title: Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.
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.
authors.affiliation: Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA. joseph.kozlowski@spcorp.com
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Kozlowski
authors.forename: Guowei
authors.initials: G
authors.lastname: Zhou
authors.forename: Jayaram R
authors.initials: JR
authors.lastname: Tagat
authors.forename: Sue Ing
authors.initials: SI
authors.lastname: Lin
authors.forename: Stuart W
authors.initials: SW
authors.lastname: McCombie
authors.forename: Vilma B
authors.initials: VB
authors.lastname: Ruperto
authors.forename: Ruth A
authors.initials: RA
authors.lastname: Duffy
authors.forename: Robert A
authors.initials: RA
authors.lastname: McQuade
authors.forename: Gordon
authors.initials: G
authors.lastname: Crosby
authors.forename: Lisa A
authors.initials: LA
authors.lastname: Taylor
authors.forename: William
authors.initials: W
authors.lastname: Billard
authors.forename: Herbert
authors.initials: H
authors.lastname: Binch
authors.forename: Jean E
authors.initials: JE
authors.lastname: Lachowicz
mesh_terms: D000109:Acetylcholine / Q000378:metabolism; D000284:Administration, Oral; D000818:Animals; D001665:Binding Sites; D008024:Ligands; D017551:Microdialysis; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D051381:Rats; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic / Q000378:metabolism*
chemical_list: D008024:Ligands; D010879:Piperazines; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic; D000109:Acetylcholine