Laboratory of Synthesis, Reactivity and Pharmacological and Toxicological Evaluation of Organochalcogens, Center of Natural and Exact Sciences, Federal University of Santa Maria, Santa Maria CEP 97105-900, RS, Brazil.
Department of Neurosciences, Psychology, Drug Research and Child Health, Section of Pharmacology and Toxicology, University of Florence, Viale G. Pieraccini 6, I-50139 Florence, Italy.
Eur J Pharmacol. 2014 Aug 5;736:44-54. doi: 10.1016/j.ejphar.2014.04.033. Epub 2014 May 4.
We investigated the antidepressant-like action of 5 compounds belonging to the selenophene class. The involvement of ERK and CREB activation in this action was also demonstrated. In the experiment 1, time-course and dose-response effect of H-DPS, CH3-DPS, Cl-DPS, F-DPS and CF3-DPS were accompanied in the mouse forced swimming test (FST). Firstly, animals received compounds at a dose of 50mg/kg, by intragastric (i.g.) route, at different times (15-240 min) before test. Results showed that the peak of maximum anti-despair behavior induced by Cl-DPS, F-DPS and CF3-DPS was at 30 min; maximum effect of H-DPS and CH3-DPS was found at 60 min, which was maintained until 120 min. Regarding dose-response effect, all compounds reduced immobility time and increased latency for the first episode of immobility at a dose of 50mg/kg. In addition, F-DPS also showed antidepressant-like action at a dose of 25mg/kg, whilst H-DPS, CH3-DPS, Cl-DPS and CF3-DPS were not effective at lower doses. Thus, F-DPS was chosen for further investigation of its mechanism of action. Experiment 2 showed that treatment of animals with F-DPS (50 mg/kg, i.g.) significantly increased phosphorylated ERK1/2 levels in the prefrontal cortex and hippocampus; however, pCREB levels were not affected. Additionally, in the experiment 3 anti-immobility effect of F-DPS was completely blocked by pretreatment of animals with PD 98,059, an inhibitor of ERK phosphorylation, suggesting that ERK signalling activation is involved in its antidepressant-like action in mice. Together our data appoint F-DPS as a promising molecule for the development of a new antidepressant therapy.
我们研究了 5 种属于噻吩类的化合物的抗抑郁作用。还证明了 ERK 和 CREB 激活在此作用中的参与。在实验 1 中,在小鼠强迫游泳试验(FST)中伴随了 H-DPS、CH3-DPS、Cl-DPS、F-DPS 和 CF3-DPS 的时间过程和剂量反应效应。首先,动物以 50mg/kg 的剂量通过灌胃(i.g.)途径在测试前的不同时间(15-240 分钟)接受化合物。结果表明,Cl-DPS、F-DPS 和 CF3-DPS 诱导的最大抗抑郁作用的峰值出现在 30 分钟;H-DPS 和 CH3-DPS 的最大作用出现在 60 分钟,直到 120 分钟保持不变。关于剂量反应效应,所有化合物均降低了不动时间并增加了首次不动时间的潜伏期,剂量为 50mg/kg。此外,F-DPS 还以 25mg/kg 的剂量表现出抗抑郁作用,而 H-DPS、CH3-DPS、Cl-DPS 和 CF3-DPS 在较低剂量下无效。因此,选择 F-DPS 进一步研究其作用机制。实验 2 表明,用 F-DPS(50mg/kg,i.g.)治疗动物显着增加了前额叶皮层和海马体中磷酸化 ERK1/2 的水平;然而,pCREB 水平不受影响。此外,在实验 3 中,F-DPS 的抗不动作用被 PD 98,059 预处理的动物完全阻断,PD 98,059 是 ERK 磷酸化的抑制剂,这表明 ERK 信号转导激活参与了其在小鼠中的抗抑郁作用。我们的数据共同表明,F-DPS 是开发新的抗抑郁治疗方法的有前途的分子。