Synthesis and autoradiographic localization of the dopamine D-1 agonists [11C]SKF 75670 and [11C]SKF 82957 as potential PET radioligands

Appl Radiat Isot. 1996 Mar;47(3):279-84. doi: 10.1016/0969-8043(95)00306-1.

Abstract

The high affinity benzazepine D1 agonists SKF 75670 and SKF 82957 were labeled with 11C by N-[11C]methylation of SKF 38393 and SKF 81297, respectively, using [11C]methyl iodide in the presence of N-ethyldiisopropylamine. Both radiotracers were purified using a semi-preparative cation exchange HPLC column. Radiochemical yields of 20-75% were obtained (from [11C]methyl iodide, decay-corrected) with a synthesis time of 30-35 min from EOB. The specific activities were 700-2500 Ci/mmol (25.9-92.5 GBq/mumol) at EOS, and the radiochemical purities were > 99%. Autoradiographic studies showed selective binding for both tracers in rat brain regions rich in D1 receptors such as the caudate-putamen, nucleus accumbens, olfactory tubercles and substantia nigra. [11C]SKF 75670 and [11C]SKF 82957 are thus potential PET radioligands for the functional high-affinity state of D1 receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Autoradiography
  • Benzazepines* / chemical synthesis
  • Benzazepines* / pharmacokinetics
  • Binding Sites
  • Brain / diagnostic imaging
  • Brain / metabolism
  • Carbon Radioisotopes*
  • Dopamine Agonists* / chemical synthesis
  • Dopamine Agonists* / pharmacokinetics
  • In Vitro Techniques
  • Ligands
  • Rats
  • Receptors, Dopamine D1 / agonists*
  • Tomography, Emission-Computed / methods*

Substances

  • Benzazepines
  • Carbon Radioisotopes
  • Dopamine Agonists
  • Ligands
  • Receptors, Dopamine D1
  • SK&F 75670
  • SKF 82957