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Potent Morphine-Like Analgesics Derived from Thebaine. The Preparation of 6,14-endo-Etheno- and 6,14-endo-Ethano tetrahydrooripavines

机译：从蒂巴因衍生的强效吗啡样镇痛药。 6,14-内 - 乙烯 - 和6,14-内 - 乙醇四氢罂粟碱的制备

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摘要

Chemical modifications of the biologically inactive opium alkaloid thebaine can produce oripavine-type analgesics with potencies very much greater than that of morphine. However, purity is a critical factor affecting the results of analgesic screening in the series, and an improved method and solvent system has been developed to prepare compounds of a quality suitable for bioevaluation. Reduction of the endo double bond in the intrinsically less active etheno series effects a significant nonlinear increase in analgetic potency in the series studied. A literature review indicates that the oripavine analgesics are extremely effective in relieving refractory pain in man and in humane immobilization of animals.

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Hydro, W. R.;
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年度 1981
页码 p.1-38
总页数 38
原文格式 PDF
正文语种 eng
中图分类工业技术;
关键词
Synthesis(Chemistry); Analgesics; Thebaine; Oripavine; Pharmacological antagonists; Opium alkaloids; Laboratory animals; Nerve agents; Purification; Molecular structure; Sulfur compounds; Recrystallization; Rats; Pain; Chemical analysis; Chemical derivatives;

机译：合成（化学）;镇痛药;蒂巴因; Oripavine;药理拮抗剂;鸦片生物碱;实验动物;神经毒剂;纯化;分子结构;硫化合物;重结晶;大鼠;疼痛;化学分析;化学衍生物;

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1. Rationally designed benzopyran fused isoxazolidines and derived beta(2,3,3)-amino alcohols as potent analgesics: Synthesis, biological evaluation and molecular docking analysis [J] . Singh Gagandeep, Singh Gurjit, Bhatti Rajbir, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2017,第期

机译：理性设计的苯并吡喃融合的异恶唑啉和衍生的β（2,3,3） - 氨基醇作为有效的镇痛药：合成，生物学评价和分子对接分析
2. Discovery of highly potent analgesic activity of isopulegol-derived (2R,4aR,7R,8aR)-4,7-dimethyl-2-(thiophen-2-yl)octahydro-2H-chromen-4-ol [J] . Nazimova Ekaterina, Pavlova Alla, Mikhalchenko Oksana, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2016,第7期

机译：发现异豆蔻醇衍生的（2R，4aR，7R，8aR）-4,7-二甲基-2-（噻吩-2-基）八氢-2H-铬-4-醇的强效镇痛活性
3. Highly potent analgesic activity of monoterpene-derived(2594aR,8R,8aR)-2-aryl-4,7-dimethyl-3,4,4a,5,8,8a-hexahydro-2H-chromene-4,8-diols [J] . Irina Ilina, Oksana Mikhalchenko, Alia Pavlova Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2014,第12期

机译：单萜衍生的（2594aR，8R，8aR）-2-芳基-4,7-二甲基-3,4,4a，5,8,8a-六氢-2H-色烯-4,8-二醇的高效止痛活性
4. Effects of Methyl and Halogens in Analgesic Peptide Molecules for Their Potent Agonist Activities at MOR/DOR and Antagonist Activity at NK1R [C] . Aswini Kumar Giri, C.R. Apostol, P. Davis American Peptide Symposium . 2015

机译：镇痛肽分子在镇痛肽分子中甲基和卤素的影响Mor / Dor和NK1R拮抗剂活性的活性激动剂活性
5. Glycopeptide enkephalin analogs: Design, synthesis, biophysical and pharmacological evaluation of potent analgesics with reduced side-effects. [D] . Palian, Michael M. 2002

机译：糖肽脑啡肽类似物：有效的止痛药的设计，合成，生物物理和药理学评估，具有减少的副作用。
6. Comparison of effect of morphine-like analgesics on transmurally stimulated guinea-pig ileum [O] . M. R. Fennessy, R. L. H. Heimans, M. J. Rand 1969

机译：类吗啡镇痛药对经皮刺激豚鼠回肠的作用比较
7. The Use of the Morphine-Like Analgesic Carfentanyl in Captive Wild Mammals at Tierpark Hellabrunn [O] . Wiesner Henning, Rietschel W., Gatesman T. 1984

机译：在Tierpark Hellabrunn的圈养野生哺乳动物中使用吗啡样镇痛性卡芬太尼

Potent Morphine-Like Analgesics Derived from Thebaine. The Preparation of 6,14-endo-Etheno- and 6,14-endo-Ethano tetrahydrooripavines

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