Syntheses of the First Endothelin-A- and -B-Selective Radioligands for Positron Emission Tomography

Authors:
  • PJPeter Johnstrüm
    Peter Johnstrüm
  • FAFranklin I. Aigbirhio
    Franklin I. Aigbirhio
  • JCJohn C. Clark
    John C. Clark
  • SDSteve P.M.J. Downey
    Steve P.M.J. Downey
  • JPJohn D. Pickard
    John D. Pickard
  • ADAnthony P. Davenport
    Anthony P. Davenport
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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.