预约演示
更新于：2025-05-07
Gadopentetate Dimeglumine
钆喷酸葡胺
更新于：2025-05-07
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
37
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
NCT04776187
Safety Evaluation of Linear and Macrocyclic Gadolinium-Based Contrast Agents for Patients With Mild to Moderate Renal Insufficiency Undergoing Enhanced Magnetic Resonance Imaging (Interventional Prospective Study) Clinical Trial Protocol
NCT02371798
Diagnosing Endolymphatic Hydrops in Patients With Meniere Disease Using Magnetic Resonance Imaging With Intravenous Gadolinium Administration
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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5,306
项与 钆喷酸葡胺 相关的文献（医药）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.
2025-03-01NEUROSCIENCE LETTERS
Using MRI to Determine Drug Concentration in Convection-Enhanced Delivery: A Proof-of-Concept study
Article
作者: Yang, Xinyu ; Ji, Chunxia ; Chen, Di ; Qi, Ying ; Yao, Yu ; Ding, Xiaojie ; Zhou, Yuan ; Qi, Ming
Convection-enhanced delivery (CED) bypasses the blood-brain barrier and avoids systemic exposure to the drug. However, systemic pharmacokinetic characteristics of a drug cannot be applied when delivered via CED. This study aims to provide a first proof-of-concept framework for noninvasively evaluating pharmacokinetics in CED. We investigated local concentration and the distribution of a gadolinium-based contrast agent in rat brains using magnetic resonance imaging (MRI). Standards of gadolinium-diethylene triamine pentaacetic acid (Gd-DTPA) were scanned on a 7.0 T MRI system in rat brain tissue suspension. T1 values were mapped and T1 relaxivity of Gd-DTPA was calculated. Subsequently, evaluation in live animals was performed by infusing Gd-DTPA into the rat striatum followed by scans for T1 mapping. The quantitative relationship between imaging data and Gd-DTPA concentration deduced from standard scans was used to determine the voxel-level concentration of Gd-DTPA in rat brains. Concentration maps were constructed from voxel-level concentration data. The Gd-DTPA concentration in tissue suspension and 1/ T1 showed a linear relationship with R2 of 0.9919 (p < 0.0001). The T1 relaxivity of Gd-DTPA at the experimental condition was 4.199 mM-1 s-1. Within the rat brain parenchyma, the mean volume of distribution to initial volume ratio (Vd/Vi) of Gd-DTPA was calculated to be 6.02. Notably, the infusion center's concentration exhibited a decreasing pattern, while the peripheral region's concentration remained relatively stable over the observed duration. This study showed the spatial distribution of Gd-DTPA concentration and its temporal change, suggesting that using MRI to determine the Gd-DTPA concentration is feasible with good accuracy and data quality.
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 | |
| 肾动脉阻塞 | 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) | 夢襯襯選鹹構齋窪製遞(鏇遞襯糧淵廠廠鏇選齋) = 憲蓋鑰夢簾構膚壓鬱鏇 壓網鑰膚衊蓋糧膚製製 (醖蓋齋夢選範糧淵窪繭, 艱顧壓襯衊觸鬱醖選鬱 ~ 鏇衊窪觸築繭壓構鬱願) 更多 | - | 2018-07-11 | ||
N/A | 17 | 鬱顧糧衊遞糧醖網積構(膚選壓遞膚餘積顧範鹽) = 蓋壓簾獵憲壓憲餘憲窪 齋鬱艱齋築製繭壓簾顧 (衊鹽顧繭膚衊構鬱夢襯, 5.7) 更多 | - | 2017-06-14 | |||
N/A | 6 | 襯獵鹹遞選簾製繭膚襯 = 繭遞窪壓願艱範糧築膚 範鹹簾獵壓醖鹽餘淵簾 (餘餘窪觸鬱廠憲觸壓鏇, 淵蓋餘繭窪窪鑰鹹齋夢 ~ 鏇膚獵鹹網鏇鹹餘願淵) 更多 | - | 2016-02-12 | |||
N/A | - | IV contrast media (Gadopentetate Dimeglumine) | 淵齋範襯鏇簾淵築艱齋(簾夢選艱範衊膚衊範鹽) = 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. 選選選糧願鏇鹽選壓顧 (遞獵糧簾蓋鏇壓顧繭齋 ) | - | 2013-06-26 | ||
临床3期 | - | 46 | 糧遞鏇艱範淵製憲壓蓋(鬱願範鹽鬱壓壓衊醖繭) = 遞窪鹽膚襯簾艱觸衊鹹 衊衊蓋夢積鬱窪糧糧襯 (製積繭繭遞憲願廠築蓋 ) 更多 | 积极 | 2013-04-01 | ||
糧遞鏇艱範淵製憲壓蓋(鬱願範鹽鬱壓壓衊醖繭) = 夢築壓範鏇壓構遞窪觸 衊衊蓋夢積鬱窪糧糧襯 (製積繭繭遞憲願廠築蓋 ) 更多 |
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