Characterisation of a chimeric hD3/D2 dopamine receptor expressed in CHO cells.
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.
McAllister
G
G
Neuroscience Research Centre, Merck, Sharp and Dohme Research Laboratories, Harlow, Essex, UK.
Knowles
M R
MR
Patel
S
S
Marwood
R
R
Emms
F
F
Seabrook
G R
GR
Graziano
M
M
Borkowski
D
D
Hey
P J
PJ
Freedman
S B
SB
D000262:Adenylyl Cyclases / Q000378:metabolism; D000595:Amino Acid Sequence; D000818:Animals; D016718:Arachidonic Acid / Q000378:metabolism; D001483:Base Sequence; D016466:CHO Cells; D000001:Calcimycin / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D005576:Colforsin / Q000494:pharmacology; D006224:Cricetinae; D004298:Dopamine / Q000494:pharmacology; D015259:Dopamine Agents / Q000378:metabolism; D018492:Dopamine Antagonists; D006220:Haloperidol / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D008024:Ligands; D008969:Molecular Sequence Data; D009838:Oligodeoxyribonucleotides; D016133:Polymerase Chain Reaction; D017433:Protein Structure, Secondary; D011954:Receptors, Dopamine / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D017448:Receptors, Dopamine D2 / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D050637:Receptors, Dopamine D3; D011993:Recombinant Fusion Proteins / Q000187:drug effects / Q000378:metabolism*; D013469:Sulpiride / Q000378:metabolism; D014162:Transfection
C493593:DRD3 protein, human; D015259:Dopamine Agents; D018492:Dopamine Antagonists; D008024:Ligands; D009838:Oligodeoxyribonucleotides; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D011993:Recombinant Fusion Proteins; D005576:Colforsin; D016718:Arachidonic Acid; D000001:Calcimycin; D013469:Sulpiride; D000262:Adenylyl Cyclases; D006220:Haloperidol; D004298:Dopamine