Charaterization of Tc‐99m‐tricarbonyl complexes as transport substrates of the multidrug resistance (<i>MDR1</i>) P‐glycoprotein

Dyszlewski, Mary; Blake, Helen M.; Dahlheimer, Julie L.; Piwnica‐Worms, David

doi:10.1002/jlcr.2580440122

Cited by 2 publications

(1 citation statement)

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“…Dyszlewski also reported it as a transport substrate of the multidrug resistance Pglycoprotein. 6 Control experiments of were carried out in mice 4 and dogs 7 earlier, in which 99m Tc-CO-MIBI showed to be a promising myocardial perfusion-imaging agent with good myocardial uptake and fast liver washout. Subsequently, we found that 99m Tc-CO-MIBI was a mixture with two main components in different reaction conditions whose biodistribution results were distinctively different.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, separation and biodistribution of ^99mTc‐CO‐MIBI complex

Hao

Zang

Zhu

et al. 2004

Labelled Comp Radiopharmac

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Tc-CO-MIBI was prepared by a two-step procedure involving the convenient preparation of the [ 99m Tc(CO) 3 (OH 2 ) 3 ] + precursor and followed by the substitution of the water molecules by the MIBI (2-methoxyisobutylisonitrile) ligands. In a second step, the reaction solution was adjusted to different pH values, and then the product, 99mTc-CO-MIBI, was confirmed to be a mixture of two complexes: complex A and complex B, whose labeling yields could be over 90%. The ratio of complex B to the sum of A and B could increase gradually from 0 to 1 when pH was shifted from 3.0 to 9.0. These changes were monitored by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). The two complexes were stable within 8 h at room temperature in vitro. The partition coefficient of the two complexes indicated that there was distinct difference between them. Biodistribution in mice demonstrated that complex B showed better myocardial imaging properties than that of complex A. The heart/liver ratios of complex A, the mixture, and complex B were 1.57, 1.93, and 2.33, respectively, for 30 min post-injection. The discovery of chemical and biological properties of 99m Tc-CO-MIBI would certainly promote the research on a new promising myocardial perfusion-imaging agent.

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Section: Introductionmentioning

confidence: 99%