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RESEARCH PRODUCT
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands
Günter LambrechtThomas M BöhmeErnst MutschlerGerd DannhardtChristine Keimsubject
QuinuclidinesTertiary amineStereochemistryClinical BiochemistryPharmaceutical ScienceIn Vitro TechniquesLigandsBiochemistryChemical synthesischemistry.chemical_compoundAlzheimer DiseaseDrug DiscoveryMuscarinic acetylcholine receptorHumansReceptorMolecular BiologyAcetylcholine receptorReceptor Muscarinic M2Bicyclic moleculeOrganic ChemistryReceptors MuscarinicchemistryMolecular MedicineRadiopharmaceuticalsSelectivityTomography Emission-ComputedQuinuclidinedescription
In our search for M2-selective muscarinic receptor antagonists, we synthesized 1,3-disubstituted indenes. The effects of different basic moieties with regard to binding and selectivity towards the five distinct muscarinic receptor subtypes were investigated. The results show that the quinuclidine series afforded the most promising compounds in terms of both receptor affinity and M2-subtype selectivity.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2001-05-01 | Bioorganic & Medicinal Chemistry Letters |