[125I]SCH 23982: the ligand of choice for identifying the D-1 dopamine receptor

Eur J Pharmacol. 1986 Sep 9;128(3):213-20. doi: 10.1016/0014-2999(86)90768-5.

Abstract

[125I]SCH 23982, [125I]8-iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol, binds reversibly and with high affinity (Kd = 0.7 +/- 0.05 nM) to specific binding sites (maximum binding = 108 +/- 3.5 fmol/mg) in the caudate nucleus of the rat brain. The caudate binding site displays pharmacological properties similar to the D-1 receptor; furthermore, the site has a low affinity for drugs favoring the D-2 receptor. GTP diminishes the affinity of dopamine, a D-1 agonist, but not SCH 23390, a D-1 antagonist, for the caudate binding site. The iodinated ligand discriminates between the D-1 and the D-2 dopamine receptors: the neurointermediate lobe of the rat pituitary gland, a tissue rich in D-2 dopamine receptors, possesses less than 4% of the specific binding sites in the caudate. Because [125I]SCH 23982 exists at a higher specific activity than [3H]SCH 23390, a ligand used previously to identify the D-1 receptor, and because the results obtained with the iodinated ligand are otherwise similar to those obtained with the [3H]SCH 23390, [125I]SCH 23982 is the ligand of choice for identifying the D-1 receptor.

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Benzazepines* / analogs & derivatives*
  • Benzazepines* / pharmacology*
  • Corpus Striatum / drug effects
  • Corpus Striatum / metabolism
  • Guanosine Triphosphate / pharmacology
  • In Vitro Techniques
  • Iodine Radioisotopes
  • Kinetics
  • Ligands
  • Male
  • Pituitary Gland / metabolism
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine / drug effects*
  • Receptors, Dopamine D1
  • Stereoisomerism

Substances

  • 8-iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol
  • Benzazepines
  • Iodine Radioisotopes
  • Ligands
  • Receptors, Dopamine
  • Receptors, Dopamine D1
  • Guanosine Triphosphate
  • Adenylyl Cyclases