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EnglishPirenzepine (2) is one of the most selective muscarinicM1 versus M2 receptor antagonists known. A series of 2 analogs, in which the piperazyl moiety was replaced by a cis- and trans-cyclohexane-1,2-diamine (3– 6) or a trans- and cis-perhydroquinoxaline rings (7 and 8) were prepared, with the aim to investigate the role of the piperazine ring of 2 in the interaction with the muscarinic receptors. The structural change leading to compounds 3–6 abolished in binding assays the muscarinic M1/M2 selectivity of 2, due to an increased M2 affinity. Rather, compounds 3–6 displayed a reversed selectivity showing more affinity at the muscarinic M2 receptor than at all the other subtypes tested.
| Titolo: | Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and a perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics | |
| Autore/i: | MINARINI, ANNA; G. Marucci; C. Bellucci; G. Giorgi; TUMIATTI, VINCENZO; BOLOGNESI, MARIA LAURA; MATERA, RICCARDO; ROSINI, MICHELA; MELCHIORRE, CARLO | |
| Autore/i Unibo: | ||
| Anno: | 2008 | |
| Rivista: | ||
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.bmc.2008.06.025 | |
| Abstract: | Pirenzepine (2) is one of the most selective muscarinicM1 versus M2 receptor antagonists known. A series of 2 analogs, in which the piperazyl moiety was replaced by a cis- and trans-cyclohexane-1,2-diamine (3– 6) or a trans- and cis-perhydroquinoxaline rings (7 and 8) were prepared, with the aim to investigate the role of the piperazine ring of 2 in the interaction with the muscarinic receptors. The structural change leading to compounds 3–6 abolished in binding assays the muscarinic M1/M2 selectivity of 2, due to an increased M2 affinity. Rather, compounds 3–6 displayed a reversed selectivity showing more affinity at the muscarinic M2 receptor than at all the other subtypes tested. | |
| Data prodotto definitivo in UGOV: | 2008-12-03 18:13:11 | |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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