Grossman A, Sutton J R
Med Sci Sports Exerc. 1985 Feb;17(1):74-81.
A generalized knowledge of opiates has been available for centuries, but it was not until 1975, following the isolation of the first endogenous opioids, that it was appreciated that their analgesic properties were mediated via specific receptors. Three general classes of opioids are now recognized: the endorphins, the enkephalins, and the dynorphins. Assaying of the endogenous opioid peptides has never been simple, and now radioimmunoassay has replaced the earlier bioassays. When coupled with immunohistochemical techniques, radioimmunoassay allows precise localization of opioids in various tissue sections. There is evidence that plasma concentration of endorphins, and possibly also met-enkephalin, increases with exercise. In addition, the opioid peptides have important implications for the effects of other hormonal functions, including the pituitary hormones and catecholamines. Few studies during exercise are available, and naloxone has been used widely as the agent to determine the role of endogenous opioids on hormonal secretions. Slightly conflicting results have been obtained, depending on the dosage of naloxone used. With high-dose naloxone, there appears to be overall endorphin inhibition of cortisol, prolactin, and growth hormone secretion. Endorphins do not appear to exert a major influence on the cardiovascular response to exercise, but in high-intensity exercise, they appear to partially inhibit the ventilatory response to exercise.
几个世纪以来,人们对阿片类药物已有普遍了解,但直到1975年,随着第一种内源性阿片类物质的分离,人们才认识到它们的镇痛特性是通过特定受体介导的。现在已确认有三大类阿片类药物:内啡肽、脑啡肽和强啡肽。对内源性阿片肽的测定从来都不简单,现在放射免疫测定法已取代了早期的生物测定法。当与免疫组织化学技术结合使用时,放射免疫测定法可精确定位阿片类药物在各种组织切片中的位置。有证据表明,内啡肽以及可能还有甲硫氨酸脑啡肽的血浆浓度会随着运动而增加。此外,阿片肽对包括垂体激素和儿茶酚胺在内的其他激素功能的影响具有重要意义。运动期间的相关研究较少,纳洛酮已被广泛用作确定内源性阿片类药物对激素分泌作用的药物。根据所用纳洛酮的剂量,已获得了略有矛盾的结果。使用高剂量纳洛酮时,内啡肽似乎会总体抑制皮质醇、催乳素和生长激素的分泌。内啡肽似乎对运动时的心血管反应没有重大影响,但在高强度运动中,它们似乎会部分抑制运动时的通气反应。