title: Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
abstract: Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzepine and nuvenzepine, were prepared and tested as ligands for muscarinic M1, M2 and M3 receptors; 5,11-dihydro-11-[(S-lupinyl)-thioacetyl]-6H-pyrido[2,3-b][1, 4]benzodiazepin-6-one exhibited IC50 = 10 nM for M1 and 760 nM for both M2 and M3 subtypes. During the synthesis some interesting side compounds were isolated and characterized.
authors.affiliation: Dipartimento di Scienze Farmaceutiche - Università di Genova, Italy.
authors.forename: F
authors.initials: F
authors.lastname: Novelli
authors.forename: A
authors.initials: A
authors.lastname: Sparatore
authors.forename: B
authors.initials: B
authors.lastname: Tasso
authors.forename: F
authors.initials: F
authors.lastname: Sparatore
mesh_terms: D000818:Animals; D001570:Benzodiazepinones / Q000737:chemistry*; D001667:Binding, Competitive; D008024:Ligands; D019832:N-Methylscopolamine / Q000378:metabolism; D010890:Pirenzepine / Q000378:metabolism; D011725:Pyridines / Q000737:chemistry*; D011807:Quinolizines / Q000737:chemistry / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D011976:Receptors, Muscarinic / Q000378:metabolism*
chemical_list: D001570:Benzodiazepinones; D008024:Ligands; D011725:Pyridines; D011807:Quinolizines; D011976:Receptors, Muscarinic; D010890:Pirenzepine; D019832:N-Methylscopolamine