预约演示
更新于：2025-05-25
Gadopentetate Dimeglumine
钆喷酸葡胺
更新于：2025-05-25
概要
基本信息
原研机构 |
在研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1988-06-02), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C21H36GdN4O15 |
InChIKeyLZQIEMULHFPUQY-BMWGJIJESA-J |
CAS号86050-77-3 |
关联
39
项与 钆喷酸葡胺 相关的临床试验NCT06861426
Patients with Acute Ischemic Stroke Receiving Ginkgo Diterpene Lactone Meglumine: a Patient Registry
NCT02371798
Diagnosing Endolymphatic Hydrops in Patients With Meniere Disease Using Magnetic Resonance Imaging With Intravenous Gadolinium Administration
NCT02278510
A Pilot Trial of Intraparenchymally-Administered Topotecan Using Convection-Enhanced Delivery (CED) in Patients With Suspected Recurrent/Progressive WHO Grade III or IV (High Grade) Glioma Requiring Stereotactic Biopsy
100 项与 钆喷酸葡胺 相关的临床结果
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100 项与 钆喷酸葡胺 相关的转化医学
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100 项与 钆喷酸葡胺 相关的专利（医药）
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5,308
项与 钆喷酸葡胺 相关的文献（医药）2025-05-06ANALYTICAL CHEMISTRY
Caspase-3-Responsive Dual-Enhanced 1H/19F MRI Bimodal Probe for In Vivo Tumor Apoptosis Imaging
Article
作者: Jiang, Zhong-Xing ; Luo, Yingying ; Zhu, Yue ; Yu, Qiao ; Zhang, Lei ; Xiao, Long ; Chen, Shizhen ; Li, Sha ; Zhou, Xin
Caspase-3 (Cas-3) is a crucial cysteine protease involved in executing cell apoptosis, a process that is a hallmark of tumor cell apoptosis response to chemotherapy. Developing molecular imaging probes that specifically detect apoptotic signals during tumor treatment is considered to be one of the most important and effective strategies for reducing cancer-associated death rates and improving treatment outcomes. However, achieving a dual-enhanced bimodal probe in a single molecule remains a significant challenge. In this study, we developed a 1H/19F dual-enhanced magnetic resonance imaging (MRI) probe, CF3DEVDFFFK(Fmoc)-Gd, responsive to caspase-3 for in vivo imaging of apoptotic cells. Upon interaction with caspase-3, CF3DEVDFFFK(Fmoc)-Gd efficiently splits into two components CF3DEVD and FFFK(Fmoc)-C2-Gd, where FFFK(Fmoc)-C2-Gd subsequently self-assembles into nanofibers. This process activates both 19F MRI and 1H MRI, with longitudinal relaxivity (r1) increasing from 9.38 ± 0.22 to 23.24 ± 2.33 mM-1 s-1 at 0.5 T and turning on the 19F MRI signal due to the absence of the paramagnetic relaxation enhancement (PRE) effect. In vivo imaging results demonstrated that, after systemic administration, CF3DEVDFFFK(Fmoc)-Gd effectively accumulated in apoptotic 4T1 tumor tissues, resulting in significantly enhanced 1H MRI signals for visualization of caspase-3 activity in doxorubicin-treated apoptotic 4T1 tumor tissues, with signal intensity three times greater than that of Gd-DTPA. 19F MRI further complemented 1H MRI, with a notable recovery of the 19F MRI signal after intratumoral injection. These results confirm that CF3DEVDFFFK(Fmoc)-Gd effectively reports tumor apoptosis through combined 1H and 19F MRI, offering a promising approach for the preliminary assessment of antitumor efficacy in vivo.
2025-04-23JOURNAL OF NEUROSCIENCE
Concentration-Dependent Bidirectional Modification of Evoked Synaptic Transmission by Gadolinium and Adverse Effects of Gadolinium-Based Contrast Agent
Article
作者: Zorigt, Odgerel ; Yasuda, Hiroki ; Nakajima, Takahito ; Tsushima, Yoshito
Gadolinium-based contrast agents (GBCAs) for magnetic resonance imaging (MRI) are gadolinium chelates and can leave gadolinium in brain regions after administration, causing damage to brain tissues. However, the exact effects of gadolinium on synaptic function and the underlying mechanisms have not yet been elucidated. Here, we report that gadolinium differentially modulates evoked and spontaneous synaptic transmission and induces bidirectional changes in the efficacy of evoked synaptic transmission in the mouse hippocampus in a concentration-dependent manner. Low-concentration gadolinium (100 μM) modestly potentiated evoked field excitatory postsynaptic potentials (fEPSPs), while high-concentration gadolinium induced group 1 metabotropic glutamate receptor (mGluR)-, endocannabinoid (eCB)-, and purinergic P2Y1 receptor (P2Y1R)-dependent, presynaptically expressed long-term depression (LTD). Higher concentration of gadolinium (1,000 μM) also induced NMDAR- and mGluR-independent, partially P2Y13R-dependent, postsynaptically expressed LTD. Low-concentration gadolinium greatly increased miniature excitatory postsynaptic current (mEPSC) frequency, while high-concentration gadolinium much more robustly increased its frequency and amplitude. Finally, we found that evoked EPSCs were not affected by a macrocyclic GBCA, gadoterate meglumine (Gd-GOTA, Magnescope). However, evoked EPSCs were enhanced by a linear GBCA, gadopentetate dimeglumine (Gd-DTPA, Magnevist), at 100 μM, a clinically relevant concentration in the human brain after repeated clinical GBCA administration and in the cerebrospinal fluid in the rodent brain during experimental GBCA administration. Thus, evoked and spontaneous synaptic transmissions are independently modulated by gadolinium. Furthermore, Gd-GOTA effectively chelated gadolinium; however, Gd-DTPA had side effects on the evoked synaptic transmission, presumably because it did not completely chelate gadolinium.
