perrhenate-188

• 分子结构分类: 无机化合物 - 各种无机化合物 - 无机氧化物
• 英文名称: perrhenate-188
• 英文别名: (199)Re-perrhenate ion；oxido(trioxo)(188Re)rhenium-188
• 化学式: O₄Re
• 分子量: 251.998
• InChiKey: WPWXHJFQOFOBAC-INZTZQCYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.55
• 重原子数：
  5
• 可旋转键数：
  0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  74.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  perrhenate-188 、 1,1,1-三甲基-N-(三苯基正膦亚基)硅烷胺 以 甲苯 为溶剂， 以>95的产率得到
  参考文献：
  名称：

  Katti, K. V.; Singh, P. R.; Katti, K. K., Phosphorus, Sulfur and Silicon and the Related Elements, 1993, vol. 75, # 1-4, p. 55 - 58

  摘要：

  DOI：

文献信息

• Rhenium and Technetium-oxo Complexes with Thioamide Derivatives of Pyridylhydrazine Bifunctional Chelators Conjugated to the Tumour Targeting Peptides Octreotate and Cyclic-RGDfK
  作者：Andrea J. North、John A. Karas、Michelle T. Ma、Philip J. Blower、Uwe Ackermann、Jonathan M. White、Paul S. Donnelly

  DOI：10.1021/acs.inorgchem.7b01247

  日期：2017.8.21

  form pyridylthiosemicarbazide ligands (SHYNIC). The new bidentate ligands were conjugated to the tumor targeting peptides Tyr3-octreotate and cyclic-RGD. The new ligands and conjugates were used to prepare well-defined M═O}3+ complexes (where M = 99mTc or natRe or 188Re) that feature two targeting peptides attached to the single metal ion. These new SHYNIC ligands are capable of forming well-defined

  这项研究旨在利用new和coordination之间配位化学的相似性来开发靶向肿瘤的新型治疗药物。锝的γ发射放射性同位素在诊断成像中是常用的，并且有两个β -铼的具有要在放射治疗的潜在发射放射性同位素。已经通过将硫酰胺官能团附加到6-肼基烟酰胺上形成吡啶基硫代氨基脲化合物（SHYNIC），制备了6-肼基烟酰胺（HYNIC）双功能配体的变体。将新的双齿配体缀合至肿瘤靶向肽Tyr 3-奥曲肽和环状RGD。新的配体和缀合物用于制备定义明确的M═O} 3+配合物（其中M = 99m Tc或nat Re或188 Re），其特征是两个靶向肽附着在单个金属离子上。这些新的SHYNIC配体能够形成明确的rh和tech配合物，并提供使用99m Tc成像和188/186 Re治疗匹配对的可能性。
• Technetium-99m and rhenium-188 complexes with one and two pendant bisphosphonate groups for imaging arterial calcification
  作者：Jayanta Kumar Bordoloi、David Berry、Irfan Ullah Khan、Kavitha Sunassee、Rafael Torres Martin de Rosales、Catherine Shanahan、Philip J. Blower

  DOI：10.1039/c4dt02965h

  日期：——

  The synthesis of the first technetium-99m and rhenium-188 complexes with two pendant bisphosphonate groups is described, along with their in vivo use in imaging the skeleton and arterial calcification.

  描述了第一个具有两个挂链双膦酸盐基团的锝-99m和铼-188配合物的合成，以及它们在体内用于成像骨骼和动脉钙化的应用。
• Re-188 Enhances the Inhibitory Effect of Bevacizumab in Non-Small-Cell Lung Cancer
  作者：Jie Xiao、Xiaobo Xu、Xiao Li、Yanli Li、Guobing Liu、Hui Tan、Hua Shen、Hongcheng Shi、Dengfeng Cheng

  DOI：10.3390/molecules21101308

  日期：——

  The malignant behaviors of solid tumors such as growth, infiltration and metastasis are mainly nourished by tumor neovascularization. Thus, anti-angiogenic therapy is key to controlling tumor progression. Bevacizumab, a humanized anti-vascular endothelial growth factor (VEGF) antibody, plus chemotherapy or biological therapy can prolong survival for cancer patients, but treatment-related mortality is a concern. To improve inhibitory effect and decrease side-effects on non-small-cell lung cancer (NSCLC), we used Re-188, which is a β emitting radionuclide, directly labeled with bevacizumab for radioimmunotherapy in a human A549 tumor model. Cytotoxic assay data showed that, after 188ReO4− or 188Re-bevacizumab at different concentration for 4 and 24 h, a time- and radioactivity does-dependent reduction in cell viability occurred. Also, an apoptosis assay conformed great apoptosis in the 188Re-bevacizumab group compared with controls and other treatment groups. In vivo, tumor volumes in the 188Re-bevacizumab (11.1 MBq/mice) group were not reduced but growth was delayed compared with other groups. Thus, 188Re-bevacizumab enhanced the therapeutic effect of bevacizumab, suggesting a potential therapeutic strategy for NSCLC treatment.

