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Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2008 Aug 28; Vol. 51 (16), pp. 4866-9. Date of Electronic Publication: 2008 Aug 05. - Publication Year :
- 2008
-
Abstract
- High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via intranasal or intratracheal administration. The novel inhaled muscarinic receptor antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease and other bronchoconstriction disorders.
- Subjects :
- Animals
Bridged Bicyclo Compounds, Heterocyclic pharmacology
Bronchoconstriction drug effects
Drug Evaluation, Preclinical methods
Guinea Pigs
Mice
Rats
Tyrosine pharmacology
Muscarinic Antagonists pharmacology
Phenylurea Compounds pharmacology
Quaternary Ammonium Compounds pharmacology
Tyrosine analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 51
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 18680280
- Full Text :
- https://doi.org/10.1021/jm800634k