Abstract
The selective dopamine D3 receptor antagonist [3H](+)S 14297 ((+)-[7-(N,N-dipropylamino)-5,6,7,8-tetrahydro-naphtho(2,3b)dihydro,2,3- furane]), labelled to high specific activity (145 Ci/mmol), bound to cloned human dopamine D3 receptors but displayed negligible binding to cloned human D2 receptors. [3H](+)S 14297 exhibited rapid association and dissociation, high affinity saturable binding (Kd = 7.0 nM) and a competition binding profile highly correlated with that of [125I]iodosulpride (r = 0.98).
MeSH terms
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2-Naphthylamine / analogs & derivatives*
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2-Naphthylamine / metabolism
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Animals
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Binding, Competitive
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CHO Cells
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Cricetinae
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Dopamine Agents / metabolism
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Furans / metabolism*
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Humans
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Ligands
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Receptors, Dopamine D2 / metabolism*
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Receptors, Dopamine D3
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Sulpiride / analogs & derivatives
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Sulpiride / metabolism
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Transfection
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Tritium
Substances
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DRD3 protein, human
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Dopamine Agents
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Furans
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Ligands
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Receptors, Dopamine D2
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Receptors, Dopamine D3
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iodosulpride
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Tritium
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7-(N,N-dipropylamino)-5,6,7,8-tetrahydronaphtho(2,3-b)dihydro-2,3-furan
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Sulpiride
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2-Naphthylamine