《标记化合物和放射性药物杂志》发表了涉及标记化合物制备和这些化合物应用的研究的所有方面。这包括用于体外和体内医学、药理学、生物学、生化和化学研究的示踪方法。《标记化合物和放射性药物杂志》特别关注放射性药物的生物医学研究、诊断和治疗应用，涵盖从基础到发展的所有阶段基于物理和化学特征的分子结构、配位化合物和纳米粒子的代谢研究和技术开发到临床前和临床研究。

The Journal of Labelled Compounds and Radiopharmaceuticals publishes research covering all aspects of the preparation and application of labelled compounds. This includes tracing methods used in in vitro and in vivo medicine, pharmacology, biology, biochemistry, and chemical research. The journal places special emphasis on biomedical research involving radiopharmaceuticals, as well as their diagnostic and therapeutic applications, covering all stages from fundamental studies to preclinical and clinical research, focusing on the metabolic studies and technological developments of molecular structures, coordination compounds, and nanoparticles based on their physical and chemical characteristics.

《Journal of Labelled Compounds and Radiopharmaceuticals》发表涉及标记化合物制备及其应用的研究，涵盖所有相关领域。这些领域包括体外和体内医学、药理学、生物学、生化和化学研究中的示踪方法。该期刊特别关注放射性药物的生物医学研究及其在诊断和治疗中的应用，涵盖从基础研究到临床前和临床研究的各个阶段，涉及基于物理和化学特征的分子结构、配位化合物和纳米粒子的代谢研究与技术开发。

Journal of Labelled Compounds and Radiopharmaceuticals

Cytochrome P450 (P450) enzymes account for ~75% of the metabolism of drugs. Most of the reactions catalyzed by P450s are mixed‐function oxidations, and a C–H bond is (usually) broken. The rate‐limiting nature of this step can be analyzed using the kinetic isotope effect (KIE) approach. The most relevant type of KIE is one termed intermolecular non‐competitive, indicative of rate‐limiting C–H bond breaking. A plot of KIE versus k cat for several P450s showed a correlation coefficient ( r 2 ) of 0.62. Deuterium substitution has been considered as a potential means of slowing drug metabolism or redirecting sites of metabolism in some cases, and several general points can be made regarding the potential for application of deuterium in drug design/development based on what is known about P450 KIEs. Copyright © 2013 John Wiley &amp; Sons, Ltd.

F. Peter Guengerich

Kinetic deuterium isotope effects in cytochrome P450 oxidation reactions

细胞色素P450氧化反应中的动力学氘同位素效应

ABSTRACT Immune checkpoint therapy has emerged as an effective treatment option for various types of cancers. Key immune checkpoint molecules, such as cytotoxic T‐lymphocyte‐associated protein 4 (CTLA‐4), programmed cell death protein 1 (PD‐1), and lymphocyte activation gene 3 (LAG‐3), have become pivotal targets in cancer immunotherapy. Antibodies designed to inhibit these molecules have demonstrated significant clinical efficacy. Nevertheless, the ability to monitor changes in the immune status of tumors and predict treatment response remains limited. Conventional methods, such as assessing lymphocytes in peripheral blood or conducting tumor biopsies, are inadequate for providing real‐time, spatial information about T‐cell distributions within heterogeneous tumors. Positron emission tomography (PET) using T‐cell specific probes represents a promising and noninvasive approach to monitor both systemic and intratumoral immune changes during treatment. This technique holds substantial clinical significance and potential utility. In this paper, we review the applications of PET probes that target immune cells in molecular imaging.

Xingguo Hou

Xiangxing Kong

Yuan Yao

Song Liu

Ya'nan Ren

Muye Hu

Zilei Wang

Hua Zhu

Zhi Yang

Next Generation of Solid Target Radionuclide Antibody Conjugates for Tumor Immuno‐Therapy

下一代用于肿瘤免疫治疗的固体靶向放射性核素抗体偶联物

ABSTRACT The rise of nucleic acid‐based therapeutics continues apace. At the same time, the need for radiolabelled oligonucleotides for determination of spatial distribution is increasing. Complex molecular structures with mostly multiple charges and low solubility in organic solvents increase the challenge of integrating radionuclides. In preclinical research, it is important to understand the fate of new drug candidates in biodistribution studies, target binding or biotransformation studies. Depending on a specific question, the selection of a respective radiolabelling strategy is crucial. Radiometals for molecular imaging with positron emission tomography or single‐photon computed tomography generally require an attached chelating agent for stable complexation of the metal with the oligonucleotide, whereas labelling using carbon‐11/‐14 or tritium allows incorporation of the radioisotope into the native structure without altering it. Moreover, the suitability of direct radiolabelling of the oligonucleotide of interest or indirect radiolabelling, for example, by a two‐step pretargeting approach, for the study design requires consideration. This review focuses on the challenges of radiolabelling nucleic acid‐based molecules with beta‐plus, gamma and beta‐minus emitters and their use for tracking and monitoring.

