Preparation of a Promising Angiogenesis PET Imaging Agent: ⁶⁸Ga-Labeled c(RGDyK)–Isothiocyanatobenzyl-1,4,7-Triazacyclononane-1,4,7-Triacetic Acid and Feasibility Studies in Mice

Development of 68Ga-labeled multivalent nitroimidazole derivatives for hypoxia imaging

“…Due to the commercial availability of NOTA and DOTA derivatives, these are extensively used for conjugational chemistry related to medical imaging, including 68 Ga applications [36,46,47]. Actually, NOTA-based ligands showed higher selectivity towards Ga 3+ ion and their complexes are more stable, as the size of the NOTA cavity is almost ideal for this ion [40,48].…”

“…68 Ga (t1/2 = 68 min, 89% β+, Eβ+max = 1.92 MeV, 11% EC) is a generator-produced radionuclide that offers excellent coordination chemistry with a wide range of bifunctional chelating agents. It also provides rapid radiolabeling in various pH ranges [35][36][37][38][39][40][41][42].…”

Current Molecular Imaging Positron Emitting Radiotracers in Oncology

“…However, due to the in vivo stability, cyclic RGD is more favorable than linear RGD and has been well studied by labeling with various radioisotopes [62]. 18 F-Galacto-c(RGDfK), radiolabeled PEGylated RGD peptide, F-18-labeled RGD dimer [63], tetramer [64], Cu-64-labeled tetramer and octamer [65], and Ga-68-labeled cyclic RGD dimers [66,67] are all reported in searching for improved pharmacokinetic behaviors, including better tumor uptake and a prolonged retention pattern (Fig. 3).…”

68Ga-Labeled Radiopharmaceuticals for Positron Emission Tomography

“…We previously found that the PET imaging agent, 68 Ga-NOTA-RGD, can be used to visualize angiogenesis in ischemic tissue, and α v β 3 integrin expression was found to play an important role [13]. Because angiogenesis is known to occur at ischemic lesions during cancer development, we used two animal biodistribution models, a hind limb ischemia and a SNU-C4 (a human colon cancer cell line) xenograft model.…”

“…68 Ga-1,4,7,10-tetra-azacyclododecane-1,4,7,10-tetraacetic acidTyr3-octreotide (DOTA-TOC), 68 Ga-DOTA-1-Nal-octreotide (DOTA-NOC), 68 Ga-DOTA-bombesin, 68 Ga-1,4,7-triazacyclononanetriacetic acid (NOTA)-RGD, 68 Ga-DOTAalbumin, and 68 Ga-DOTA-human epidermal growth factor (hEGF) are examples of such agents (Fig. 1) [8,[10][11][12][13][14][15]. Similarly, some agents, such as 68 Ga-[(4,6-MeO 2 sal) 2-BAPEN] + and 68 Ga-N 2 S 2 , are chelates of radioactive gallium and used for myocardial imaging [16][17][18].…”