Abstract
A new series of benzopyrano[3,4-c]pyrrole derivatives were synthesized and evaluated for their interaction with dopamine D3 versus D2 receptors. Amongst these compounds, 4x (S 33084) was found to be a potent and selective dopamine D3 receptor antagonist.
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin / analogs & derivatives
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8-Hydroxy-2-(di-n-propylamino)tetralin / chemistry
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Animals
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Benzopyrans / chemical synthesis*
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Benzopyrans / pharmacology*
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CHO Cells / metabolism
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Cricetinae
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Dopamine Agonists / chemistry
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Dopamine Antagonists / chemical synthesis*
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Dopamine Antagonists / pharmacology*
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Dopamine D2 Receptor Antagonists*
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Humans
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Iodine Radioisotopes
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Pyrroles / chemistry
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Pyrrolidines / chemistry
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Receptors, Dopamine D2 / genetics
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Receptors, Dopamine D2 / metabolism
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Receptors, Dopamine D3
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Structure-Activity Relationship
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Sulpiride / metabolism
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Tetrahydronaphthalenes / chemistry
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Transfection
Substances
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Benzopyrans
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DRD3 protein, human
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Dopamine Agonists
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Dopamine Antagonists
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Dopamine D2 Receptor Antagonists
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Iodine Radioisotopes
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Pyrroles
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Pyrrolidines
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Receptors, Dopamine D2
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Receptors, Dopamine D3
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Tetrahydronaphthalenes
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Guanosine 5'-O-(3-Thiotriphosphate)
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5-hydroxy-2-N,N-dipropylaminotetralin
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Sulpiride
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7-hydroxy-2-N,N-dipropylaminotetralin