Specific binding of 125I SCH 23982, a selective dopamine (D1) receptor ligand to plasma membranes derived from human kidney cortex.
Binding of the selective D-1 dopamine receptor ligand 125I SCH 23982 was studied using crude plasma membranes derived from human renal cortex. 125I SCH 23982 bound saturably to a single high affinity site (Kd = 650 pM, Bmax = 19 fmol/mg protein). Binding at 37 degrees was rapid and reversible with forward and reverse rate constants of 5.79 x 10(8) min-1 m-1 and 0.156 min-1 respectively. Antagonist and agonist competition for 125I SCH 23982 binding was also consistent with the existence of a single site possessing pharmacological characteristics similar to a D-1 dopamine receptor. It is suggested that this site may represent a D-1 (or DA1) dopamine receptor present in human renal cortex.
Hughes
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Department of Clinical Pharmacology, St Mary's Hospital Medical School, London, U.K.
Sever
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D001552:Benzazepines / Q000031:analogs & derivatives* / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D018492:Dopamine Antagonists; D006801:Humans; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D007672:Kidney Cortex / Q000378:metabolism*; D007700:Kinetics; D011954:Receptors, Dopamine / Q000032:analysis*; D017447:Receptors, Dopamine D1
C049558:8-iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol; D001552:Benzazepines; D018492:Dopamine Antagonists; D007457:Iodine Radioisotopes; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1