Dissertation Abstract

Evaluation of the Iron(III) Complex of the 3,5-Diethylsulfonamide Derivative of Catechol as an Organ-selective Magnetic Resonance Imaging Contrast Agent.

Publication Number:  AI9620111
Author:  Sayed, Gary
School:  Medical College of Ohio, Toledo
Date:  1995
Pages:  113
Subject:  Magnetic Resonance Imaging

The iron (III) diethylsulfonamide derivative of catechol (Fe(III)-DESAC) is a new target selective magnetic resonance imaging contrast agent based on the second-sphere interaction mechanism. It is a highly stable tris-complex that was chemically characterized for potential use as a magnetopharmaceutical. The contrast agent was evaluated for gross toxicity and biodistribution in a Fisher 344 rat model. The agent showed no significant acute toxicity at low doses. At a higher dose, 0.15 mmol/kg, the contrast agent exhibited toxic effects in test animals. No signs of abnormal behavior or chronic toxicity was noted. Biodistribution studies revealed increased uptake by the liver parenchyma and the kidneys suggesting combined hepatobiliary and renal excretion. Its potential as a magnetopharmaceutical was evaluated using a GE Signa MRI scanner at 0.1 mmol/kg doses in phantom and an animal model. Relaxivity measurements resulted in R$„sb1$ and R$„sb2$ relaxivity values of 2.47 mM$„sp{-1}$ sec$„sp{-1}$ and 3.16 mM$„sp{-1}$ sec$„sp{-1}$, respectively. T$„sb1$-weighted MR images showed 63% increase in the liver image values and 99% increase in the kidney values. This contrast enhancement was approximately 75% greater in the healthy parenchyma compared to the imbedded mammary adenocarcinoma.

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