Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.

Article Details

Citation

Starck JP, Talaga P, Quere L, Collart P, Christophe B, Lo Brutto P, Jadot S, Chimmanamada D, Zanda M, Wagner A, Mioskowski C, Massingham R, Guyaux M

Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):373-7. Epub 2005 Nov 3.

PubMed ID
16275087 [ View in PubMed
]
Abstract

The synthesis and biological evaluation of a novel family of M(3) muscarinic antagonists are described. A systematic modification of the substituents to a novel alkyne-quinuclidine scaffold yielded original compounds displaying potent in vitro anticholinergic properties.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DarifenacinMuscarinic acetylcholine receptor M2Ki (nM)50N/AN/ADetails
DarifenacinMuscarinic acetylcholine receptor M3Ki (nM)1.3N/AN/ADetails
OxybutyninMuscarinic acetylcholine receptor M2Ki (nM)16N/AN/ADetails
OxybutyninMuscarinic acetylcholine receptor M3Ki (nM)1.3N/AN/ADetails
TolterodineMuscarinic acetylcholine receptor M2Ki (nM)4N/AN/ADetails
TolterodineMuscarinic acetylcholine receptor M3Ki (nM)3.2N/AN/ADetails