Abstract
The D2 dopamine receptor is known to be functionally coupled when expressed in CHO cells, whereas the effector systems for the D3 dopamine receptor remain unclear. A chimeric, human D3/D2 receptor (hD3/D2) was constructed containing the third intracellular loop region of the D2 receptor. CHO cells stably expressing the D2, D3, or hD3/D2 receptors were created and the pharmacology of the receptors was examined. The chimeric hD3/D2 receptor retained D3-like affinities for dopaminergic ligands. However, in contrast to the D2 receptor neither the D3 receptor nor the hD3/D2 receptor could functionally couple to the adenylate cyclase or arachidonic acid release mechanisms.
MeSH terms
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Adenylyl Cyclases / metabolism
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Amino Acid Sequence
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Animals
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Arachidonic Acid / metabolism
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Base Sequence
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CHO Cells
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Calcimycin / pharmacology
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Cell Membrane / metabolism
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Colforsin / pharmacology
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Cricetinae
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Dopamine / pharmacology
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Dopamine Agents / metabolism
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Dopamine Antagonists
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Haloperidol / pharmacology
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Humans
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Kinetics
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Ligands
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Molecular Sequence Data
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Oligodeoxyribonucleotides
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Polymerase Chain Reaction
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Protein Structure, Secondary
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Receptors, Dopamine / drug effects
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Receptors, Dopamine / genetics
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Receptors, Dopamine / metabolism*
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Receptors, Dopamine D2 / drug effects
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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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Recombinant Fusion Proteins / drug effects
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Recombinant Fusion Proteins / metabolism*
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Sulpiride / metabolism
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Transfection
Substances
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DRD3 protein, human
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Dopamine Agents
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Dopamine Antagonists
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Ligands
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Oligodeoxyribonucleotides
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Receptors, Dopamine
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Receptors, Dopamine D2
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Receptors, Dopamine D3
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Recombinant Fusion Proteins
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Colforsin
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Arachidonic Acid
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Calcimycin
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Sulpiride
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Adenylyl Cyclases
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Haloperidol
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Dopamine