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首页> 外文期刊>Journal of Medicinal Chemistry >Gadolinium-free Magnetic Resonance Imaging of the Liver via an Oatp1-Targeted Manganese(III) Porphyrin
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Gadolinium-free Magnetic Resonance Imaging of the Liver via an Oatp1-Targeted Manganese(III) Porphyrin

机译:Gadolinium-free Magnetic Resonance Imaging of the Liver via an Oatp1-Targeted Manganese(III) Porphyrin

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摘要

Controversy surrounding gadolinium-based contrast agents (GBCAs) has rendered their continued utility highly contentious, but the liver-specific GBCA Gd­(III) ethoxybenzyl-diethylene triamine pentaacetic acid (Gd­(III)-EOB-DTPA) remains in use because it provides unique diagnostic information that could not be obtained by any other means. To address the need for an alternate liver-specific MRI probe, we synthesized Mn­(III) 20-(4-ethoxyphenyl) porphyrin-5,10,15-tricarboxylate (Mn­(III)­TriCP-PhOEt), which exhibited significantly higher r 1 relaxivity than Gd­(III)-EOB-DTPA in vitro, while also targeting hepatocyte-specific organic anion-transporting polypeptide 1 (Oatp1) channels as a marker of viability. In mice, Mn­(III)­TriCP-PhOEt resulted in significant and specific increases in liver signal intensity on T 1-weighted images and significant decreases in liver T 1 time relative to pre-contrast measurements. Our findings suggest that Mn­(III)­TriCP-PhOEt operates as a specific and sensitive MR probe for Oatp1-targeted imaging in vivo.

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