title: Microwave-assisted synthesis of HYNIC protected analogue for 99mTc labeled antibody.
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.
authors.forename: María F
authors.initials: MF
authors.lastname: García
authors.forename: Victoria
authors.initials: V
authors.lastname: Calzada
authors.forename: Ximena
authors.initials: X
authors.lastname: Camacho
authors.forename: Enzo
authors.initials: E
authors.lastname: Goicochea
authors.forename: Juan Pablo
authors.initials: JP
authors.lastname: Gambini
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Quinn
authors.forename: Williams
authors.initials: W
authors.lastname: Porcal
authors.affiliation: Laboratorio de Radiofarmacia, Centro de Investigaciones Nucleares, Mataojo 2055, Facultad de Ciencias, Universidad de la Republica, 11400 Montevideo, Uruguay. pcabral@cin.edu.uy.
authors.forename: Pablo
authors.initials: P
authors.lastname: Cabral
mesh_terms: D061067:Antibodies, Monoclonal, Humanized / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D007553:Isotope Labeling; D008872:Microwaves; D009536:Niacinamide / Q000031:analogs & derivatives / Q000494:pharmacology; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D013667:Technetium / Q000737:chemistry*; D014269:Trifluoroacetic Acid / Q000138:chemical synthesis* / Q000493:pharmacokinetics
chemical_list: D061067:Antibodies, Monoclonal, Humanized; D019275:Radiopharmaceuticals; C530514:hydrazinonictinamide; D009536:Niacinamide; C501466:nimotuzumab; D013667:Technetium; D014269:Trifluoroacetic Acid