体内微透析评价Sigma1受体激动剂SA-4503对清醒大鼠前额皮质单胺水平的影响

F. Crespi
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引用次数: 0

摘要

Sigma受体广泛存在于中枢神经系统,分为sigma1和sigma2两种亚型。特别是,sigma1受体亚型似乎能够影响与神经变性相关的生物学机制。此外,一些研究暗示sigma1受体激动剂与抗抑郁活性有关。临床抑郁症患者前额皮质异常的证据已被一些研究报道,单胺类如5 -羟色胺和儿茶酚胺可能与这种异常有关。到目前为止,大多数分析sigma1受体激动剂对脑区儿茶酚胺能和血清素能活性影响的临床前工作都是通过体外和离体方法完成的。在这里,SA-4503,一种具有潜在抗抑郁活性的选择性sigma1受体激动剂,通过微透析检测自由运动大鼠内侧前额叶皮层(mPFC)的多巴胺(DA)、去甲肾上腺素(NA)和血清素(5-HT)水平,在体内进行了测试。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Microdialysis in vivo Evaluation of the effects of SA-4503, a Sigma1 Receptor Agonist, on the Levels of Monoamines in the Prefrontal Cortex of Conscious Rats
Sigma receptors are widespread in the central nervous system and are differentiated in two subtypes, sigma1 and sigma2. In particular, the sigma1 receptor subtype appears to be able to influence biological mechanisms connected with neuro-degeneration. Furthermore, several studies are implicating sigma1 receptor agonists within antidepressant activity. Evidence of prefrontal cortex abnormalities in clinically depressed subjects have been reported by several works and that monoamines such as serotonin and cathecolamines can be involved in such malfunctions. Up to now the most of the preclinical work performed to analyze the influence of sigma1 receptor agonists upon catecholaminergic and serotoninergic activities in brain areas has been done by means of in vitro as well as ex vivo methodologies. Here, SA-4503, a selective sigma1 receptor agonist with potential antidepressant activity has been tested in vivo upon dopamine (DA), noradrenaline (NA) and serotonin (5-HT) levels detected by micro-dialysis in the medial Prefrontal Cortex (mPFC) of freely moving rats.
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