Article
Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.
Journal of medicinal chemistry - 14 Nov 2013
Tautermann Christofer S, Kiechle Tobias, Seeliger Daniel, Diehl Sonja, Wex Eva, Banholzer Rolf, Gantner Florian, Pieper Michael P, Casarosa Paola
Abstract excerpt
Antagonizing the human M3 muscarinic receptor (hM3R) over a long time is a key feature of modern bronchodilating COPD drugs aiming at symptom relief. The long duration of action of the antimuscarinic drug tiotropium and its kinetic subtype selectivity over hM2R are investigated by kinetic mapping of the binding site and the exit channel of hM3R. Hence, dissociation experiments have been performed with a set of...
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