Abstract—The discovery of a new series of selective and high-affinity a1-adrenoceptor (a1-AR) ligands, characterized by a 1H-pyrrolo[ 2,3-d]pyrimidine-2,4(3H,7H)-dione system, is described in this paper. Some synthesized compounds, including 20, 22, and 30, displayed affinity in the nanomolar range for a1-ARs and substantial selectivity with respect to 5-HT1A and dopaminergic D1 and D2 receptors. Functional assays, performed on selected derivatives, showed antagonistic properties.
|Titolo:||3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel,high-affinity and selective a1-adrenoceptor ligands|
|Data di pubblicazione:||2006|
|Appare nelle tipologie:||1.1 Articolo in rivista|