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153Sm3+ and 111In3+ DTPA derivatives with high hepatic specificity: in vivo and in vitro studies

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TLDR
Two DTPA derivatives, a mono-amide derivative containing an iodinated synthon, DTPA-IOPsp and the ligand DTPA(BOM) 3, were studied as potential hepatospecific gamma scintigraphic agents, showing that the main excretory pathway for all the chelates studied is the hepatobiliary system.
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This article is published in Journal of Inorganic Biochemistry.The article was published on 2002-07-25 and is currently open access. It has received 10 citations till now.

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Journal ArticleDOI

Silencing of Phosphonate-Gadolinium Magnetic Resonance Imaging Contrast by Hydroxyapatite Binding

TL;DR: In vitro experiments demonstrated that GdDOTP5−-induced changes in relaxivity were silenced upon HA binding but could be recovered by acid elution of the complex, suggesting a novel strategy for creating highly sensitive, switchable MRI contrast agents.
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In vivo MRI assessment of a novel GdIII-based contrast agent designed for high magnetic field applications.

TL;DR: The dynamic gamma scintigraphic studies and the biodistribution experiments performed in Wistar rats with (153)Sm-enriched (*)Sm(3)L are indicative of a fast elimination via the kidneys, and the ratio of the relaxivities of the two compounds determined in vitro is retained under in vivo conditions.
Journal ArticleDOI

Radiotheranostics with radiolanthanides: Design, development strategies, and medical applications

TL;DR: This review discusses radiotheranostics with radiolanthanides, focusing on the design, development strategies, and medical applications of radiolAnthanide-labeled probes.
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Lanthanide chelates of (bis)-hydroxymethyl-substituted DTTA with potential application as contrast agents in magnetic resonance imaging.

TL;DR: The bis-hydroxymethyl-substituted DTTA skeleton can be seen as a new lead for the synthesis of high relaxivity contrast agents, although its low thermodynamic and kinetic stability will limit its use to in vitro and animal studies.
References
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Gadolinium-ethoxybenzyl-DTPA, a new liver-specific magnetic resonance contrast agent. Kinetic and enhancement patterns in normal and cholestatic rats.

TL;DR: Data indicate that transport of Gd-EOB-DTPA through the liver into bile is driven by the organic anion transporter, indicating that persistent enhancement of liver, even in the presence of severe hyperbilirubinemia, should be sufficient to identify focal mass lesions.
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The role of the canalicular multispecific organic anion transporter in the disposal of endo- and xenobiotics.

TL;DR: A wide range of glucuronide-, glutathione- and sulfate-conjugates are transported by this system, and TR- rats, which lack c MOAT activity, have been valuable in defining the substrate specificity of cMOAT.
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Molecular mechanisms for the hepatic uptake of magnetic resonance imaging contrast agents.

TL;DR: Data indicate that the hepatic uptake of the MRI contrast agent Gd-B 20790 is a carrier-mediated mechanism operated by OATP while MRI compounds with other chemical structures enter the hepatocyte by other mechanisms.
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Preparation, physico-chemical characterization, and relaxometry studies of various gadolinium(III)-DTPA-bis(amide) derivatives as potential magnetic resonance contrast agents

TL;DR: The chelates containing long alkyl side chains, such as Gd(DTPA-HPA2), showed increased relaxivity values in the presence of human serum albumin (HSA), indicative of noncovalent interaction with the protein, which could be useful as nonionic hepatobiliary contrast agents.
Journal ArticleDOI

Identification and functional characterization of the promoter region of the human organic anion transporting polypeptide gene

TL;DR: Reverse‐transcription polymerase chain reaction analysis showed an increase in OATP messenger RNA in the livers of four patients with chronic cholestatic liver disease compared with three noncholestasis controls, suggesting the up‐regulation of O ATP expression by taurocholate could serve to enhance the sinusoidal efflux of toxic intracellular compounds during chronic choledude.
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Q1. What contributions have the authors mentioned in the paper "Sm and in dtpa derivatives with high hepatic specificity: in vivo and in vitro studies" ?

Two DTPA derivatives, a mono-amide derivative containing an iodinated synthon, DTPA-IOPsp ( L ) and the ligand DTPA ( BOM ) 1 3 153 31 111 31 ( BOM5benzyloxymethyl ) ( L ), radiolabelled with Sm and In, were studied as potential hepatospecific gamma scintigraphic 2 agents. In vivo studies with Wistar rats show that the main excretory pathway for all the chelates studied is the hepatobiliary system. The La 31 1 and In chelates of L and L show some structural and dynamic differences in aqueous solution, as studied by H NMR spectroscopy.