Stein Gregor, Aly Janine S, Lange Lisa, Manzolillo Annamaria, Riege Konstantin, Brancato Anna, Hübner Christian A, Turecki Gustavo, Hoffmann Steve, Engmann Olivia
Institute for Biochemistry and Biophysics, Friedrich-Schiller-University Jena, Jena, Germany.
Institute of Human Genetics, Jena University Hospital, Am Klinikum 1, F2E20, 07747, Jena, Germany.
Mol Psychiatry. 2025 May;30(5):1828-1835. doi: 10.1038/s41380-024-02790-4. Epub 2024 Oct 21.
Chronic stress is a major risk factor for depression, a leading cause of disability and suicide. Because current antidepressants work slowly, have common side effects, and are only effective in a minority of patients, there is an unmet need to identify the underlying molecular mechanisms. Here, we identify the receptor for neuropeptides B and W, Npbwr1, as a key regulator of depressive-like symptoms. Npbwr1 is increased in the nucleus accumbens of chronically stressed mice and postmortem in patients diagnosed with depression. Using viral-mediated gene transfer, we demonstrate a causal link between Npbwr1, dendritic spine morphology, the biomarker Bdnf, and depressive-like behaviors. Importantly, microinjection of the synthetic antagonist of Npbwr1, CYM50769, rapidly ameliorates depressive-like behavioral symptoms and alters Bdnf levels. CYM50769 is selective, well tolerated, and shows effects up to 7 days after administration of a single dose. In summary, these findings advance our understanding of mood and chronic stress and warrant further investigation of CYM50769 as a potential fast-acting antidepressant.
慢性应激是抑郁症的主要风险因素,抑郁症是导致残疾和自杀的主要原因。由于目前的抗抑郁药起效缓慢、有常见副作用且仅对少数患者有效,因此识别其潜在分子机制的需求尚未得到满足。在此,我们确定神经肽B和W的受体Npbwr1是抑郁样症状的关键调节因子。在慢性应激小鼠的伏隔核中以及被诊断为抑郁症患者的尸检样本中,Npbwr1均有所增加。通过病毒介导的基因转移,我们证明了Npbwr1、树突棘形态、生物标志物脑源性神经营养因子(Bdnf)与抑郁样行为之间存在因果联系。重要的是,微量注射Npbwr1的合成拮抗剂CYM50769可迅速改善抑郁样行为症状并改变Bdnf水平。CYM50769具有选择性,耐受性良好,且单次给药后7天内均有效果。总之,这些发现增进了我们对情绪和慢性应激的理解,并为进一步研究CYM50769作为一种潜在的速效抗抑郁药提供了依据。