title: Comparative evaluation of Bis(thiosemicarbazone)- Biotin and Met-ac-TE3A for tumor imaging.
abstract: 2,2',2″-(11-(2-((4-mercapto-1-methoxy-1-oxobutan-2-yl)amino)-2-oxoethyl)-1,4,8,11-tetraaza cyclotetradecane-1,4,8-triyl)triacetic acid, Met-ac-TE3A and (E)-N-methyl-2-((E)-3-(2-(2-(5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoyl)hydrazinecarbono-thioyl)hydrazonobutan-2-ylidene)hydrazinecarbothioamide, Bis(thiosemicarbazone)- Biotin were synthesized and evaluated for imaging application. The pharmacokinetics of these ligands were determined by tracer methods. In vitro human serum stability of (99m)Tc Met-ac-TE3A/(99m)Tc Bis(thiosemicarbazone)-Biotin after 24h was found to be 96.5% and 97.0% respectively. Blood kinetics of both ligands in normal rabbits showed biphasic clearance pattern. Ex vivo biodistribution study revealed significant initial tumor uptake and high tumor/muscles ratio which is a pre-requisite condition for a ligand to work as SPECT-radiopharmaceutical for tumor imaging.
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi 110054, India; Department of Chemistry, Banaras Hindu University, Varanasi 221005, India.
authors.forename: Sweta
authors.initials: S
authors.lastname: Singh
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi 110054, India.
authors.forename: Anjani K
authors.initials: AK
authors.lastname: Tiwari
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi 110054, India.
authors.forename: Raunak
authors.initials: R
authors.lastname: Varshney
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi 110054, India.
authors.forename: R
authors.initials: R
authors.lastname: Mathur
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi 110054, India.
authors.forename: Gauri
authors.initials: G
authors.lastname: Shukla
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi 110054, India.
authors.forename: N
authors.initials: N
authors.lastname: Bag
authors.affiliation: Department of Chemistry, Banaras Hindu University, Varanasi 221005, India.
authors.forename: B
authors.initials: B
authors.lastname: Singh
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi 110054, India. Electronic address: akmishra63@gmail.com.
authors.forename: Anil K
authors.initials: AK
authors.lastname: Mishra
mesh_terms: D000085:Acetates / Q000737:chemistry*; D000818:Animals; D001681:Biological Assay; D001710:Biotin / Q000138:chemical synthesis / Q000737:chemistry*; D045744:Cell Line, Tumor; D003952:Diagnostic Imaging / Q000379:methods*; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008819:Mice, Nude; D009369:Neoplasms / Q000175:diagnosis*; D011199:Potentiometry; D011522:Protons; D011817:Rabbits; D019275:Radiopharmaceuticals; D044967:Serum / Q000378:metabolism; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000737:chemistry*; D014018:Tissue Distribution
chemical_list: D000085:Acetates; D006573:Heterocyclic Compounds, 1-Ring; C000610665:Met-ac-TE3A; D011522:Protons; D019275:Radiopharmaceuticals; D013882:Thiosemicarbazones; D001710:Biotin
keywords: Amino Acid; Biodistribution; Imaging; Kinetics; Macrocycles