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J Med Chem. 2007 Apr 5;50(7):1693-7. Epub 2007 Mar 13.

Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).

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1
NiKem Research, Via Zambeletti 25, 20021 Baranzate, Milan, Italy. ilaria.peretto@nikemresearch.com

Abstract

Synthesis and biological activity of a novel class of quaternary ammonium salt muscarinic M3 receptor antagonists, showing high selectivity versus the M2 receptor, are described. Selected compounds exhibited potent anticholinergic properties, in isolated guinea-pig trachea, and good functional selectivity for trachea over atria. In vivo, the same compounds potently inhibited acetylcholine-induced bronchoconstriction after intratracheal administration in the guinea pig.

PMID:
17352463
DOI:
10.1021/jm061160+
[Indexed for MEDLINE]
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