Syntheses of the first endothelin-A- and -B-selective radioligands for positron emission tomography

J Cardiovasc Pharmacol. 2000 Nov;36(5 Suppl 1):S58-60. doi: 10.1097/00005344-200036001-00020.

Abstract

We have synthesized two potential positron emission tomography (PET) radioligands for the endothelin (ET) receptor. [11C]-PD156707 was produced by O-methylation of PD169390 using [11C]iodomethane. Radiochemical conversions of the order of 74 +/- 3.2% (n = 8) were obtained. The radiochemical purity of the isolated [11C]-PD156707 was 99% and the specific activity was 538 mCi/micromol. [18F]-BQ3020 was produced from [18F]fluoride in a total radiochemical yield of 2.7 +/- 0.4% (n = 10) in 238 +/- 5 min. The radiochemical purity was 95% and specific activities of the order of 670-930 mCi/micromol were obtained.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Carbon Radioisotopes*
  • Dioxoles / chemical synthesis*
  • Endothelins / chemical synthesis*
  • Fluorine Radioisotopes*
  • Humans
  • Ligands
  • Molecular Sequence Data
  • Peptide Fragments / chemical synthesis*
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Receptors, Endothelin / analysis*
  • Tomography, Emission-Computed*

Substances

  • Carbon Radioisotopes
  • Dioxoles
  • Endothelins
  • Fluorine Radioisotopes
  • Ligands
  • PD 156707
  • Peptide Fragments
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Receptors, Endothelin
  • BQ 3020