Abstract
The discovery of a new series of selective and high-affinity alpha(1)-adrenoceptor (alpha(1)-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 alpha(1)-ARs and substantial selectivity with respect to 5-HT(1A) and dopaminergic D(1) and D(2) receptors. Functional assays, performed on selected derivatives, showed antagonistic properties.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Chlorine / chemistry
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Dopamine Agents / metabolism
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Dose-Response Relationship, Drug
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Humans
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Kinetics
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Ligands
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Magnetic Resonance Spectroscopy
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Models, Chemical
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Piperazines / chemistry
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Piperazines / pharmacology*
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Protein Binding
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Pyrimidinones / chemistry
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Pyrroles / chemistry*
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Receptors, Adrenergic, alpha-1 / chemistry*
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Receptors, Adrenergic, alpha-1 / metabolism
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Receptors, Serotonin / chemistry
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Receptors, Serotonin, 5-HT1 / chemistry
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Time Factors
Substances
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Dopamine Agents
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Ligands
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Piperazines
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Pyrimidinones
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Pyrroles
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Receptors, Adrenergic, alpha-1
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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Chlorine