The synthesis of [26,27-11C]dihydroxyvitamin D(3), a tracer for positron emission tomography (PET). |
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Authors: | Thomas A Bonasera Gunnar Grue-S rensen Giuseppina Ortu Ernst Binderup Mats Bergstr m Fredrik Bj rkling and Bengt L ngstr m |
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Institution: | a Uppsala University PET Centre, UAS, SE-751 85 Uppsala, Sweden b Department of Medicinal Chemistry, Leo Pharmaceutical Products, Industriparken 55, DK-2750 Ballerup, Denmark |
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Abstract: | 1 ,25-Dihydroxyvitamin D3, an endogenous ligand with the highest affinity for the vitamin D receptor (VDR), was labeled with 11C for use in biological experiments. The radionuclide was incorporated via the reaction of 11C]methyllithium on a methyl ketone precursor in tetrahydrofuran at ?10 °C. Deprotection of the labeled intermediate yielded 2.5–3 GBq 26,27-11C]1 ,25-dihydroxyvitamin D3 11C-1,25(OH)2 D3] with specific radioactivity averaging 100 GBq/μmol at the end of synthesis and HPLC purification. The entire process took 48 min from the end of radionuclide production. In vitro binding experiments in rachitic chick purified VDR demonstrated the high affinity binding of this novel tracer. Thus; 11C-1,25(OH)2 D3 is available for in vivo distribution studies and may be suitable for the positron emission tomography (PET) determination of VDR levels and occupancy in animals and humans. |
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