Martin R. Edelmann

Filippo Sladojevich

Stephen M. Husbands

Michael B. Otteneder

Ian S. Blagbrough

A Brief Review of Radiolabelling Nucleic Acid‐Based Molecules for Tracking and Monitoring

放射性标记核酸分子用于追踪和监测的简要综述

ABSTRACT Deuterium‐labeled pyocyanin was prepared from deuterium‐labeled phenazine methosulfate in gram scale by a simplified flow photosynthesis in water. The main product was the protonated red form of pyocyanin‐d 3 (Pyo‐d 3 ‐H + ) in 85 % yield. Quantum chemical calculations of NMR support that nitrogen‐10 is protonated. The by‐products of the photolysis and the stability of the photolysis mixture were carefully characterized by LC‐MS and NMR. Four by‐products were identified: An isomer of pyocyanin‐d 3 (9%), 8‐hydroxypyocyanin‐d 3 (4%), 1‐hydroxyphenazine (0.4%), and phenazine (1%). The Pyo‐d 3 ‐H + product was stable in the photolysis solution after storage at 8°C for 2.5 years. Pure blue pyocyanin‐d 3 powder was isolated from the red photolysis solution by the Surrey method in 94 % yield. The addition of the red photolysis solution of Pyo‐d 3 ‐H + (100 μM) and commercial pyocyanin (100 μM) to Pseudomonas aeruginosa cultures showed the same growth curves demonstrating that the minor impurities in the photolysis solution do not affect the growth behavior of the bacteria. The protonated deuterium‐labeled pyocyanin may be used directly in biological experiments, which make the methodology extremely simple and useful for biologists.

Torben Lund

Niels Jacob Krake

Poul Erik Hansen

Fatima AlZahraa Alatraktchi

Simplified Flow Photosynthesis of Deuterium‐Labeled Pyocyanin

简化流式光合作用中的氘标记绿脓菌素

ABSTRACT DOTA‐functionalized bisphosphonates can be useful tools for PET imaging of bone metastases when radiolabeled with 68 Ga. Moreover, the versatility of DOTA allows the complexation of radiometals with therapeutic applications (e.g., 177 Lu), positioning these bisphosphonates as attractive theranostic agents. Among these molecules, BPAMD is a compound whose radiolabeling with 68 Ga has already been described, but only through manual methods. Thus, a fully automated protocol for 68 Ga radiolabeling of BPAMD on the GAIA® ± LUNA® synthesis module was designed, and a thorough study of the radiolabeling conditions was undertaken. [ 68 Ga]Ga‐BPAMD was produced in good radiochemical purity (&gt; 93%) and high radiochemical yield (&gt; 91%) using 0.3 M HEPES buffer. The nature of the reaction vessel showed no significant effect on the radiolabeling outcome. Similarly, addition of an antiradiolysis compound to the reaction medium did not significantly improve the already excellent stability of [ 68 Ga]Ga‐BPAMD over time. The radiolabeled product obtained by automated synthesis was evaluated in vivo in healthy mice and confirmed high accumulation in the joints and along the backbone.

Céleste Souche

Juliette Fouillet

Léa Rubira

Charlotte Donzé

Audrey Sallé

Yann Dromard

Emmanuel Deshayes

Cyril Fersing

Towards Optimal Automated 68Ga‐Radiolabeling Conditions of the DOTA‐Bisphosphonate BPAMD Without Pre‐Purification of the Generator Eluate

迈向无需发生器洗脱液预纯化的DOTA-双膦酸盐BPAMD的68Ga放射性标记最佳自动化条件

ABSTRACT Herein, the successful syntheses of D 3 ‐ and 13 C‐ N ‐methyl and D 9 ‐ tert‐ butyl Hoechst dyes are presented. This includes the preparation of the labelled D 3 ‐ and 13 C‐ N‐ methyl piperazines and D 9 ‐ tert ‐butylated hydroxytoluene precursors. The tert‐ butyl Hoechst dye is known to bind a specific RNA aptamer. Spectroscopic NMR studies of the labelled Hoechst dye‐aptamer complexes allowed for the unambiguous assignment of chemical shifts, as well as the dynamics of the bound dye.

Yulia A. Vlasenko

Avery J. To

Tess Fortier

Natasha M. Evans

Cole J. Lindsay

Peter J. Palermo

Thorsten Dieckmann

Graham K. Murphy

Synthesis and Application of D‐ and 13C‐Labelled tert‐Butyl Hoechst Dye

D‐和13C‐标记的叔丁基Hoechst染料的合成与应用

Abbreviation	Labelled Comp Radiopharmac
Journal Impact	0.83
Quartiles(Global)	CHEMISTRY, MEDICINAL(Q4)

ISSN	0022-2135, 0362-4803, 1099-1344
h-index	54

Publication Information	Publisher: John Wiley and Sons Ltd，Publishing cycle: ，Journal Type: journal，Open Access Journals: No
Basic data	Year of publication: 1976，Proportion of original research papers: ，Self Citation Rate:， Gold OA Rate:

Journal of Labelled Compounds and Radiopharmaceuticals

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Kinetic deuterium isotope effects in cytochrome P450 oxidation reactions

Next Generation of Solid Target Radionuclide Antibody Conjugates for Tumor Immuno‐Therapy

A Brief Review of Radiolabelling Nucleic Acid‐Based Molecules for Tracking and Monitoring

Simplified Flow Photosynthesis of Deuterium‐Labeled Pyocyanin

Towards Optimal Automated ⁶⁸Ga‐Radiolabeling Conditions of the DOTA‐Bisphosphonate BPAMD Without Pre‐Purification of the Generator Eluate

Towards Optimal Automated ⁶⁸Ga‐Radiolabeling Conditions of the DOTA‐Bisphosphonate BPAMD Without Pre‐Purification of the Generator Eluate

A Brief Review of Radiolabelling Nucleic Acid‐Based Molecules for Tracking and Monitoring

Simplified Flow Photosynthesis of Deuterium‐Labeled Pyocyanin

Next Generation of Solid Target Radionuclide Antibody Conjugates for Tumor Immuno‐Therapy

Synthesis and Application of D‐ and ¹³C‐Labelled tert‐Butyl Hoechst Dye