The functional role of cytochrome P450 (CYP) enzymes in the brain is an exciting and evolving field of research. CYPs are present and active in the brain, with heterogeneous patterns of expression, activity, and sensitivity to modulation across cell types, regions, and species. Despite total brain CYP expression being a fraction of hepatic CYP expression, the expanding literature of in vitro and in vivo experiments has provided evidence that brain CYPs can impact acute and chronic drug response, susceptibility to damage by neurotoxins, and are associated with altered personality, behaviour, and risk of neurological disease. They may also play a role in endogenous neurotransmitter and neurosteroid homeostasis. This review goes through the characterization of brain CYPs across species, the patterns of susceptibility of brain CYPs to exogenous induction, and recent preclinical evidence of the potential role of brain CYPs in vivo (e.g. CYP2D), along with the development of experiment paradigms that allow modulation of brain CYP activity without affecting CYP activity in the liver. Understanding brain CYP function, and changes therein, may provide unique strategies for the development of CNS-acting therapeutics metabolized locally in the brain, as well as therapeutics to target brain CYPs directly.

细胞色素P450（CYP）酶在大脑中的功能作用是一个令人兴奋且不断发展的研究领域。CYP存在于大脑中并在大脑中活跃，在细胞类型，区域和物种之间的表达，活性和对调制的敏感性不同。尽管全脑CYP表达只是肝脏CYP表达的一部分，但越来越多的体外和体内实验文献提供了证据，表明脑CYP可影响急性和慢性药物反应，对神经毒素损害的易感性，并与人格改变相关，行为和神经系统疾病的风险。它们也可能在内源性神经递质和神经甾体稳态中起作用。这项审查通过跨物种的大脑CYP的表征，CYP对外源诱导的易感性模式，以及近期临床CYP在体内的潜在作用的临床证据（例如CYP2D），以及允许调节CYP活性而不影响肝脏中CYP活性的实验范式的发展。了解脑CYP功能及其变化可能为开发在脑中局部代谢的中枢神经系统作用疗法以及直接靶向脑CYP的疗法提供独特的策略。