title: Characterisation of a chimeric hD3/D2 dopamine receptor expressed in CHO cells.
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.
authors.affiliation: Neuroscience Research Centre, Merck, Sharp and Dohme Research Laboratories, Harlow, Essex, UK.
authors.forename: G
authors.initials: G
authors.lastname: McAllister
authors.forename: M R
authors.initials: MR
authors.lastname: Knowles
authors.forename: S
authors.initials: S
authors.lastname: Patel
authors.forename: R
authors.initials: R
authors.lastname: Marwood
authors.forename: F
authors.initials: F
authors.lastname: Emms
authors.forename: G R
authors.initials: GR
authors.lastname: Seabrook
authors.forename: M
authors.initials: M
authors.lastname: Graziano
authors.forename: D
authors.initials: D
authors.lastname: Borkowski
authors.forename: P J
authors.initials: PJ
authors.lastname: Hey
authors.forename: S B
authors.initials: SB
authors.lastname: Freedman
mesh_terms: 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
chemical_list: 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