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Substituted 2-(R)-methyl piperazines as muscarinic M(2) 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, Gordon; Taylor, Lisa A; Billard, William; Binch, Herbert; Lachowicz, Jean E.
Bioorg Med Chem Lett ; 12(5): 791-4, 2002 Mar 11.
Article in English | MEDLINE | ID: mdl-11859004

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.


Subject(s)
Piperazines/chemical synthesis , Piperazines/metabolism , Receptors, Muscarinic/metabolism , Acetylcholine/metabolism , Administration, Oral , Animals , Binding Sites , Ligands , Microdialysis , Molecular Structure , Piperazines/chemistry , Rats , Receptor, Muscarinic M1 , Receptor, Muscarinic M2
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