1,4-Dioxane, a Suitable Scaffold for the Development of Novel M-3 Muscarinic Receptor Antagonists (Articolo in rivista)

Type
Label
  • 1,4-Dioxane, a Suitable Scaffold for the Development of Novel M-3 Muscarinic Receptor Antagonists (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/jm2013216 (literal)
Alternative label
  • Del Bello, F (Del Bello, Fabio)2; Barocelli, E (Barocelli, Elisabetta)1; Bertoni, S (Bertoni, Simona)1; Bonifazi, A (Bonifazi, Alessandro)2; Camalli, M (Camalli, Mercedes)3; Campi, G (Campi, Gaetano)3; Giannella, M (Giannella, Mario)2; Matucci, R (Matucci, Rosanna)4; Nesi, M (Nesi, Marta)4; Pigini, M (Pigini, Maria)2; Quaglia, W (Quaglia, Wilma)2; Piergentili, A (Piergentili, Alessandro)2 (2012)
    1,4-Dioxane, a Suitable Scaffold for the Development of Novel M-3 Muscarinic Receptor Antagonists
    in Journal of medicinal chemistry; ACS, American chemical society, Washington, DC (Stati Uniti d'America)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Del Bello, F (Del Bello, Fabio)2; Barocelli, E (Barocelli, Elisabetta)1; Bertoni, S (Bertoni, Simona)1; Bonifazi, A (Bonifazi, Alessandro)2; Camalli, M (Camalli, Mercedes)3; Campi, G (Campi, Gaetano)3; Giannella, M (Giannella, Mario)2; Matucci, R (Matucci, Rosanna)4; Nesi, M (Nesi, Marta)4; Pigini, M (Pigini, Maria)2; Quaglia, W (Quaglia, Wilma)2; Piergentili, A (Piergentili, Alessandro)2 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 55 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 5 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 4 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • 1. Univ Parma, Dipartimento Sci Farmacol Biol & Chim Applicate, I-43124 Parma, Italy 2. Univ Camerino, Scuola Sci Farmaco & Prod Salute, I-62032 Camerino, Italy 3. CNR, Ist Cristallog, Area Ric Roma 1, Monterotondo Stn, I-00016 Rome, Italy 4. Univ Florence, Dipartimento Farmacol, I-50139 Florence, Italy (literal)
Titolo
  • 1,4-Dioxane, a Suitable Scaffold for the Development of Novel M-3 Muscarinic Receptor Antagonists (literal)
Abstract
  • In this study the modulation of the pharmacological profile from agonist to antagonist was successfully obtained by replacing the methyl group in position 6 of the 1,4-dioxane scaffold of the potent M-2/M-3 muscarinic agonist 1 with bulkier groups. In particular, the 6,6-diphenyl substitution provided the potent M-3 preferring antagonist (+/-)-17, which in in vivo study proved to be effective in reducing the volume-induced contractions of rat urinary bladder and was devoid of cardiovascular effects. (literal)
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