Abstract
We described herein a simple and efficient microwave assisted synthesis of HYNIC analogues. Two different activated esters of HYNIC, the hydrazine protected with a trifluoroacetyl group (5) and the free hydrazine (6) were conjugated to the monoclonal antibody Nimotuzumab. Technetium-99m radiolabeling of Nimotuzumab was achieved with high efficiency using 5 and 6 derivates. The NHS-HYNIC-Tfa derivate allowed better labeling yields during longer times of preservation of the conjugated antibody.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Antibodies, Monoclonal, Humanized / chemistry*
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Antibodies, Monoclonal, Humanized / pharmacokinetics
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Humans
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Isotope Labeling*
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Microwaves*
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Niacinamide / analogs & derivatives
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Niacinamide / pharmacology
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacokinetics
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Technetium / chemistry*
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Trifluoroacetic Acid / chemical synthesis*
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Trifluoroacetic Acid / pharmacokinetics
Substances
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Antibodies, Monoclonal, Humanized
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Radiopharmaceuticals
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hydrazinonictinamide
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Niacinamide
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nimotuzumab
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Technetium
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Trifluoroacetic Acid