Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan; Laboratory of Molecular Pharmacology, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Japan; Addictive Substance Project, Tokyo Metropolitan Institute of Medical Science, Tokyo, Japan; Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan.
Int J Neuropsychopharmacol. 2017 Jul 1;20(7):575-584. doi: 10.1093/ijnp/pyx023.
Resolvin D1 and D2 are bioactive lipid mediators that are generated from docosahexaenoic acid. Although recent preclinical studies suggest that these compounds have antidepressant effects, their mechanisms of action remain unclear.
We investigated mechanisms underlying the antidepressant effects of resolvin D1 and resolvin D2 in lipopolysaccharide (0.8 mg/kg, i.p.)-induced depression model mice using a tail suspension test.
I.c.v. infusion of resolvin D1 (10 ng) and resolvin D2 (10 ng) produced antidepressant effects; these effects were significantly blocked by a resolvin D1 receptor antagonist WRW4 (10 µg, i.c.v.) and a resolvin D2 receptor antagonist O-1918 (10 µg, i.c.v.), respectively. The mammalian target of rapamycin complex 1 inhibitor rapamycin (10 mg/kg, i.p.) and a mitogen-activated protein kinase kinase inhibitor U0126 (5 µg, i.c.v.) significantly blocked the antidepressant effects of resolvin D1 and resolvin D2. An AMPA receptor antagonist NBQX (10 mg/kg, i.p.) and a phosphoinositide 3-kinase inhibitor LY294002 (3 µg, i.c.v.) blocked the antidepressant effects of resolvin D1 significantly, but not of resolvin D2. Bilateral infusions of resolvin D1 (0.3 ng/side) or resolvin D2 (0.3 ng/side) into the medial prefrontal cortex or dentate gyrus of the hippocampus produced antidepressant effects.
These findings demonstrate that resolvin D1 and resolvin D2 produce antidepressant effects via the mammalian target of rapamycin complex 1 signaling pathway, and that the medial prefrontal cortex and dentate gyrus are important brain regions for these antidepressant effects. These compounds and their receptors may be promising targets for the development of novel rapid-acting antidepressants, like ketamine and scopolamine.
解析素 D1 和 D2 是从二十二碳六烯酸生成的生物活性脂质介质。尽管最近的临床前研究表明这些化合物具有抗抑郁作用,但它们的作用机制尚不清楚。
我们使用悬尾试验研究了脂多糖(0.8mg/kg,腹腔注射)诱导的抑郁模型小鼠中解析素 D1 和 D2 的抗抑郁作用的机制。
脑室内输注解析素 D1(10ng)和解析素 D2(10ng)产生抗抑郁作用;这些作用分别被解析素 D1 受体拮抗剂 WRW4(10μg,脑室内)和解析素 D2 受体拮抗剂 O-1918(10μg,脑室内)显著阻断。雷帕霉素(mammalian target of rapamycin complex 1 抑制剂)(10mg/kg,腹腔注射)和丝裂原活化蛋白激酶激酶抑制剂 U0126(5μg,脑室内)显著阻断了解析素 D1 和 D2 的抗抑郁作用。AMPA 受体拮抗剂 NBQX(10mg/kg,腹腔注射)和磷脂酰肌醇 3-激酶抑制剂 LY294002(3μg,脑室内)显著阻断了解析素 D1 的抗抑郁作用,但对解析素 D2 无作用。双侧脑室内输注解析素 D1(0.3ng/侧)或解析素 D2(0.3ng/侧)到内侧前额叶皮层或海马齿状回产生抗抑郁作用。
这些发现表明,解析素 D1 和 D2 通过哺乳动物雷帕霉素靶蛋白复合物 1 信号通路产生抗抑郁作用,而内侧前额叶皮层和海马齿状回是这些抗抑郁作用的重要脑区。这些化合物及其受体可能是开发新型快速作用抗抑郁药(如氯胺酮和东莨菪碱)的有前途的靶点。