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.
3-arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective alpha(1)-adrenoceptor ligands
MARUCCI, Gabriella;ANGELI, Piero;
2006-01-01
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.File in questo prodotto:
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