Iodination and radiolabeling of alpha-allocryptopine with iodine-125.
A procedure for labeling of alpha-allocryptopine with 125I is reported in this article. Alpha-allocryptopine is first iodinated with largely excessive iodine monochloride, and then radiolabeled by isotopic exchange with Na125I in a dichloromethane-water two-phase system. The radiochemical purity and yield of the labeled product are typically as high as 94% and 72%, respectively. Further chromatographic purification gives a highly pure product (radiochemical purity > 99%). The distribution of 125I-labeled alpha-allocryptopine in mice at 2 h after injection shows that the uptake of radioiodine in thyroid is negligibly low.
Wei
Yu
Y
Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, PR China.
Wei
Xionghui
X
Wang
Yi
Y
Liu
Xinqi
X
Chu
Taiwei
T
Hu
Shaowen
S
Wang
Xiangyun
X
D000818:Animals; D001600:Berberine Alkaloids / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D004355:Drug Stability; D007457:Iodine Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D007553:Isotope Labeling / Q000379:methods*; D008657:Metabolic Clearance Rate; D051379:Mice; D009928:Organ Specificity; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D013961:Thyroid Gland / Q000000981:diagnostic imaging* / Q000378:metabolism*; D014018:Tissue Distribution
D001600:Berberine Alkaloids; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; C109505:allocryptopine