl groups at the benzylic center and at the piperazine 2-position, high levels of selective, M2 subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted.
Substituted 2-(R)-Methyl piperazines as muscarinic M2 selective ligands
Kozlowski, Joseph A,Zhou, Guowei,Tagat, Jayaram R.,Lin, Sue-Ing,McCombie, Stuart W.,Ruperto, Vilma B.,Duffy, Ruth A.,McQuade, Robert A.,Crosby Jr., Gordon,Taylor, Lisa A.,Billard, William,Binch III, Herbert,Lachowicz, Jean E.
, p. 791 - 794 (2007/10/03)
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.
