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吡嗪咪唑啉类化合物的结构与α-肾上腺素能活性

Structure and alpha-adrenergic activity of pyrazinimidazolines.

作者信息

Kaliszan R, Damasiewicz B, Nasal A, Radwańska A, Foks H, Kuźmierkiewicz W, Pancechowska-Ksepko D, Rudnicka K, Wisterowicz K, Ośmiałowski K

出版信息

Agents Actions. 1985 Jul;16(5):435-42. doi: 10.1007/BF01982885.

DOI:10.1007/BF01982885
PMID:2996322
Abstract

The effects of newly synthetized pyrazinimidazolines on the contraction of isolated rat tail artery and on the chronotropic action of rat atria as well as the effects on blood pressure in anaesthetized rats were determined. The structure-activity relationships were studied, including standard imidazoline drugs. Starting from practically inactive derivatives the step-by-step structural modifications have been made resulting in markedly active chemical congeners, which were designed, synthetized and tested pharmacologically.

摘要

测定了新合成的吡嗪咪唑啉对离体大鼠尾动脉收缩、大鼠心房变时作用的影响以及对麻醉大鼠血压的影响。研究了包括标准咪唑啉药物在内的构效关系。从实际无活性的衍生物开始,逐步进行结构修饰,得到了活性显著的化学同系物,对其进行了设计、合成及药理测试。

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Structure and alpha-adrenergic activity of pyrazinimidazolines.吡嗪咪唑啉类化合物的结构与α-肾上腺素能活性
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引用本文的文献

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本文引用的文献

1
Comparison of crystallographic and quantum mechanical analysis with biological data on clonidine and some related analogues.可乐定及一些相关类似物的晶体学和量子力学分析与生物学数据的比较。
Mol Pharmacol. 1982 Mar;21(2):400-8.
2
Chromatography in studies of quantitative structure-activity relationships.
J Chromatogr. 1981 May 1;220(1):71-83. doi: 10.1016/s0021-9673(00)98504-2.
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Chemistry of lofexidine.洛非西定的化学性质。
Arzneimittelforschung. 1982;32(8a):916-8.
4
alpha 1-adrenoceptors can mediate chronotropic responses in the rat heart.α1肾上腺素能受体可介导大鼠心脏的变时反应。
Br J Pharmacol. 1981 Jul;73(3):586-8. doi: 10.1111/j.1476-5381.1981.tb16791.x.
5
Hypotensive and alpha-adrenergic activities of 2-(2,3,6-trichlorophenylimino) and 2-(2,3-dichloro-6-methylphenylimino) imidazolidine, two potent derivatives of clonidine.可乐定的两种有效衍生物2-(2,3,6-三氯苯基亚氨基)和2-(2,3-二氯-6-甲基苯基亚氨基)咪唑烷的降压及α-肾上腺素能活性
Br J Pharmacol. 1983 Mar;78(3):479-87. doi: 10.1111/j.1476-5381.1983.tb08808.x.
6
Receptor interactions of imidazolines. XI. Alpha-adrenergic and antihypertensive effects of clonidine and its methylene-bridged analog, St 1913.咪唑啉的受体相互作用。XI. 可乐定及其亚甲基桥连类似物St 1913的α-肾上腺素能和降压作用。
Pharmacology. 1982;25(4):187-201. doi: 10.1159/000137742.
7
Presynaptic activity of the imidazolidine derivative ST 587, a highly selective alpha 1-adrenoceptor agonist.咪唑烷衍生物ST 587(一种高度选择性的α1肾上腺素能受体激动剂)的突触前活性。
Eur J Pharmacol. 1982 Aug 27;82(3-4):203-6. doi: 10.1016/0014-2999(82)90514-3.
8
Studies on some para-substituted clonidine derivatives that exhibit an alpha-adrenoceptor stimulant activity.对一些表现出α-肾上腺素能受体刺激活性的对-取代可乐定衍生物的研究。
Br J Pharmacol. 1980;71(1):5-9. doi: 10.1111/j.1476-5381.1980.tb10902.x.
9
A perfused tail artery preparation from the rat.大鼠的灌注尾动脉标本。
J Pharm Pharmacol. 1969 Dec;21(12):826-32. doi: 10.1111/j.2042-7158.1969.tb08180.x.
10
A search for new antihypertensive agents. I. Alpha-adrenergic activity and selection of structures among pyrazine substituted imidazolines.新型抗高血压药物的研究。I. 吡嗪取代咪唑啉类化合物的α-肾上腺素能活性及结构筛选
Pol J Pharmacol Pharm. 1985 Jan-Feb;37(1):79-88.