Journal of Cardiovascular Pharmacology 2000-11-01

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

P Johnström, F I Aigbirhio, J C Clark, S P Downey, J D Pickard, A P Davenport

Index: J. Cardiovasc. Pharmacol. 36(5 Suppl 1) , S58-60, (2000)

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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.

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