Wang G D, Zhao Z Q, Li C Q
Shanghai Brian Research Institute, Chinese Academy of Sciences.
Sheng Li Ke Xue Jin Zhan. 1997 Oct;28(4):311-6.
With the development of cDNA cloning technique in molecular biology, the research of opioids and opioid receptor as well as the mechanism of peripheral analgesia have made a great progress in the fields of receptor researches including molecular structure, morphology, molecular pharmacology, ion channel and intercellular signal transduction systems. The functional properties of mu, delta and kappa opioid receptor were determined by their structures. Depending on different proportional distribution in the primary sensory neurons, opioid receptor activation increases or decreases the potassium current and inhibits the calcium channel. There are different second message systems which are involved in the signal transduction between opioid receptors and ion channels. In addition, pharmacological evidence has also proved the existence of sub-types of opioid receptor, and the activation of these receptors can inhibit transmitters release from primary sensory neuron directly, which may be an important mechanism that opioid receptor has an analgesic effect in the peripheral nervous system.
随着分子生物学中cDNA克隆技术的发展,在受体研究领域,包括分子结构、形态学、分子药理学、离子通道和细胞间信号转导系统等方面,阿片类物质、阿片受体以及外周镇痛机制的研究取得了巨大进展。μ、δ和κ阿片受体的功能特性由其结构决定。根据在初级感觉神经元中的不同比例分布,阿片受体激活可增加或减少钾电流并抑制钙通道。在阿片受体与离子通道之间的信号转导中涉及不同的第二信使系统。此外,药理学证据也证实了阿片受体亚型的存在,这些受体的激活可直接抑制初级感觉神经元释放递质,这可能是阿片受体在外周神经系统中发挥镇痛作用的重要机制。