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导致十二指肠溃疡和肾上腺皮质坏死的烷基亲核化学物质之间的构效关系。

Structure-activity relations between alkyl nucleophilic chemicals causing duodenal ulcer and adrenocortical necrosis.

作者信息

Szabo S, Reynolds E S, Unger S H

出版信息

J Pharmacol Exp Ther. 1982 Oct;223(1):68-76.

PMID:7120129
Abstract

Structure-activity relationships were qualitatively and quantitatively examined for 56 chemicals (e.g., derivatives of propionitrile, acrylonitrile and cysteamine) which caused duodenal ulcer and/or adrenocortical necrosis in rats. For the first time the duodenal ulcerogenic property of numerous chemicals has been studied in a rational and predictive manner. Ulcerogenic activity was most intense in the carbonitriles attached to two or three carbon backbones and diminished by shortening, lengthening, branching, unsaturating, halogenating or hydroxylating the carbon chains. Different modes of action are implied. Adrenocorticolytic potency was associated with unsaturation of the carbon chain and substitution of the nitrile by thiol or amine radicals. An action of these chemicals on the central nervous system has been suggested.

摘要

对56种能在大鼠中引发十二指肠溃疡和/或肾上腺皮质坏死的化学物质(如丙腈、丙烯腈和半胱胺的衍生物)进行了结构-活性关系的定性和定量研究。众多化学物质的十二指肠溃疡ogenic特性首次以合理且可预测的方式得到研究。溃疡ogenic活性在连接到两个或三个碳骨架的碳腈中最为强烈,并通过缩短、延长、分支、不饱和化、卤化或羟基化碳链而减弱。这暗示了不同的作用模式。肾上腺皮质溶解效力与碳链的不饱和性以及腈基被硫醇或胺基取代有关。已有人提出这些化学物质对中枢神经系统有作用。

相似文献

1
Structure-activity relations between alkyl nucleophilic chemicals causing duodenal ulcer and adrenocortical necrosis.导致十二指肠溃疡和肾上腺皮质坏死的烷基亲核化学物质之间的构效关系。
J Pharmacol Exp Ther. 1982 Oct;223(1):68-76.
2
Structure-activity relationships for ulcerogenic and adrenocorticolytic effects of alkyl nitriles, amines, and thiols.烷基腈、胺和硫醇的致溃疡作用及肾上腺皮质溶解作用的构效关系。
Environ Health Perspect. 1975 Jun;11:135-40. doi: 10.1289/ehp.7511135.
3
Somatostatin depletion by cysteamine: mechanism and implication for duodenal ulceration.半胱胺导致生长抑素耗竭:机制及其与十二指肠溃疡形成的关联
Fed Proc. 1985 Jun;44(9):2540-5.
4
Somatostatin depleting potency of cysteamine-related thiols and amines in the rat: structure-activity relation.
J Pharmacol Exp Ther. 1992 Nov;263(2):752-6.
5
Stereomicroscopic and ultrastructural characterization of propionitrile-induced duodenal ulcer in the rat.
Lab Invest. 1978 Jan;38(1):1-7.
6
[Interrelation between the analgesic and ulcerogenic action of cysteamine].[半胱胺的镇痛作用与致溃疡作用之间的相互关系]
Biull Eksp Biol Med. 1984 Nov;98(11):582-3.
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Potentiation of duodenal ulcerogenic action of acrylonitrile by PCB or phenobarbital in the rat.多氯联苯或苯巴比妥对大鼠丙烯腈致十二指肠溃疡作用的增强效应
Toxicol Appl Pharmacol. 1983 Dec;71(3):451-4. doi: 10.1016/0041-008x(83)90034-0.
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Adrenal gland: chemically induced structural and functional changes in the cortex.肾上腺:化学诱导的皮质结构和功能变化。
Toxicol Pathol. 1989;17(2):317-29. doi: 10.1177/019262338901700208.
9
Pathogenesis of experimental adrenal hemorrhagic necrosis ("apoplexy"): ultrastructural, biochemical, neuropharmacologic, and blood coagulation studies with acrylonitrile in the rat.实验性肾上腺出血性坏死(“中风”)的发病机制:用丙烯腈对大鼠进行的超微结构、生化、神经药理学及血液凝固研究
Lab Invest. 1980 May;42(5):533-46.
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Adrenocortical hemorrhagic necrosis: the role of catecholamines and retrograde medullary-cell embolism.
Arch Pathol Lab Med. 1981 Oct;105(10):536-9.

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2
Inappropriate angiogenic response as a novel mechanism of duodenal ulceration and impaired healing.异常的血管生成反应是十二指肠溃疡和愈合障碍的新机制。
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3
Intravenous injection of micafungin counteracts Candida albicans-induced aggravation of duodenal ulcers caused by cysteamine in rats.
静脉注射米卡芬净可对抗白色念珠菌引起的大鼠半胱胺所致十二指肠溃疡加重。
Dig Dis Sci. 2008 Sep;53(9):2422-8. doi: 10.1007/s10620-007-0159-9. Epub 2008 Jan 19.
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Detection of duodenal ulcer-associated genes in rats.
Dig Dis Sci. 2008 Feb;53(2):375-84. doi: 10.1007/s10620-007-9890-5. Epub 2007 Aug 4.
5
Duodenal ulcerogens cysteamine and propionitrile decrease duodenal neutralization of acid in the rat.十二指肠溃疡原半胱胺和丙腈可降低大鼠十二指肠对酸的中和作用。
Dig Dis Sci. 1983 Aug;28(8):716-23. doi: 10.1007/BF01312562.
6
Understanding biologic stress for study design and interpretation of results.理解生物应激以用于研究设计和结果解读。
Dig Dis Sci. 1985 Dec;30(12 Suppl):28S-31S. doi: 10.1007/BF01296969.
7
Predicting chemically induced duodenal ulcer and adrenal necrosis with classification trees.用分类树预测化学诱导的十二指肠溃疡和肾上腺坏死。
Proc Natl Acad Sci U S A. 1991 Jul 15;88(14):6298-302. doi: 10.1073/pnas.88.14.6298.
8
Haloalkylamine-induced renal papillary necrosis: a histopathological study of structure-activity relationships.卤代烷基胺诱导的肾乳头坏死:结构-活性关系的组织病理学研究
Int J Exp Pathol. 1991 Dec;72(6):631-46.