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改变吗啡骨架合成麻醉性镇痛药的报道已很多,就其结构活性研究成果发现,具天然吗啡相同的R~((-))这一立体特异性,确认了它们有强力的镇痛活性.麻醉性镇痛药设想有特异结合能的阿片受体,1973年已被实验证实脑内存在。但其分布不均一,在调节痛觉深部的脊髓后角,兰斑核,三叉神经下行核的罗氏胶质区、中脑导水管周围灰质等高密度地存在阿片受体。有关阿片受体的内在性活性物质,已从一组含多肽哺乳动物的脑、下垂体分离出两种脑啡肽(蛋-脑啡肽和亮-脑啡肽)及β-内啡肽的单体.从类阿片肽的发现推测可能存在调节内在性疼痛的机能,为阐明其生理作用,佐藤应用电生理学实验,从外部给予类阿片肽,就镇痛作用进行
There are a lot of reports about the morphological changes of morphine analgesics. Based on the results of their structural activity studies, we found that the stereospecificity of the same R ~ ((-)) of natural morphine confirms their potent analgesic activity. Narcotic analgesics envisage opioid receptors with specific binding energy that have been experimentally demonstrated in the brain in 1973. But its distribution is not uniform, in the regulation of deep pain of spinal dorsal horn, blue plaque nucleus, the trigeminal nucleus of the Roche glial area, midbrain pericardium and other high-density peripheral opioid receptors. For the intrinsic activity of opioid receptors, two enkephalin (egg-enkephalin and leu-enkephalin) and beta-endorphin have been isolated from the brain and pituitary gland of mammalian-containing peptides Monomers. From the discovery of opioid peptides, there may be the function of regulating intrinsic pain. To elucidate its physiological role, Sato applied electrophysiological experiments to administer opioid peptides from the outside to make analgesic effects