title: Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).
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.
authors.affiliation: NiKem Research, Via Zambeletti 25, 20021 Baranzate, Milan, Italy. ilaria.peretto@nikemresearch.com
authors.forename: Ilaria
authors.initials: I
authors.lastname: Peretto
authors.forename: Claudia
authors.initials: C
authors.lastname: Fossati
authors.forename: Giuseppe A M
authors.initials: GA
authors.lastname: Giardina
authors.forename: Alessandra
authors.initials: A
authors.lastname: Giardini
authors.forename: Matilde
authors.initials: M
authors.lastname: Guala
authors.forename: Elena
authors.initials: E
authors.lastname: La Porta
authors.forename: Paola
authors.initials: P
authors.lastname: Petrillo
authors.forename: Stefano
authors.initials: S
authors.lastname: Radaelli
authors.forename: Luigi
authors.initials: L
authors.lastname: Radice
authors.forename: Luca F
authors.initials: LF
authors.lastname: Raveglia
authors.forename: Enza
authors.initials: E
authors.lastname: Santoro
authors.forename: Roberta
authors.initials: R
authors.lastname: Scudellaro
authors.forename: Francesca
authors.initials: F
authors.lastname: Scarpitta
authors.forename: Alberto
authors.initials: A
authors.lastname: Cerri
authors.forename: Sergio
authors.initials: S
authors.lastname: Menegon
authors.forename: Giulio M
authors.initials: GM
authors.lastname: Dondio
authors.forename: Andrea
authors.initials: A
authors.lastname: Rizzi
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Armani
authors.forename: Gabriele
authors.initials: G
authors.lastname: Amari
authors.forename: Maurizio
authors.initials: M
authors.lastname: Civelli
authors.forename: Gino
authors.initials: G
authors.lastname: Villetti
authors.forename: Riccardo
authors.initials: R
authors.lastname: Patacchini
authors.forename: Marco
authors.initials: M
authors.lastname: Bergamaschi
authors.forename: Franco
authors.initials: F
authors.lastname: Bassani
authors.forename: Maurizio
authors.initials: M
authors.lastname: Delcanale
authors.forename: Bruno P
authors.initials: BP
authors.lastname: Imbimbo
mesh_terms: D000818:Animals; D016084:Bronchoconstriction / Q000187:drug effects; D001993:Bronchodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006168:Guinea Pigs; D006801:Humans; D048289:Imidazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D009200:Myocardial Contraction / Q000187:drug effects; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D043587:Receptor, Muscarinic M3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014132:Trachea / Q000187:drug effects / Q000502:physiology
chemical_list: D001993:Bronchodilator Agents; D048289:Imidazolidines; D000644:Quaternary Ammonium Compounds; D043587:Receptor, Muscarinic M3