Dopamine D2 receptor binding properties of [3H]U-86170, a dopamine receptor agonist.
U-86170F, an imidazoguinolinone, is a potent dopamine D2 agonist, binding with high affinity to the dopamine D2 receptor. A Kd of 0.99 nM was determined in membranes from Chinese hamster ovarian (CHO) cells transfected with the D2 receptor and a Kd of 1.72 nM was obtained in rat striatal homogenates. GTP sensitivity was demonstrated when its addition (300 microM) reduced [3H]U-86170 binding by 60%. This agonist ligand is especially effective in identifying agonists and partial agonists, as well as antagonists, and affords a more precise evaluation of their affinity for the dopamine D2 receptor, without the use of multiple site analysis, than does an antagonist [3H]-ligand.
CNS Diseases Research, Upjohn Laboratories, Upjohn Company, Kalamazoo, MI 49001.
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D000634:Aminoquinolines / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D016466:CHO Cells / Q000187:drug effects / Q000378:metabolism; D003001:Cloning, Molecular; D003342:Corpus Striatum / Q000378:metabolism; D006224:Cricetinae; D015259:Dopamine Agents / Q000378:metabolism / Q000494:pharmacology*; D018492:Dopamine Antagonists; D019204:GTP-Binding Proteins / Q000378:metabolism; D006160:Guanosine Triphosphate / Q000494:pharmacology; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000378:metabolism; D017448:Receptors, Dopamine D2
D000634:Aminoquinolines; D015259:Dopamine Agents; D018492:Dopamine Antagonists; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; C073698:5-(dipropylamino)-5,6-dihydro-4H-imidazo-(5,1ij)quinolin-2(1H)-one; D006160:Guanosine Triphosphate; D019204:GTP-Binding Proteins