摘要
阿片(opioids)及阿片受体与外周神经系统镇痛机制的研究,随着分子生物学技术的发展,已在受体的分子结构、形态学、分子药理学、离子通道和细胞内信号转导系统等方面取得了显著进展。μ、δ、κ阿片受体分子结构上的部分差异决定了它们各自的功能特征。三种受体在初级感觉神经元分布的比例不同,但都能介导细胞Ca2+通道的抑制和K+电流增加及减少。阿片受体和通道之间由多种第二信使系统偶联。分子药理学研究表明它们还存在亚型受体。阿片受体的激活直接和间接地抑制初级感觉神经元的递质释放,可能是阿片受体在外周神经系统中发挥镇痛效应的重要机制。
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 μ, δ and κ 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.
出处
《生理科学进展》
CAS
CSCD
北大核心
1997年第4期311-316,共6页
Progress in Physiological Sciences