86050-77-3

• 常用中文名：钆喷酸葡胺
• 常用英文名：Gadopentetate dimeglumine
• CAS号：86050-77-3
• 分子式：C₂₈H₅₄GdN₅O₂₀
• 分子量：938.000
• 相关类别： 原料药 诊断用药 影象检查用药
• 发布时间：2018-04-16 08:00:00
• 更新时间：2024-01-02 22:12:28
• Gadopentetate dimeglumine (SH-L-451A) 用于核磁共振成像 (MRI) 中，更清晰地看到血管，器官和其他非骨组织。

名称

• 中文名: 钆喷酸葡胺
• 英文名: gadopentetate dimeglumine
• 英文别名: Meglumine gadopentetate; Gadopentetic acid dimeglumine salt; Gadolinium-DTPA; GADOPENTETATE DIMEGLUMINE; 2-[bis[2-[carboxylatomethyl(carboxymethyl)amino]ethyl]amino]acetate,gadolinium(3+),(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol; Gd-DTPA; Dimeglumine-gadolinium-dtpa; Magnevist; Gadolinium (bis{2-[(carboxylatomethyl)(carboxymethyl)amino]ethyl}amino)acetate - (2R,3R,4R,5S)-6-(methylamino)-1,2,3,4,5-hexanepentol (1:1:2); Gadopentetate dimeglumine (JAN/USP); Gadolinium dtpa; Diethylenetriaminepentaacetic acid dimeglumine salt gadolinium chelate

物化性质

• 分子式: C₂₈H₅₄GdN₅O₂₀
• 分子量: 938.000
• 精确质量: 938.260315
• PSA: 389.58000
• 储存条件: 室温

生物活性

• 描述: Gadopentetate dimeglumine (SH-L-451A) 用于核磁共振成像 (MRI) 中,更清晰地看到血管,器官和其他非骨组织。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 其他
• 体外研究: Gadobenate dimeglumine增强MRI显着改善癌症检测,相比于钆喷酸二甲基葡胺增强MRI,乳房X线照相术和超声波在选择的一组患者进行乳房MRI进行术前分期或由于常规成像的不确定结果[1]。具有钆喷酸二葡甲胺(Gd-DTPA)或钆布酸二钠(Gd-EOB-DTPA)的间质MR淋巴造影允许健康小鼠中淋巴途径的清晰可视化,并且在两种药剂之间未发现显着差异。它们的快速动力学限制了成像定时窗口,但是,有助于在单个成像期间重复评估[2]。直接观察溢出的胃肠道钆喷酸二葡甲胺有助于在该模型中区分缺血性和对照大鼠[3]。
• 动物实验: 大鼠：麻醉28只大鼠并进行中线剖腹手术。将动物分成四组：对照，单个肠系膜拱廊的结扎，六个连续的拱廊的结扎，以及肠系膜前动脉的结扎（类似于人的肠系膜上动脉）。通过管饲法给予用无菌水（1：1）稀释的1.0mL钆喷酸二葡甲胺肠溶丸。在剖腹术后2小时进行磁共振成像，并由两位经验丰富的观察者检查腹膜内钆喷酸二葡甲胺的存在。手术后24小时处死动物进行病理检查[3]。小鼠：在六只健康小鼠的右足垫皮下注射钆喷酸二葡甲胺（Gd-DTPA）或钆布酸二钠（Gd-EOB-DTPA）（每只小鼠0.1,0.5或2.0mmol）后进行MR淋巴造影。评估对比度增强的时间过程。此外，两个不同部位的淋巴途径通过间质MR淋巴造影研究进行评估[2]。
• 参考文献:

  [1]. Gilbert FJ, et al. Comparison of gadobenate dimeglumine-enhanced breast MRI and gadopentetate dimeglumine-enhanced breast MRI with mammography and ultrasound for the detection of breast cancer. J Magn Reson Imaging. 2014 May;39(5):1272-86.

  [2]. Sheng F, et al. Interstitial MR lymphography in mice with gadopentetate dimeglumine and gadoxetate disodium. J Magn Reson Imaging. 2011 Feb;33(2):490-7.

  [3]. Montalbano JM, et al. Magnetic resonance imaging detection of extraluminal enterally administered gadopentetate dimeglumine in a rat model of intestinal ischemia. Acad Radiol. 1996 Jun;3(6):486-92.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : LW1001000 CAS REGISTRY NUMBER : 86050-77-3 LAST UPDATED : 199412 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C14-H18-Gd-N3-O10.2C7-H17-N-O5.2H HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 9411 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AAJRDX AJR, American Journal of Roentgenology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.126- 1976- Volume(issue)/page/year: 142,619,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Parenteral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 612 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AAJRDX AJR, American Journal of Roentgenology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.126- 1976- Volume(issue)/page/year: 142,619,1984 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 4291 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: (Suppl),254,1992