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新型毒蕈碱M3选择性拮抗剂——二芳基咪唑烷-2-酮衍生物的发现（第2部分）

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

作者信息

Peretto Ilaria, Fossati Claudia, Giardina Giuseppe A M, Giardini Alessandra, Guala Matilde, La Porta Elena, Petrillo Paola, Radaelli Stefano, Radice Luigi, Raveglia Luca F, Santoro Enza, Scudellaro Roberta, Scarpitta Francesca, Cerri Alberto, Menegon Sergio, Dondio Giulio M, Rizzi Andrea, Armani Elisabetta, Amari Gabriele, Civelli Maurizio, Villetti Gino, Patacchini Riccardo, Bergamaschi Marco, Bassani Franco, Delcanale Maurizio, Imbimbo Bruno P

机构信息

NiKem Research, Via Zambeletti 25, 20021 Baranzate, Milan, Italy.

出版信息

J Med Chem. 2007 Apr 5;50(7):1693-7. doi: 10.1021/jm061160+. Epub 2007 Mar 13.

DOI:10.1021/jm061160+
PMID:17352463
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.

摘要

描述了一类新型季铵盐毒蕈碱M3受体拮抗剂的合成及其生物活性，这类拮抗剂对M2受体具有高选择性。所选化合物在离体豚鼠气管中表现出强效抗胆碱能特性，并且对气管的功能选择性优于心房。在体内，相同的化合物在豚鼠气管内给药后能有效抑制乙酰胆碱诱导的支气管收缩。

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Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).新型毒蕈碱M3选择性拮抗剂——二芳基咪唑烷-2-酮衍生物的发现（第2部分）
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