N-homolupinanoyl and N-(omega-lupinylthio)alkanoyl derivatives of some tricyclic systems as ligands for muscarinic M1 and M2 receptor subtypes
Articolo
Data di Pubblicazione:
2003
Citazione:
N-homolupinanoyl and N-(omega-lupinylthio)alkanoyl derivatives of some tricyclic systems as ligands for muscarinic M1 and M2 receptor subtypes / B. Tasso, A. Sparatore, F. Sparatore. - In: IL FARMACO. - ISSN 0014-827X. - 58:9(2003 Sep), pp. 669-676. [10.1016/S0014-827X(03)00104-6]
Abstract:
A set of N-homolupinanoyl- and N-(omega-lupinylthio)alkanoyl derivatives of tricyclic systems (as phenothiazine, iminodibenzyl and dihydropyridobenzodiazepinone) has been prepared and tested for affinity for rat muscarinic M(1) and M(2) receptor subtypes labeled with [3H]pirenzepine and [3H]AF-DX 384. Good affinity for both M(1) and M(2) subtypes was displayed by most compounds, often with nanomolar K(i) values, which for lupinylthiopropionyl- and lupinylthiobutyryl-phenothiazines (13-16) were comparable to those of pirenzepine and methoctramine, respectively. However, only moderate selectivity for one or the other subtype was seen.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Muscarinic receptors ligands; N-(Homolupinanoyl)phenothiazines; N-(tert-Aminoalkanoyl)tricyclic systems; N-[(ω -lupinylthio)alkanoyl]phenothiazines; Quinolizidine derivatives
Elenco autori:
B. Tasso, A. Sparatore, F. Sparatore
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