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Nuclear Medicine and Biology

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Presentation on theme: "Nuclear Medicine and Biology"— Presentation transcript:

1 Nuclear Medicine and Biology
Novel pyridine-containing azacrown-ethers for the chelation of therapeutic bismuth radioisotopes: Complexation study, radiolabeling, serum stability and biodistribution  Egorova B.V. , Matazova E.V. , Mitrofanov A.A. , Aleshin G.Yu. , Trigub A.L. , Zubenko A.D. , Fedorova O.A. , Fedorov Yu.V. , Kalmykov S.N.   Nuclear Medicine and Biology  Volume 60, Pages 1-10 (May 2018) DOI: /j.nucmedbio Copyright © Terms and Conditions

2 Fig. 1 Structures and abbreviated names of ligands investigated in this work L1–L6, and known in literature H4DOTA, H3DO3A-Bu, H5DTPA, H4EDTA, L7. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

3 Fig. 2 Mass-spectra of L6·Bi complex in positive (a) and negative (b) mode. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

4 Fig. 3 1H NMR spectra of a) L6 and b) L6⋅Bi3+ in D2O at pH 2.5 at 298 K. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

5 Fig. 4 Dependence of the extraction of Bi3+ by 0.01 M HDEHP in toluene on ligand concentration in aqueous phase in terms of Eq. (1) for: a) L1, L2 and L3 (pH 3.00 ± 0.05); b) L4 (pH 3.10 ± 0.05 and 4.10 ± 0.05); c) L5 (pH 3.10 ± 0.05 and 4.30 ± 0.05); d) L6 (pH 3.10 ± 0.05). Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

6 Fig. 5 Dependence of D0D−1L on [L] for L2 in terms of Eq. (3) upon extraction by 0.01 M HDEHP in toluene. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

7 Fig. 6 Dependence of Bi3+ concentration in aqueous phase on concentration of ligands L5 (a) and L6 (b) at different pH. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

8 Fig. 7 Dependence of calculated logKapp for L·Bi3+ on pH: a) L1–L3; b) L4–L6. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

9 Fig. 8 Dependence of Kapp on OH– concentration in terms of Eq. (4) for ligands: a) L5; b) L4. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

10 Fig. 9 Relationship between logKBiL and ∑pKa for ligands studied in this work and L7, DOTA and DO3A-Bu. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

11 Fig. 10 Optimized geometry of L6⋅Bi3+ complex in two views.
Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

12 Fig. 11 The fitted spectrum of X-ray absorption for L6⋅Bi3+ in R- and k-spaces. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

13 Fig. 12 Radiolabeling yield of 207Bi and L6 in ligand's concentrations varying in the range 0.01–1 mM. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions

14 Fig. 13 Time-dependent chelation of 207Bi3+ by serum proteins and its transchelation from complexes with EDTA and L6. Nuclear Medicine and Biology  , 1-10DOI: ( /j.nucmedbio ) Copyright © Terms and Conditions


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