D-Amino Acid Oxidase 抑制剤 (CAS 39793-31-2)

D-Amino Acid Oxidase Inhibitor is a cell-permeable thienopyrrole compound that potently inhibits cellular activity of transfected D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) in CHO cells (IC₅₀ against human and rat DAO = 145 and 114 nM, respectively). Exhibits no activity towards D-aspartate oxidase (DDO; IC₅₀ >5 µM), P450 enzymes CYP3A4/2D6/3C9 (IC₅₀ >10 µM), and a panel of over 150 other enzymes, receptors, and ion channels. Although treatment of Compound 8 (200 mg/kg, i.p.) is shown to effectively inhibit DAO activity in rat brain and kidney (by 96% and 80%, respectively), the resulting D-serine concentration increase in the periphery and central nervous system appears to be far from sufficient to produce adequate antipsychotic and cognitive enhancing effects.

参考文献

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