NOTA and NODAGA [<sup>99m</sup>Tc]Tc- and [<sup>186</sup>Re]Re-Tricarbonyl Complexes: Radiochemistry and First Example of a [<sup>99m</sup>Tc]Tc-NODAGA Somatostatin Receptor-Targeting Bioconjugate
作者:George Makris、Lauren L. Radford、Marina Kuchuk、Fabio Gallazzi、Silvia S. Jurisson、Charles J. Smith、Heather M. Hennkens
DOI:10.1021/acs.bioconjchem.8b00670
日期:2018.12.19
Radiolabeled complexes [99mTc]Tc/[186Re]Re-1/2 and [99mTc]Tc-3 were prepared in high radiochemical yield (>90%, determined by radio-HPLC) by reacting [99mTc]/[186Re][Tc/Re(OH2)3(CO)3]+ with 1–3 and correlated well with the respective Re-1 through Re-3 standards in comparative HPLC studies. All radiotracers remained intact through 24 h (99mTc-labeled complexes) or 48 h (186Re-labeled complexes) against 1 mM l-histidine
出于开发用于核医学的分子治疗剂的长期目标,在这项工作中,我们评估了[ 99m Tc / 186 Re] Tc / Re- trimethoxy核芯作为双功能螯合剂(BFC)的著名NOTA和NODAGA螯合剂。特别是,我们报告了通式为fac- [M(L)(CO)3 ] +(M = Re,99m Tc,186 Re)的模型配合物,其中L表示NOTA-Pyr(1)或NODAGA-Pyr(2),它们是由NOTA / NODAGA与吡咯烷(Pyr)偶联而成的。此外,作为原理的证明,我们合成了肽生物共轭物NODAGA-sst 2 -ANT(3)并探讨了其与fac- [Re(CO)3 ] +和fac- [ 99m Tc] [Tc(CO)3 ] +核的络合作用;sst 2 -ANT表示生长抑素受体(SSTR)拮抗剂4-NO 2 -Phe-c(DCys-Tyr-DTrp-Lys-Thr-Cys)-DTyr-NH