Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.
Article Details
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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.
- PubMed ID
- 21524581 [ View in PubMed]
- 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