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Nelson等于1949年发现,2,2—双—[对氯苯基]—1,1—二氯乙烷(简称DDD)对狗的肾上腺皮质机能有抑制作用,引起了人们的注意。因为它给临床及实验内分泌开辟了一个新的方向,即无须手术而用药物达到干预肾上腺皮质功能的目的。一年后,Allen等又合成了对人和动物肾上腺皮质类固醇的生物合成具有明显的抑制作用的氨苯酮。但是这两种药物都因其毒性较大而未能广泛应用。此后,人们又陆续合成了许多氨苯酮的衍生物,麦托匹龙(metopirone或称为mepyrapone)(简称Su-4885)即其中之一种。其毒性小于氨苯酮,对肾上腺皮质中的皮质醇和皮质甾酮的生物合成具有强烈的抑制作用。关于Su-4885的临床及实验研究报告已有很多,借助于麦托匹龙试验已解决了许多内分泌学的理论和内分泌疾病的诊断及治疗问题。本文旨在综述麦托匹龙的实验研究以及临床应用的概况。
Nelson et al. Found in 1949 that 2,2-bis- [p-chlorophenyl] -1,1-dichloroethane (DDD) inhibits adrenal cortical function in dogs and draws attention. Because it has opened up a new direction for clinical and experimental endocrine, that is, without surgery and medication to achieve the purpose of intervention adrenocortical function. A year later, Allen et al. Synthesized aminobenzophenone, which has a significant inhibitory effect on the biosynthesis of human and animal adrenal corticosteroids. However, both drugs are not widely used due to their toxicity. Since then, many people have gradually synthesized derivatives of aminobenzene ketone, metopirone (metopirone or mepyrapone) (referred to as Su-4885) is one of them. Its toxicity is less than that of benzophenone and has a strong inhibitory effect on the biosynthesis of cortisol and corticosterone in the adrenal cortex. Su-4885 has many clinical and experimental research reports, with the help of the test of the metoprolol has solved many endocrinology and endocrine disease diagnosis and treatment problems. This article aims to summarize the experimental study of mesotrion and its clinical application.