Terran Biosciences Inc, New York, NY, USA.
Handb Exp Pharmacol. 2022;271:525-546. doi: 10.1007/164_2020_396.
The kappa opioid receptor (KOR) and its endogenous ligands dynorphins (DYN) have been implicated in the development or symptomatology of a variety of neuropsychiatric disorders. This review covers a brief history of the development of KOR agonists and antagonists, their effects in healthy volunteers, and the potential role of DYN/KOR dysfunction in schizophrenia and major depressive disorder from a translational perspective. The potential role of DYN/KOR dysfunction in schizophrenia is based on several lines of evidence. Selective KOR agonists induce affective states in healthy volunteers with similarities to the symptoms of schizophrenia. Studies have shown increased DYN in patients with schizophrenia, although the data have been mixed. Finally, meta-analytic data have shown that opioid antagonists are associated with reductions in the symptoms of schizophrenia. The potential role of DYN/KOR dysfunction in major depressive disorder is also based on a combination of preclinical and clinical data. Selective KOR agonists have shown pro-depressive effects in human volunteers, while selective KOR antagonists have shown robust efficacy in several preclinical models of antidepressant activity. Small studies have shown that nonselective KOR antagonists may have efficacy in treatment-resistant depression. Additionally, recent clinical data have shown that the KOR may be an effective target for treating anhedonia, a finding relevant to both schizophrenia and depression. Finally, recommendations are provided for translating preclinical models for schizophrenia and major depressive disorder into the clinic.
κ 阿片受体(KOR)及其内源性配体强啡肽(DYN)与多种神经精神疾病的发生或症状有关。本综述从转化的角度简要回顾了 KOR 激动剂和拮抗剂的发展、它们在健康志愿者中的作用,以及 DYN/KOR 功能障碍在精神分裂症和重度抑郁症中的潜在作用。DYN/KOR 功能障碍在精神分裂症中的潜在作用基于以下几方面的证据。选择性 KOR 激动剂在健康志愿者中引起与精神分裂症症状相似的情感状态。研究表明,精神分裂症患者的 DYN 增加,尽管数据不一。最后,荟萃分析数据表明,阿片类拮抗剂与精神分裂症症状的减轻有关。DYN/KOR 功能障碍在重度抑郁症中的潜在作用也基于临床前和临床数据的综合。选择性 KOR 激动剂在人类志愿者中表现出促抑郁作用,而选择性 KOR 拮抗剂在几种抗抑郁活性的临床前模型中显示出强大的疗效。小型研究表明,非选择性 KOR 拮抗剂可能对治疗难治性抑郁症有效。此外,最近的临床数据表明,KOR 可能是治疗快感缺失的有效靶点,这与精神分裂症和抑郁症都有关。最后,为将精神分裂症和重度抑郁症的临床前模型转化为临床治疗提供了建议。