Characterisation of a chimeric hD3/D2 dopamine receptor expressed in CHO cells

FEBS Letters

Seabrook, Guy R.²  Marwood, Rosemarie²  Borkowski, Doreen¹  Patel, Shil²  Freedman, Stephen B.²  Emms, Frances²  Hey, Patricia J.¹  Graziano, Michael¹  McAllister, George²  Knowles, Michael R.² 

[1] Molecular Pharmacology and Biochemistry, Merck, Sharp and Dohme Research Laboratories, Rahway, NJ, USA;Neuroscience Research Centre, Merck, Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Rd., Harlow, Essex, CM20 2QR, UK

关键词: Dopamine receptor;    Signal transduction;    Functional coupling;    hD2;    human D2 dopamine receptor;    hD3;    human D3 dopamine receptor;    hD3/D2;    human chimeric D3/D2 dopamine receptor;    GTP;    guanosine triphosphate;    cAMP;    adenosine 3';    5'-cyclic monophosphate;   

DOI  :  10.1016/0014-5793(93)81537-A

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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.

【 授权许可】

Unknown