Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
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.
Novelli
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Dipartimento di Scienze Farmaceutiche - Università di Genova, Italy.
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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*
D001570:Benzodiazepinones; D008024:Ligands; D011725:Pyridines; D011807:Quinolizines; D011976:Receptors, Muscarinic; D010890:Pirenzepine; D019832:N-Methylscopolamine