摘要
Salvinorin A(SA)是一种选择性kappa阿片受体激动剂,能通过作用于阿片受体系统产生多种药理效应。其在体内的代谢迅速,不易成瘾。其主要的药理作用包括产生分离效应、调节多巴胺系统等。最新研究表明:SA在动物神经系统中对脑血管和神经元都起到一定作用,其作用机制包括:MAPK/ERK通路作用下恢复脑血管的自身调节;通过NOS和KATP通道的调节扩张血管;通过MAPK/ERK通路和VEGF保护神经元;抑制AQP-4的表达以减轻脑水肿。SA作用于中枢能调节情绪,针对抑郁和焦虑有一定的作用,而作用于外周则能抑制胃肠道炎症,调节胃肠道的运动和离子转运。SA在高浓度下则具有一定的细胞毒性。由于SA具有较为广泛的药理作用,期望研究能为其临床应用提供更丰富的理论基础。
Salvinorin A is a selective kappa opioid receptor agonist that exerts various pharmacological effects via opioid receptor system. It can be metabolized rapidly in vivo, hardly leading to addiction of subjects. The major pharmaceutical effects of SA include dissociative effects and regulations of dopamine system. A number of researches have confirmed the positive effects of Salvinorin A in the animal nervous system and the mechanisms are as follows. Salvinorin A preserves cerebrovascular autoregulation via MAPK/ERK pathway and dilates arteries through NOS and KATP channels; neurons are protected via MAPK/ERK pathway and the expression of VEGF; it reduces the brain edema via the inhibition of AQP-4. The central effect of Salvinorin A reflects in its role in regulating the emotion especially depression and anxiety. When acting on periphery, Salvinorin A regulates the motility and ion transportation of gastro-intestine tract, with its additional anti-inflammatory effects. In a high level of concentration, SA can exert a cytotoxic effect. For the reason that SA owns a wide range of pharmaceutical effects, current studies can provide more fundamental theories for its clinical application in the future.
出处
《解剖科学进展》
2017年第5期532-537,共6页
Progress of Anatomical Sciences
基金
国家自然科学基金(81471186)
