Structure, synthesis, and pharmacological activity of a metabolite of etimizole

Aleksandrova, I. Ya.; Ткаченко, Е. И.; Sapronov, N. S.; Sholtes, L.; Trnovets, T.; Plotrovskii, L. B.

doi:10.1007/bf00766900

Cited by 1 publication

(1 citation statement)

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“…Another advantage of the I45DC probes is the ease of modification through the schemes presented in this article, allowing adjustment of the exchange properties and biodistribution for a particular medical application. On the other hand, while some toxicity data for I45DC compounds are available in the literature, with the LD50 reported at 200–350 mg/kg in rodents , a clear advantage of the aforementioned iodinated CEST agents is their prior approval for administration to patients at high concentrations, which has allowed pilot studies of pH imaging technology in patients . Another disadvantage of the current group of I45DCs is that, with the largest chemical shift around 7.8 ppm, the k ex values (~4000/s) are still not ideal for 3 T scanners .…”

Section: Resultsmentioning

confidence: 99%

Developing imidazoles as CEST MRI pH sensors

Yang

Song

Banerjee

et al. 2016

Contrast Media & Molecular

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A series of intra-molecular hydrogen bonded imidazoles and related heterocyclic compounds were screened for their N–H chemical exchange saturation transfer (CEST) magnetic resonance imaging (MRI) contrast properties. Of the compounds, imidazole-4,5-dicarboxamides (I45DCs) were found to provide the strongest contrast, with the contrast produced at a large chemical shift from water (7.8 ppm) and strongly dependent on pH. We have tested several probes based on this scaffold, and demonstrated that these probes could be applied for in vivo detection of kidney pH after intravenous administration.

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Section: Resultsmentioning

confidence: 99%