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Preclinical evaluation of Gd-EOB-DTPA as a contrast agent in MR imaging of the hepatobiliary system.
Abstract
Gadolinium diethylenetriaminepentaacetic acid (DTPA) covalently linked to the lipophilic ethoxybenzyl moiety (Gd-EOB-DTPA) was designed for use as a contrast agent in hepatobiliary magnetic resonance imaging. With T1 relaxivity values of 8.7 L/mmol.second in plasma and 16.6 L/mmol.second in rat liver tissue and a median lethal dose of 10 mmol/kg when administered intravenously in mice and rats, Gd-EOB-DTPA has a fairly high margin of safety. In rats and monkeys, biodistribution studies performed 7 days after administration of 0.25 mmol/kg revealed very little retention of gadolinium (less than 1%) in the tissues, indicating complete elimination via renal and biliary excretion. Biliary excretion was inhibited by coadministration of sulfobromophthalein, indicating the involvement of a carrier-mediated transport system based on the enzyme glutathione-S-transferase. In rats, the biliary transport maximum was 5 mumol gadolinium/min.kg. High T1 relaxivity of Gd-EOB-DTPA in rat liver in vivo can be explained by transient interaction with intracellular components and by increased microviscosity inside the hepatocyte.
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Cited by
Villaraza, A. J. L., Bumb, A., & Brechbiel, M. W. (2010) · Chemical Reviews · doi:10.1021/cr900232t · Cited by 632
Huppertz, A., Balzer, T., Blakeborough, A., Breuer, J., Giovagnoni, A., Heinz-Peer, G., Laniado, M., Manfredi, R. M., Mathieu, D. G., Mueller, D., et al. (2004) · Radiology · doi:10.1148/radiol.2301020269 · Cited by 396
Gadoxetate acid-enhanced MR imaging for HCC: A review for clinicians
Chanyaputhipong, J., Low, S.-C. A., & Chow, P. K. H. (2011) · International Journal of Hepatology · doi:10.4061/2011/489342 · Cited by 41
Metadata
- Authors
- Schuhmann-Giampieri, G., Schmitt-Willich, H., Press, W. R., Negishi, C., Weinmann, H. J., & Speck, U.
- Venue
- Radiology
- Published
- 1992-04
- Volume
- 183
- Issue
- 1
- Pages
- 59-64
- ISSN
- 0033-8419 (ISSN-L)
- 1527-1315
- OpenAlex
- W1964911576
- Cited by
- 380
- References
- 0
- FWCI
- 9.88
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Preclinical evaluation of Gd-EOB-DTPA as a contrast agent in MR imaging of the hepatobiliary system. https://app.cochat.ai/papers/10.1148/radiology.183.1.1549695
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- Schuhmann-Giampieri, G., Schmitt-Willich, H., Press, W. R., Negishi, C., Weinmann, H. J., & Speck, U. (1992). Preclinical evaluation of Gd-EOB-DTPA as a contrast agent in MR imaging of the hepatobiliary system. Radiology. https://doi.org/10.1148/radiology.183.1.1549695
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