Some scientific research about tert-Butyl piperidin-4-ylcarbamate

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Platelet-derived growth factor receptor beta (PDGFRbeta) is a transmembrane tyrosine kinase receptor and it is upregulated in various malignant tumors. Radiolabeled PDGFRbeta inhibitors can be a convenient tool for the imaging of tumors overexpressing PDGFRbeta. In this study, [125I]-1-{5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinoline-8-yl}piperidin-4-amine ([125I]IIQP) and [125I]-N-3-iodobenzoyl-1-{2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl}-piperidin-4-amine ([125I]IB-IQP) were designed and synthesized, and their potential as PDGFRbeta imaging agents was evaluated. In cellular uptake experiments, [125I]IIQP and [125I]IB-IQP showed higher uptake by PDGFRbeta-positive cells than by PDGFRbeta-negative cells, and the uptake in PDGFRbeta-positive cells was inhibited by co-culture with PDGFRbeta ligands. The biodistribution of both radiotracers in normal mice exhibited hepatobiliary excretion as the main route. In mice inoculated with BxPC3-luc (PDGFRbeta-positive), the tumor uptake of radioactivity at 1 h after the injection of [125I]IIQP was significantly higher than that after the injection of [125I]IB-IQP. These results indicated that [125I]IIQP can be a suitable PDGFRbeta imaging agent. However, further modification of its structure will be required to obtain a more appropriate PDGFRbeta-targeted imaging agent with a higher signal/noise ratio.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H14110N – PubChem