Technetium carbonyl marked 2-nitroimidazole complex as well as preparation method and application thereof
A technology of nitroimidazole and carbonyl technetium, applied in the field of radionuclide-labeled compounds, can solve the problems of unsatisfactory clinical imaging performance, low absolute tumor uptake, slow tissue clearance, etc. Imaging diagnostic effect and drug intake improvement effect
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[0058] Preparation method of carbonyl technetium-labeled 2-nitroimidazole complex
[0059] [ 99m Tc(CO) 3 (NNN-PEG 3 -NIM)] + , [ 99m Tc(CO) 3 (NNO-PEG 3 -NIM)] and [ 99m Tc(CO) 3 (NOO-PEG 3 -NIM)] - Preparation of:
[0060] Freshly prepared [ 99m Tc(CO) 3 (H 2 O) 3 ] + The intermediate was adjusted to pH = 7 with 1N and 0.01N hydrochloric acid; 0.1 mL of 500 μg / mL NNN-PEG was added to a vial 3 -NIM or NNO-PEG 3 -NIM or NOO-PEG 3 -NIM ligand solution, 0.4mL intermediate solution (10mCi) whose pH value has been adjusted and 0.5mL PBS solution with pH=7.4, shake well and heat in a boiling water bath for 15min to obtain the desired product. The structural formula of each corresponding product is shown in formula 3:
[0061]
[0062] [ 99m Tc(CO) 3 (NNN-PEG 3 -NIM)] + [ 99m Tc(CO) 3 (NNO-PEG 3 -NIM)] [ 99m Tc(CO) 3 (NOO-PEG 3 -NIM)] -
[0063]
[0064] Formula 3: Structure of carbonyl technetium-labeled 2-nitroimidazole complex
[0065] Detect...
Embodiment 4
[0068] Example 4: Lipid-water partition coefficient of carbonyl technetium-labeled 2-nitroimidazole complexes
[0069] Mix equal volumes of n-octanol and phosphate buffer (25mM, pH=7.4), add an appropriate amount of labeled complex to be tested, shake fully, and centrifuge at high speed to separate layers, take equal volumes of organic phase and aqueous phase, and measure the two phases respectively. The radioactive count of the phase, the partition coefficient P of the complex to be measured is the ratio of the radioactive count of the organic phase to the aqueous phase, and the operation is repeated many times to obtain the average value. The lipid-water partition coefficient is generally expressed in LogP.
[0070] Measurement result shows that each complex is water-soluble, [ 99m Tc(CO) 3 (NNN-PEG 3 -NIM)] + , [ 99m Tc(CO) 3 (NNO-PEG 3 -NIM)] and [ 99m Tc(CO) 3 (NOO-PEG 3 -NIM)] - The Log P values were -1.11±0.08, -0.44±0.10, -1.64±0.10, respectively.
[0071...
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