2025-04-01Small
One‐Dose Bioorthogonal Gadolinium Nanoprobes for Prolonged Radiosensitization of Tumor
Article
作者: Liu, Dinghua ; Shao, Chunlin ; Wu, Zhuoyao ; Yi, Jinyan ; Yang, Weitao ; Bai, Yang ; Wang, Hui ; Cui, Tianming ; Zhang, Bingbo ; Bian, Kexin
Abstract:
Developing effective radiotherapy is impeded by tumor radioresistance, imprecise treatment, and the need for accurate imaging. Herein, a multifunctional gadolinium‐based nanoprobe (GBD) is presented, integrating bioorthogonal click chemistry and theranostics to enhance tumor retention, magnetic resonance imaging (MRI) contrast, and radiosensitivity. GBD synthesis involved biomimetic mineralization of bovine serum albumin (BSA) with gadolinium ions to form nanoparticles (GB), followed by conjugation with dibenzocyclooctyne (DBCO). The optimized GBD exhibited an elevated longitudinal relaxivity (r1) of 25.54 mM−1 s−1, which represented a 6.7‐fold enhancement compared to the clinical MRI contrast agent magnevist (Gd‐DTPA, 3.81 mM−1 s−1). Notably, the application of bioorthogonal click chemistry enhanced the affinity and retention of GBD within tumor cells modified to express azide as an artificial receptor. This novel strategy enhanced tumor retention up to 16 days postinjection, outperforming DBCO‐modified small molecule gadolinium (Gd‐DBCO) with less than 1‐day retention. Such prolonged retention facilitated continuous radiosensitization throughout the radiotherapy course, negating the need for multiple injections, and substantially boosted the effectiveness of radiotherapy. This study demonstrates the transformative potential of combining bioorthogonal click chemistry with nanotechnology in radiotherapy, offering a precise tumor targeting platform, real‐time monitoring, and improved treatment outcomes.
100 项与 钆喷酸葡胺 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 造影剂 | 美国 | 1988-06-02 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 心血管畸形 | 临床3期 | - | 2003-12-01 | |
| 病理性缩窄 | 临床3期 | - | 2003-12-01 | |
| 肾动脉狭窄 | 临床3期 | - | 2003-12-01 | |
| 血管动脉疾病 | 临床3期 | - | 2003-12-01 | |
| 外周血管疾病 | 临床3期 | - | 2003-03-01 | |
| 脑转移瘤 | 临床3期 | 日本 | 2003-02-01 | |
| 心肌梗塞 | 临床2期 | 美国 | 2006-03-01 | |
| 心肌梗塞 | 临床2期 | 阿根廷 | 2006-03-01 | |
| 外周动脉疾病 | 临床2期 | 日本 | 2004-07-01 | |
| 原发性免疫缺陷疾病 | 临床2期 | 美国 | - |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 2 | 3 Tesla Magnetic Resonance Imaging+Magnevist® (Intravenous (IV) administration of MRI contrast agent) | 膚壓鬱鹽齋鏇築鏇醖遞(廠醖遞鏇淵繭鏇廠觸窪) = 壓糧鏇選鹽簾艱範鹹淵 蓋選選鏇構選襯艱齋鹹 (簾鹹觸廠顧蓋築鏇醖壓, 淵憲餘鬱醖衊顧遞鹽獵 ~ 壓築獵鹽鹽窪廠鹽簾製) 更多 | - | 2018-07-11 | ||
N/A | 17 | 鏇範鹹餘鏇積衊餘襯齋(顧簾製獵衊選顧襯餘鹹) = 鹽範窪憲積築鑰艱構構 壓製鹽鑰憲襯鏇蓋餘鹽 (壓鏇憲鬱膚願廠廠鏇艱, 5.7) 更多 | - | 2017-06-14 | |||
N/A | 6 | 鬱觸鏇蓋願蓋齋夢餘醖 = 夢觸獵築製網膚淵膚積 衊憲獵襯網網選鬱窪選 (顧淵遞淵獵遞蓋鹽繭製, 鹹顧壓觸蓋網鏇壓觸壓 ~ 製壓鏇鹹製夢選餘衊艱) 更多 | - | 2016-02-12 | |||
N/A | - | IV contrast media (Gadopentetate Dimeglumine) | 遞蓋鹹鹽範夢構鑰蓋觸(鑰憲廠鏇構範選鹹襯製) = This is a rare case of grand mal seizures that occurred in a patient without any previous seizure history and not immediately after the injection of the contrast media, as it was till now reported in the literature. 觸製範廠廠遞窪製製遞 (鹹鹽網鬱壓衊鑰範選範 ) | - | 2013-06-26 | ||
临床3期 | - | 46 | 窪願餘鹽壓獵壓衊淵獵(衊夢壓顧膚膚廠獵壓夢) = 鬱鹽鹹製齋糧壓憲壓夢 艱艱顧獵廠夢繭選窪夢 (餘獵憲顧願獵鬱壓淵顧 ) 更多 | 积极 | 2013-04-01 | ||
窪願餘鹽壓獵壓衊淵獵(衊夢壓顧膚膚廠獵壓夢) = 遞膚醖鬱選觸顧醖鏇願 艱艱顧獵廠夢繭選窪夢 (餘獵憲顧願獵鬱壓淵顧 ) 更多 |
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