title: Preparation of hydrazino-modified proteins and their use for the synthesis of 99mTc-protein conjugates.
abstract: The syntheses and protein linking properties of succinimidyl 4-hydrazinobenzoate hydrochloride (SHBH) and succinimidyl 6-hydrazinonicotinate hydrochloride (SHNH), two new heterobifunctional linkers which lead to hydrazino-modified proteins, are described. SHBH-modified proteins are unstable due to the presence of the phenylhydrazine moiety. This problem was overcome by synthesizing the hydrazinopyridine analogue SHNH, and the conjugates derived from this linker are stable. Tc(V) oxo precursors readily add to hydrazinopyridine-modified proteins to yield the desired 99mTc-radiolabeled protein. 99mTc-hydrazinopyridine-polyclonal IgG conjugates are useful agents for the imaging of focal sites of infection.
authors.affiliation: Johnson Matthey Pharmaceutical Research, West Chester, Pennsylvania 19380-1497.
authors.forename: D A
authors.initials: DA
authors.lastname: Schwartz
authors.forename: M J
authors.initials: MJ
authors.lastname: Abrams
authors.forename: M M
authors.initials: MM
authors.lastname: Hauser
authors.forename: F E
authors.initials: FE
authors.lastname: Gaul
authors.forename: S K
authors.initials: SK
authors.lastname: Larsen
authors.forename: D
authors.initials: D
authors.lastname: Rauh
authors.forename: J A
authors.initials: JA
authors.lastname: Zubieta
mesh_terms: D003432:Cross-Linking Reagents / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D007074:Immunoglobulin G / Q000737:chemistry; D007553:Isotope Labeling / Q000379:methods; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D015609:Organotechnetium Compounds / Q000737:chemistry; D010659:Phenylhydrazines / Q000138:chemical synthesis / Q000737:chemistry*; D011506:Proteins / Q000737:chemistry*; D013388:Succinimides / Q000138:chemical synthesis / Q000737:chemistry*; D013400:Sugar Acids / Q000737:chemistry; D013667:Technetium / Q000737:chemistry*
chemical_list: D003432:Cross-Linking Reagents; D007074:Immunoglobulin G; D015609:Organotechnetium Compounds; D010659:Phenylhydrazines; D011506:Proteins; D013388:Succinimides; D013400:Sugar Acids; C073103:succinimidyl 4-hydrazinobenzoate; C073102:succinimidyl 6-hydrazinonicotinate; D009536:Niacinamide; D013667:Technetium; C100014:technetium Tc 99m gluceptate