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β3肾上腺素能受体激动剂SR58611A的行为效应:它是一类新型抗抑郁/抗焦虑药物的推定原型吗?

Behavioral effects of the beta3 adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs?

作者信息

Consoli Daniele, Leggio Gian Marco, Mazzola Carmen, Micale Vincenzo, Drago Filippo

机构信息

Department of Experimental and Clinical Pharmacology, Faculty of Medicine, University of Catania, Italy.

出版信息

Eur J Pharmacol. 2007 Nov 14;573(1-3):139-47. doi: 10.1016/j.ejphar.2007.06.048. Epub 2007 Jul 4.

Abstract

A large body of evidence corroborates the notion that deficiencies of serotonergic system are likely involved in the pathogenesis of both depression and anxiety. Activation of beta(3) adrenoceptors has been shown to increase brain tryptophan content suggesting an elevation of brain serotonin (5HT) synthesis. SR58611A is a selective beta(3) adrenergic agent possessing a profile of antidepressant activity in routine rodents' experimental models of depression. The present study was undertaken to evaluate in rodents the antidepressant properties of SR58611A and to assess its putative anxiolytic value in experimental models of depression and anxiety. Compared to the control group, SR58611A (0.1, 1, 5 or 10 mg/kg) caused a dose-dependent reduction in immobility of Wistar male rats in the forced swim test. The maximum dose appeared to be equivalent to an effective dose of clomipramine (50 mg/kg). In addition, acute injection of SR58611A induced in rats a dose-dependent decrease in grooming response to a novel environment (novelty-induced grooming test). For any dose, the effect was lower than that of diazepam (1 mg/kg). Chronic treatment with SR58611A resulted also in an increased social interaction time in the social interaction test without affecting motor activity of rats. Furthermore, similarly to diazepam a chronic treatment with the highest doses of SR58611A was followed by increased exploratory behavior in Swiss male mice exposed to the elevated plus maze test. These effects are mediated by beta(3) adrenoceptors since i.p. pretreatment with the selective beta(3) adrenoceptor antagonist SR59230A (5 mg/kg) blocked the effects of SR58611A. Finally, also the 5HT antagonist methysergide (2 mg/kg) prevented the antidepressant and anxiolytic-like activity of SR58611A indicating that 5HT transmission is strictly involved in its action.

摘要

大量证据证实了血清素能系统缺陷可能参与抑郁症和焦虑症发病机制这一观点。已表明β(3)肾上腺素能受体的激活会增加脑内色氨酸含量,提示脑内血清素(5-羟色胺,5HT)合成增加。SR58611A是一种选择性β(3)肾上腺素能药物,在常规啮齿动物抑郁症实验模型中具有抗抑郁活性。本研究旨在评估SR58611A在啮齿动物中的抗抑郁特性,并在抑郁症和焦虑症实验模型中评估其假定的抗焦虑价值。与对照组相比,SR58611A(0.1、1、5或10mg/kg)在强迫游泳试验中使Wistar雄性大鼠的不动时间呈剂量依赖性减少。最大剂量似乎相当于氯米帕明(50mg/kg)的有效剂量。此外,急性注射SR58611A可使大鼠对新环境的理毛反应(新奇诱导理毛试验)呈剂量依赖性降低。对于任何剂量,该效应均低于地西泮(1mg/kg)的效应。SR58611A的慢性治疗还导致社交互动试验中的社交互动时间增加,而不影响大鼠的运动活动。此外,与地西泮类似,用最高剂量的SR58611A进行慢性治疗后,暴露于高架十字迷宫试验的瑞士雄性小鼠的探索行为增加。这些效应是由β(3)肾上腺素能受体介导的,因为腹腔注射选择性β(3)肾上腺素能受体拮抗剂SR59230A(5mg/kg)可阻断SR58611A的效应。最后,5HT拮抗剂甲基麦角新碱(2mg/kg)也可阻止SR58611A的抗抑郁和抗焦虑样活性,表明5HT传递严格参与其作用。

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