scholarly journals Re-Evaluations of Zr-DFO Complex Coordination Chemistry for the Estimation of Radiochemical Yields and Chelator-to-Antibody Ratios of 89Zr Immune-PET Tracers

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4977
Author(s):  
Ryota Imura ◽  
Hiroyuki Ida ◽  
Ichiro Sasaki ◽  
Noriko S. Ishioka ◽  
Shigeki Watanabe

(1) Background: Deferoxamine B (DFO) is the most widely used chelator for labeling of zirconium-89 (89Zr) to monoclonal antibody (mAb). Despite the remarkable developments of the clinical 89Zr-immuno-PET, chemical species and stability constants of the Zr-DFO complexes remain controversial. The aim of this study was to re-evaluate their stability constants by identifying species of Zr-DFO complexes and demonstrate that the stability constants can estimate radiochemical yield (RCY) and chelator-to-antibody ratio (CAR). (2) Methods: Zr-DFO species were determined by UV and ESI-MS spectroscopy. Stability constants and speciation of the Zr-DFO complex were redetermined by potentiometric titration. Complexation inhibition of Zr-DFO by residual impurities was investigated by competition titration. (3) Results: Unknown species, ZrHqDFO2, were successfully detected by nano-ESI-Q-MS analysis. We revealed that a dominant specie under radiolabeling condition (pH 7) was ZrHDFO, and its stability constant (logβ111) was 49.1 ± 0.3. Competition titration revealed that residual oxalate inhibits Zr-DFO complex formation. RCYs in different oxalate concentration (0.1 and 0.04 mol/L) were estimated to be 86% and >99%, which was in good agreement with reported results (87%, 97%). (4) Conclusion: This study succeeded in obtaining accurate stability constants of Zr-DFO complexes and estimating RCY and CAR from accurate stability constants established in this study.

2015 ◽  
Vol 3 (1) ◽  
pp. 25 ◽  
Author(s):  
Abdalazeem Omar ◽  
Elmugdad Ali

<p>The present work, deals with the study of proton-ligand (pK) and metal-ligand (logK) of acetic acid, oxalic acid, and oxalacetic acid with Cr (Ⅲ) and Zr (IV) by potentiometric titration technique. The stoichiometries and stability constants of these complexes were evaluated, usingCalvin-Bjerrum pH-titration technique as adopted by Irriving and Rossotti.</p><p>Graphic and algebraic methods have been employed, for determination of the stability constants, in purpose to select the most accurate and sensitive method. Furthermore, aiming to determine, the factor that effectingthe precision of those methods under investigation, and to compare the complexes of these ligands with first and second series transition elements of D-block Cr and Zr taken as an example. The obtained results were in a good agreement with each other.</p>


1986 ◽  
Vol 84 ◽  
Author(s):  
Jordi Bruno ◽  
Ignasi Casas ◽  
Bo Lagerman ◽  
Maria Munoz

AbstractWe have measured the solubility 8f amorphous UO2in a wide pH range (2 to 10.5), in 0.5 M NaClO, at T=25 C. The species responsible for the solubility are U(OH) + and U'0H)h, with the stability constants lo:1,3=-1.1± 0.1 and log, 4 =- 5.4_.O. 2, respectively. No evidence for U(OH) is f6und up to pH=10.5. The same model explains satisfactorily the solubility data obtained by Parks and Pohl(5) at T=1000 C., in the pH range 1 to 10. The measured solubility of amorphous UO2 (s) in the pH_ýange 6 to 10.5, under reducing conditions, is rather high,. U(IV) =5 10 mols/l. This is in good agreement with previous data of Gayer and Leider(6) and Galkin and Stepanov(9).


2021 ◽  
Vol 14 ◽  
Author(s):  
Kurtulus Eryilmaz ◽  
Benan Kilbas

Background: Synthesis of 225Actinium derivatives using PSMA-617, DOTATATE peptides and EDTMP ligand was afforded. Detailed experimental, quality control (QC) and stability studies were well described. The radiolabelling reactions were performed in mild conditions with desirable radiochemical yields and high radiochemical purities. Methods: PSMA-617, and DOTATATE were radiolabelled with 225Actinium in 0.1 M HCl in the presence of ascorbate buffer solution and passed through the C-18 light cartridge for purification and the product was eluted by ethanol-water solution. EDTMP was also radiolabelled with 225Actinium without using any stabilizer and purification step. All products were well analyzed by R-TLC and R-HPLC. The stability of those compounds was also studied within the valid time. Results: 225Ac-DOTATATE and 225Ac-PSMA-617 were obtained at the same condition. The radiochemical yield of 225Ac-DOTATATE was less than 225Ac-PSMA 617. Stability experiments indicated decay daughters of 225Actinium appeared after T0 +1 h due to the recoil effect radiolysis. On the other hand, 225Ac-EDTMP was more stable than DOTA-peptide radiolabelled compounds. 225Ac-EDTMP was produced with more than 95% radiochemical yield and 99% radiochemical purity. Conclusion: A detailed chemistry study was presented for the synthesis of 225Actinium derivatives in mild conditions with absolute radiochemical purities and high yields. Experimental results showed that 225Ac-EDTMP could be a suitable alternative radiopharmaceutical for bone metastases arising from primer tumors as a cocktail therapy.


