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PDE1是與中樞和外周疾病密切相關(guān)的藥物靶點(diǎn),研究人員合成一種PDE1 抑制劑在大鼠肝微粒體中具有良好的代謝穩(wěn)定性。其中穩(wěn)定性測(cè)試通過(guò)美迪西進(jìn)行

2023-07-06
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Phosphodiesterase-1 (PDE1) is a promising drug target closely related to central and peripheral diseases. Compound 2j with the IC50 of 21 nM against PDE1B, shows good metabolic stability in the rat liver microsomes. Stability test in the rat liver microsomes were performed by Medicilon.

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Reference:

Bei Zhang, et al. Design, synthesis and biological evaluation of novel pyrazolopyrimidone derivatives as potent PDE1 inhibitors. Bioorg Chem. 2021 Sep;114:105104. doi: 10.1016/j.bioorg.2021.105104. 

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