Gillman M A, Lichtigfeld F J
South African Brain Research Institute, Waverely, Johannesburg, South Africa.
Int J Neurosci. 1994 May;76(1-2):5-12. doi: 10.3109/00207459408985986.
We show that psychotropic analgesic nitrous oxide is a partial opioid agonist since it fulfills all the following criteria to be classified as an opioid: 1) its effects are antagonised by various opioid antagonists including stereospecific naloxone antagonism; 2) it is cross tolerant with morphine; 3) its effects are potentiated by enkephalinase inhibition; 4) it provokes the release of endogenous opioids; 5) it interferes at low concentrations with specific opioid ligand binding at radio-receptor assay. Like the prototype opioid morphine it acts directly and indirectly at opioid receptors. PAN, although considered an exogenous inorganic molecule was also the first gas to be shown to have a direct role in influencing neurotransmission. We also describe some of the relationships that exist between nitrous oxide and its close relative, the endogenous gas nitric oxide. We describe the use of PAN as a safe, effective tool for investigating and treating the endogenous opioid system in man.
我们表明，精神类镇痛剂一氧化二氮是一种部分阿片样物质激动剂，因为它满足以下所有被归类为阿片样物质的标准：1）其作用可被各种阿片样物质拮抗剂拮抗，包括立体特异性纳洛酮拮抗作用；2）它与吗啡有交叉耐受性；3）其作用可因脑啡肽酶抑制而增强；4）它能促使内源性阿片样物质释放；5）在低浓度下，它会干扰放射性受体测定中特异性阿片样物质配体的结合。与原型阿片样物质吗啡一样，它直接和间接作用于阿片样物质受体。尽管PAN被认为是一种外源性无机分子，但它也是第一种被证明在影响神经传递方面具有直接作用的气体。我们还描述了一氧化二氮与其近亲内源性气体一氧化氮之间存在的一些关系。我们描述了将PAN用作研究和治疗人类内源性阿片样物质系统的安全、有效工具。