2020 ◽  
Vol 129 (1D) ◽  
pp. 15-23
Author(s):  
Mai Van Bay ◽  
Nguyen Khoa Hien ◽  
Hoang Kim Thanh ◽  
Pham Cam Nam ◽  
Duong Tuan Quang

Accurately predicting the stability constant ( ) of the Cu2+ complex with organic fluorescent ligands provides an important basis to design molecular fluorescent sensors for selective detection of Cu2+. With appropriate reference complexes, the calculated stability constants are in good agreement with experimental values. The  values of the predicted stability constants of Cu2+ complexes with Calcein blue (H3Cb) and FluoZin-1 (H2Fz) are 13.33 (exp. 14.27) and 6.59 (exp. 6.01), respectively. More importantly, the results could be applied to the investigation of complexes.


1985 ◽  
Vol 50 (3) ◽  
pp. 581-599 ◽  
Author(s):  
Petr Vaňura ◽  
Emanuel Makrlík

Extraction of microamounts of Sr2+ and Ba2+ (henceforth M2+) from the aqueous solutions of perchloric acid (0.0125-1.02 mol/l) by means of the nitrobenzene solutions of dicarbolide (0.004-0.05 mol/l of H+{Co(C2B9H11)2}-) was studied in the presence of monoglyme (only Ba2+), diglyme, triglyme, and tetraglyme (CH3O-(CH2-CH2O)nCH3, where n = 1, 2, 3, 4). The distribution of glyme betweeen the aqueous and organic phases, the extraction of the protonized glyme molecule HL+ together with the extraction of M2+ ion and of the glyme complex with the M2+ ion, i.e., ML2+ (where L is the molecule of glyme), were found to be the dominating reactions in the systems under study. In the systems with tri- and tetraglymes the extraction of H+ and M2+ ions solvated with two glyme molecules, i.e., the formation of HL2+ and ML22+ species, can probably play a minor role. The values of the respective equilibrium constants, of the stability constants of complexes formed in the organic phase, and the theoretical separation factors αBa/Sr were determined. The effect of the ligand structure on the values of extraction and stability constants in the organic phase is discussed.


2012 ◽  
Vol 239-240 ◽  
pp. 1573-1576
Author(s):  
Zhu Qing Gao ◽  
Xiao Dong Cai ◽  
Kai Cheng Ling

At different temperatures, the protonation constants of tannic acid and the complex apparent stability constants between tannic acid and VO2+ were determined by using pH potentimetric method. The results showed that the protonation constants and the complex apparent stability constants slightly decreased with the raising temperature. In accordance with the pH value in the tannin extract technology, the conditional stability constants of the complex were calculated on the basis of the acid effect of tannic acid and the hydrolysis effect of VO2+. It was found that pH greatly affected the stability constants of the complex , so pH must be strictly controlled in the tannin extract technology.


1992 ◽  
Vol 38 (4) ◽  
pp. 562-565 ◽  
Author(s):  
M A Kline ◽  
C Orvig

Abstract The stability constants for the Fe(III) complexes of the orally active iron decorporation drug L1 (3-hydroxy-1,2-dimethyl-4-pyridinone) have been determined by potentiometric titration [glass electrode, 25.0 degrees C, mu = 0.15 mol/L (isotonic) NaCl]. A simple computer model of blood plasma (citrate 100 mumol/L, transferrin 37 mumol/L) has been used to compare the Fe(III) binding efficacies in blood of L1 and the clinically used intravenously administered chelating agent deferoxamine.


2006 ◽  
Vol 17 (01) ◽  
pp. 65-73 ◽  
Author(s):  
SHIRO SAWADA

The optimal velocity model which depends not only on the headway but also on the relative velocity is analyzed in detail. We investigate the effect of considering the relative velocity based on the linear and nonlinear analysis of the model. The linear stability analysis shows that the improvement in the stability of the traffic flow is obtained by taking into account the relative velocity. From the nonlinear analysis, the relative velocity dependence of the propagating kink solution for traffic jam is obtained. The relation between the headway and the velocity and the fundamental diagram are examined by numerical simulation. We find that the results by the linear and nonlinear analysis of the model are in good agreement with the numerical results.


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