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(+)SKF 10,047,一种 sigma-1 受体激动剂,对焦虑的影响,在两种小鼠实验室模型中进行测试。

Effects of (+) SKF 10,047, a sigma-1 receptor agonist, on anxiety,tested in two laboratory models in mice.

机构信息

Universidad de Málaga.

出版信息

Psicothema. 2012;24(3):427-30.

PMID:22748735
Abstract

Recently, sigma-1 receptor modulators have been considered drugs with an interesting therapeutic potential for the treatment of anxiety. However, there is no clear information in preclinical studies about the possible effects of sigma-1 ligands on anxiety in experimental animal models. Therefore, the present study examined the effects of (+)SKF 10,047 (2-8 mg/kg, ip), a sigma-1 agonist, on anxiety, tested in two classical laboratory models (social interaction test and elevated plus maze). (+)SKF 10,047 (8 mg/kg) produced a significant decrease of social investigation in the "social interaction test", whereas in the "elevated plus maze", the drug (4 and 8 mg/kg) provoked a significant reduction in the number of entries into open arms, as well as in the time spent in this area, as compared with the control group, without affecting motor activity. Overall, these findings indicate that (+)SKF 10,047 exhibits an anxiogenic-like profile in mice. It is suggested that anxiogenic effects of this sigma-1 ligand could be related to its potent ability to modulate diverse neurotransmitter systems involved in anxiety regulation.

摘要

最近,西格玛-1 受体调节剂已被认为是具有治疗焦虑症潜力的药物。然而,在临床前研究中,关于西格玛-1 配体在实验动物模型中对焦虑的可能影响,尚无明确信息。因此,本研究在两个经典的实验室模型(社交互动测试和高架十字迷宫测试)中,检测了西格玛-1 激动剂 (+)SKF 10,047(2-8mg/kg,ip)对焦虑的影响。(+)SKF 10,047(8mg/kg)在“社交互动测试”中显著降低了社交探索,而在“高架十字迷宫”中,与对照组相比,药物(4 和 8mg/kg)显著减少了进入开放臂的次数,以及在该区域的时间,而不影响运动活动。总体而言,这些发现表明 (+)SKF 10,047 在小鼠中表现出类焦虑样特征。据推测,这种西格玛-1 配体的焦虑作用可能与其调节焦虑的多种神经递质系统的强大能力有关。

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