Abstract
In this study a bispidine ligand has been applied to the complexation of gallium(III) and radiolabelled with gallium-68 for the first time. Despite its 5-coordinate nature, the resulting complex is stable in serum for over two hours, demonstrating a ligand system well matched to the imaging window of gallium-68 positron emission tomography (PET). To show the versatility of the bispidine ligand and its potential use in PET, the bifunctional chelator was conjugated to a porphyrin, producing a PET/PDT-theranostic, which showed the same level of stability to serum as the non-conjugated gallium-68 complex. The PET/PDT complex killed >90 % of HT-29 cells upon light irradiation at 50 μm. This study shows bispidines have the versatility to be used as a ligand system for gallium-68 in PET.
Highlights
Positron emission tomography (PET) is a highly sensitive imaging technique with high tissue penetration.[1–3] This technique can allow for the in vivo imaging of diseased tissues by targeting biochemical processes; allowing for detection of disease before physical changes occur
The methyl group attached to the amine of the bispidine ring is significantly deshielded (CH3, ΔδH = 0.9 ppm); this suggests that the amine of the ring is involved in complexation
We describe the application of a bispidine ligand, L1, to the complexation of Ga(III)
Summary
Evaluation of a bispidine-based chelator for gallium-68 and of the porphyrin conjugate as PET/PDT theranostic agent. Yap,[c] Dr Raphaël Gillet,[d] Huguette Savoie,[c] Dr Loïc J.
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