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Fluorine-18 Labeled Fluorofuranylnorprogesterone ([18F]FFNP) and Dihydrotestosterone ([18F]FDHT) Prepared by "Fluorination on Sep-Pak" Method.
Basuli, Falguni; Zhang, Xiang; Blackman, Burchelle; White, Margaret E; Jagoda, Elaine M; Choyke, Peter L; Swenson, Rolf E.
Afiliação
  • Basuli F; Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD 20850, USA. bhattacharyyaf@mail.nih.gov.
  • Zhang X; Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD 20850, USA.
  • Blackman B; Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD 20850, USA.
  • White ME; Molecular Imaging Program, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
  • Jagoda EM; Laboratory of Genitourinary Cancer Pathogenesis, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
  • Choyke PL; Molecular Imaging Program, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
  • Swenson RE; Molecular Imaging Program, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
Molecules ; 24(13)2019 Jun 28.
Article em En | MEDLINE | ID: mdl-31261651
ABSTRACT
To further explore the scope of our recently developed "fluorination on Sep-Pak" method, we prepared two well-known positron emission tomography (PET) tracers 21-[18F]fluoro-16α,17α-[(R)-(1'-α-furylmethylidene)dioxy]-19-norpregn-4-ene-3,20-dione furanyl norprogesterone ([18F]FFNP) and 16ß-[18F]fluoro-5α-dihydrotestosterone ([18F]FDHT). Following the "fluorination on Sep-Pak" method, over 70% elution efficiency was observed with 3 mg of triflate precursor of [18F]FFNP. The overall yield of [18F]FFNP was 64-72% (decay corrected) in 40 min synthesis time with a molar activity of 37-81 GBq/µmol (1000-2200 Ci/mmol). Slightly lower elution efficiency (~55%) was observed with the triflate precursor of [18F]FDHT. Fluorine-18 labeling, reduction, and deprotection to prepare [18F]FDHT were performed on Sep-Pak cartridges (PS-HCO3 and Sep-Pak plus C-18). The overall yield of [18F]FDHT was 25-32% (decay corrected) in 70 min. The molar activity determined by using mass spectrometry was 63-148 GBq/µmol (1700-4000 Ci/mmol). Applying this quantitative measure of molar activity to in vitro assays [18F]FDHT exhibited high-affinity binding to androgen receptors (Kd~2.5 nM) providing biological validation of this method.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Di-Hidrotestosterona / Radioisótopos de Flúor / Norpregnenos Limite: Female / Humans / Male Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Di-Hidrotestosterona / Radioisótopos de Flúor / Norpregnenos Limite: Female / Humans / Male Idioma: En Ano de publicação: 2019 Tipo de documento: Article