  实体瘤的恶性行为，如生长、浸润和转移，主要由肿瘤新生血管形成提供营养。因此，抗血管生成疗法是控制肿瘤进展的关键。贝伐单抗是一种人源化抗血管内皮生长因子（VEGF）抗体，与化疗或生物疗法联合使用可延长癌症患者的生存期，但治疗相关死亡率令人担忧。为了改善抑制效果并减少对非小细胞肺癌（NSCLC）的副作用，我们使用Re-188，这是一种β发射放射性核素，直接标记贝伐单抗，用于人类A549肿瘤模型的放射免疫治疗。细胞毒性测定数据显示，在188ReO4-或188Re-贝伐单抗不同浓度下作用4和24小时后，细胞活力出现时间和放射性依赖性降低。此外，与对照组和其他治疗组相比，188Re-贝伐单抗组中的细胞凋亡测定结果也符合细胞凋亡。在体内，与其他组相比，188Re-贝伐单抗（11.1 MBq/小鼠）组的肿瘤体积没有减少，但生长延迟。因此，188Re-贝伐单抗增强了贝伐单抗的治疗效果，为NSCLC治疗提供了潜在的治疗策略。
• Structural Study by NMR of an Oxorhenium−RGD Decapeptide Complex for Application in Radiotherapy
  作者：Basil Costopoulos、Dimitra Benaki、Maria Pelecanou、Emmanuel Mikros、Chariklia I. Stassinopoulou、Alexandra D. Varvarigou、Spyridon C. Archimandritis

  DOI：10.1021/ic049519c

  日期：2004.9.1

  (Re-188) yielding a single, stable oxorhenium complex. This complex is being evaluated for possible application in oncology as a target-specific radiotherapeutic agent, because its radioactive technetium-99m analogue has already been applied for the scintigraphic detection of malignant melanoma in humans. For structural characterization purposes, the complex of the decapeptide was synthesized at the macroscopic

  十肽Arg-Gly-Asp-Ser-Cys-Arg-Gly-Asp-Ser-Tyr，其序列中包含两个Arg-Gly-Asp（RGD）部分，已成功用放射性rh标记（Re-188）产生单一的稳定的stable鎓配合物。由于该复合物的放射性tech 99m类似物已被用于人体恶性黑色素的闪烁显像检测，因此正在评估这种复合物作为靶标特异性放射治疗剂在肿瘤学中的可能应用。出于结构表征的目的，使用非放射性rh（Re-185 / Re-187）在宏观水平上合成了十肽的配合物。非放射性氧化or络合物的NMR和质谱分析表明，十肽通过Asp3的N（酰胺），Ser4的N（酰胺）与氧化or核配位，
• Preparation and evaluation of 188Re-labeled octreotide analog in C6 glioma tumor
  作者：Mostafa Erfani、Zhila Fallah、Mostafa Goudarzi、Azadeh Mikaeili

  DOI：10.1007/s10967-024-09479-6

  日期：2024.5

  In the present study, preparation of [188Re]Re-Tricine-HYNIC-Tyr3-octreotide, stability in human serum, internalization, cell viability analysis, and in vivo tissue biodistribution in rats bearing C6 glioma tumor were investigated. Radiolabeled peptide exhibited a molar activity of 8.60 ± 0.76 GBq/µmol, with over 90% (n = 3) of radiochemical yield. The findings indicated significant internalization

  在本研究中，研究了[ 188 Re]Re-Tricine-HYNIC-Tyr 3 -奥曲肽的制备、在人血清中的稳定性、内化、细胞活力分析以及在患有C6神经胶质瘤肿瘤的大鼠中的体内组织生物分布。放射性标记肽的摩尔活性为 8.60 ± 0.76 GBq/μmol，放射化学产率超过 90% (n = 3)。研究结果表明，放射性标记的肽显着内化到神经胶质瘤细胞中，并且在 MTT 分析中能够降低癌细胞的活力。在注射后的不同时间点观察到高肿瘤与肌肉比率。结果表明，放射性标记的肽可考虑用于治疗表达生长抑素受体的肿瘤。