Studies of technetium-99m nitridobisdithiocarboxylate leucocyte specific radiopharmaceutical: [99mTcN(DTCX)2], DTCX = CH3(CH2)8CS2. The cellular and subcellular distribution in human blood cells, and chemical behaviour. Synthesis of the analogous rhenium-188 radiopharmaceutical.
The distribution of the radiopharmaceutical ([99mTcN(DTCX)2], DTCX = CH3(CH2)8CS2) in the leucocyte population determined by a density separation with double gradient Polymorphprep was studied. Microautoradiographic analysis showed a subcellular distribution of the radiomarker in human blood cells. This technique confirmed the observed lymphocyte selectivity (69%) and revealed that the uptake was predominantly cytoplasmic around the nucleus. A labeling mechanism by passive endocytosis could be proposed involving a required lipophilicity of the radiopharmaceutical for lymphocyte targeting. Finally, we describe the new synthesis with an efficient yield and radiochemical purity of the analogous radiopharmaceutical [188ReN(DTCX)2].
Demaimay
F
F
Laboratoire de Chimie Organique et Des Substances Naturelles, CNRS ESA 6052, Ecole Nationale Suprieure de Chimie de Rennes, France.
Roucoux
A
A
Dazord
L
L
Noiret
N
N
Moisan
A
A
Patin
H
H
D001345:Autoradiography; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D006801:Humans; D007962:Leukocytes / Q000378:metabolism*; D008214:Lymphocytes / Q000378:metabolism; D009942:Organometallic Compounds / Q000138:chemical synthesis*; D015609:Organotechnetium Compounds / Q000097:blood* / Q000493:pharmacokinetics; D011854:Radiochemistry; D019275:Radiopharmaceuticals / Q000097:blood* / Q000138:chemical synthesis; D013347:Subcellular Fractions / Q000378:metabolism*
D009942:Organometallic Compounds; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C119667:rhenium nitridobisdithiocarboxylate; C119666:technetium Tc 99m nitridobisdithiocarboxylate