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mGlu2/3 受体拮抗剂 TP0178894 在慢性社会挫败应激模型中的抗抑郁作用:与艾司西酞普兰的比较。

Antidepressant-like actions of the mGlu2/3 receptor antagonist TP0178894 in the chronic social defeat stress model: Comparison with escitalopram.

机构信息

Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba 260-8670, Japan.

Taisho Pharmaceutical Co., Ltd., Saitama, 331-9530, Japan.

出版信息

Pharmacol Biochem Behav. 2022 Jan;212:173316. doi: 10.1016/j.pbb.2021.173316. Epub 2021 Dec 27.

Abstract

The metabotropic glutamate 2/3 (mGlu2/3) receptor antagonists are reported to produce ketamine-like rapid-acting and sustained antidepressant-like effects in rodents. In this study, we compared the effects of single administration of the new mGlu2/3 receptor antagonist TP0178894 and the selective serotonin reuptake inhibitor (SSRI) escitalopram in the chronic social defeat stress (CSDS) model of depression, a model which has been shown to be resistant to treatment with a single dose of SSRI. In the tail suspension test and forced swimming test, high dose (3.0 mg/kg) of TP0178894 significantly attenuated the increased immobility time of these tests in CSDS susceptible mice, compared with vehicle-treated mice. In contrast, low doses (0.3 and 1.0 mg/kg) of TP0178894 and escitalopram (10 mg/kg) did not alter the increased immobility time of these two tests. In the sucrose preference test, TP0178894 (3.0 mg/kg) significantly improved the reduced sucrose preference of CSDS susceptible mice, three and seven days after a single dose. In addition, Western blot analyses showed that TP0178894 (3.0 mg/kg), but not low doses of TP0178894 and escitalopram, significantly attenuated the reduced expression of synaptic proteins [α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (GluA1) and postsynaptic density protein 95 (PSD-95)] in the prefrontal cortex from CSDS susceptible mice. This study suggests that TP0178894 shows rapid-acting and sustained antidepressant-like effects in CSDS model, as ketamine does.

摘要

代谢型谷氨酸 2/3(mGlu2/3)受体拮抗剂据报道可在啮齿动物中产生类似于氯胺酮的快速起效和持续的抗抑郁样作用。在这项研究中,我们比较了新型 mGlu2/3 受体拮抗剂 TP0178894 和选择性 5-羟色胺再摄取抑制剂(SSRI)依地普仑单次给药在慢性社交挫败应激(CSDS)抑郁模型中的作用,该模型已被证明对 SSRI 的单次剂量治疗具有抗性。在悬尾试验和强迫游泳试验中,高剂量(3.0 mg/kg)的 TP0178894 显著减轻了 CSDS 易感小鼠这些试验中不动时间的增加,与载体处理的小鼠相比。相比之下,低剂量(0.3 和 1.0 mg/kg)的 TP0178894 和依地普仑(10 mg/kg)并未改变这两种试验中不动时间的增加。在蔗糖偏好试验中,TP0178894(3.0 mg/kg)在单次给药后三天和七天显著改善了 CSDS 易感小鼠的蔗糖偏好降低。此外,Western blot 分析表明,TP0178894(3.0 mg/kg),而不是低剂量的 TP0178894 和依地普仑,显著减轻了 CSDS 易感小鼠前额叶皮质中突触蛋白[α-氨基-3-羟基-5-甲基-4-异恶唑丙酸受体(GluA1)和突触后密度蛋白 95(PSD-95)]表达的降低。这项研究表明,TP0178894 像氯胺酮一样,在 CSDS 模型中表现出快速起效和持续的抗抑郁样作用。

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