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

Authors
Johnstrom, P Aigbirhio, FI Clark, JC Downey, SPMJ Pickard, JD Davenport, AP
Citation
P. Johnstrom et al., Syntheses of the first endothelin-A- and -B-selective radioligands for positron emission tomography, J CARDIO PH, 36, 2000, pp. S58-S60
Citations number
9
Categorie Soggetti
Cardiovascular & Respiratory Systems","Cardiovascular & Hematology Research
Journal title
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY
ISSN journal
01602446 → ACNP
Volume
36
Year of publication
2000
Supplement
1
Pages
S58 - S60
Database
ISI
SICI code
0160-2446(2000)36:<S58:SOTFEA>2.0.ZU;2-A
Abstract
We have synthesized two potential positron emission tomography (PET) radiol igands for the endothelin (ET) receptor. [C-11]-PD156707 was produced by O- methylation of PD169390 using [C-11]iodomethane. Radiochemical conversions of the order of 74 +/- 3.2% (n = 8) were obtained. The radiochemical purity of the isolated [C-11]-PD156707 was 99% and the specific activity was 538 mCi/mu mol. [F-18]-BQ3020 was produced from [18F]fluoride in a total radioc hemical yield of 2.7 +/- 0.48 (n = 10) in 238 +/- 5 min. The radiochemical purity was 95% and specific activities of the order of 670-930 mCi/mu mol w ere obtained.