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@INPROCEEDINGS{Strecker:1027702,
author = {Strecker, Jonas and Spahn, Ingo and Neumaier, Bernd and
Giesen, Kai and Gülez, Salim},
title = {52g{M}n({II})-{L}abelled {PSMA}-ligands as bimodal
{PET}/{MR} imaging probes},
issn = {0969-8051},
reportid = {FZJ-2024-04012},
year = {2022},
abstract = {Introduction: By combining the advantages of two or more
complementaryimaging modalities, hybrid techniques like
PET/MR allowfor sequential or simultaneous acquisition of
anatomical and molecularinformation. Although the alignment
of hybrid datasets acquiredin simultaneous PET/MR has been
shown to be more accurate, thereis still a lack of probes
for bimodal PET/MR imaging. Radiolabellingwith isotopic
mixtures of 52gMn/55Mn provides direct access to
suchprobes1,2, as the paramagnetic 55Mn acts as an MRI
contrast agent3,while 52gMn is a promising +-emitter for
PET imaging (t½ = 5.6 d, E+,end = 0,58 MeV). In the
present work, the PSMA-selective moiety Glu-C(O)-Lys was
functionalized by CuAAC click reaction with the
chelatortrans-1,2-diaminocyclohexane-N,N,N`,N`-tetraacetic
acid (CDTA)for Mn complexation and radiolabeling with 52gMn.
In addition, thestability of the novel PET/MR probe was
evaluated by preliminary invitro studies.Materials and
Methods: Following its production by the52Cr(p,n)52gMn
nuclear reaction, 52gMn was separated from the Crtarget
using anion exchange chromatography. To this end, the
Crtarget was dissolved in 2 m HCl, which was then evaporated
todryness. The residue was dissolved in MeOH/conc. HAc (1:1)
andtrapped on an AG-MP1 anion exchange column. The column
waswashed with 30 mL MeOH/conc. HAc. (1:1) at 44°C and
[52gMn]MnCl2was eluted with 3 m HCl.The CDTA ligand was
synthesized using a modification of a previouslypublished
method4 and coupled to the PSMA-selective Glu-C(O)-Lys
pharmacophore by the copper(I)-catalyzed
alkyne-azidecycloaddition (CuAAC) click reaction.The
functionalized CDTA-ligand (2.5 mg) was dissolved in 0.1
mNaOAc buffer (pH 6) and treated with no-carrier added
[52gMn]MnCl2for 30 min at ambient temperature, and the
radiolabelled productwas subsequently isolated by HPLC.The
stability of the PET/MR probe in the presence of human
serumwas measured in HBS buffer at 37°C and analysed by
HPLC.Results and Conclusion: No-carrier added 52gMn was
isolatedfrom the Cr target with a separation yield of
$93\%.$ An improved labellingprotocol for the CDTA
functionalized PSMA-selective ligand wasestablished,
yielding a radiochemical yield of 50 $\%$ (based on
HPLCanalysis of the crude product). After 24 h, $28.2\%$ of
the complex wasstill intact justifying further evaluation by
in vivo animal studies.References:[1] Thomas G. et al.
Innovative Magnetic Nanoparticles for PET/MRIBimodal
Imaging. ACS Omega. 2019, 4, 2637-2648[2] de Rosales R.T.M.
Potential clinical applications of bimodalPET-MRI or
SPECT-MRI agents J. Label Compd. Radiopharm. 2014,57,
298–303[3] Glover, P., Mansfield, S. P. Limits to magnetic
resonance microscopy.Reports Prog. Phys. 2002, 65, 1489.[4]
Vanasschen, C., Brandt, M., Ermert, J., Coenen, H. H.
Radiolabellingwith isotopic mixtures of 52g/55Mn(II) as a
straight route to stablemanganese complexes for bimodal
PET/MR imaging. Dalt. Trans.2016, 45, 1315–1321.},
month = {May},
date = {2022-05-29},
organization = {24th International Symposium on
Radiopharmaceutical Sciences, Nantes
(France), 29 May 2022 - 3 Jun 2022},
subtyp = {After Call},
cin = {INM-5},
ddc = {570},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {5253 - Neuroimaging (POF4-525)},
pid = {G:(DE-HGF)POF4-5253},
typ = {PUB:(DE-HGF)6},
doi = {10.1016/S0969-8051(22)00335-3},
url = {https://juser.fz-juelich.de/record/1027702},
}