TAK-063 is an inhibitor of phosphodiesterase 10A (PDE10A), an enzyme highly expressed in medium spiny neurons of the striatum. PDE10A hydrolyzes both cyclic adenosine monophosphate and cyclic guanosine monophosphate and modulates dopamine signaling downstream of receptor activation in both direct and indirect pathways of the striatum. TAK-063 exhibited antipsychotic-like effects in animal models; however, the translatability of these models to the clinical manifestations of schizophrenia and the meaningfulness for new targets such as PDE10A has not been established.

中文翻译：

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TAK-063（一种磷酸二酯酶 10A 抑制剂）的转化开发策略。


TAK-063 是磷酸二酯酶 10A (PDE10A) 的抑制剂，磷酸二酯酶 10A 是一种在纹状体中型多棘神经元中高度表达的酶。 PDE10A 水解环单磷酸腺苷和环单磷酸鸟苷，并调节纹状体直接和间接通路中受体激活下游的多巴胺信号传导。 TAK-063 在动物模型中表现出抗精神病样作用；然而，这些模型对精神分裂症临床表现的可转化性以及对 PDE10A 等新靶点的意义尚未确定。