Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.

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Prat M, Buil MA, Fernandez MD, Castro J, Monleon JM, Tort L, Casals G, Ferrer M, Huerta JM, Espinosa S, Lopez M, Segarra V, Gavalda A, Miralpeix M, Ramos I, Vilella D, Gonzalez M, Cordoba M, Cardenas A, Anton F, Beleta J, Ryder H

Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3457-61. doi: 10.1016/j.bmcl.2011.03.096. Epub 2011 Apr 3.

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21524581 [ View in PubMed

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Abstract

Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M(3) muscarinic antagonists with long duration of action in an in vivo model of bronchoconstriction. These compounds have also presented a high level of metabolic transformation (human liver microsomes). The synthesis, structure-activity relationships and biological evaluation of these compounds are reported.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Solifenacin	Muscarinic acetylcholine receptor M1	IC 50 (nM)	63.5	N/A	N/A	Details
Solifenacin	Muscarinic acetylcholine receptor M2	IC 50 (nM)	573.7	N/A	N/A	Details
Solifenacin	Muscarinic acetylcholine receptor M3	IC 50 (nM)	130.8	N/A	N/A	Details