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胍和脒衍生物的结构与去甲肾上腺素耗竭作用之间的关系(作者译)

[Relationships between structure and the noradrenaline depleting effects of guanidine and amidine derivatives (author's transl)].

作者信息

Benkert B, Benthe H F, Göthert M, Schmoldt A

出版信息

Arzneimittelforschung. 1975 Sep;25(9):1404-8.

PMID:1242662
Abstract

In guinea pigs we studied the noradrenaline (NA) depletion in the sympathetic nerve terminals of the heart exerted by 24 derivatives of guanidine and amidine; the effects of these substances being considerably similar in their chemical structure were compared to those of reserpine, guanethidine, guanoxan and cyclazenin. Substitution of the free guanidine group to give an imidazoline or imidazolidine ring diminished the activity of the compounds. If the benzodioxane ring of guanoxan was "opened" to give a diether of catechol, the activity of the substances was not altered. We also observed a NA depletion after injection of some guanidine derivatives substituted with piperazine. The elongation of the aliphatic chain between guanidine and the aromatic substituent considerably decreased the activity of the compounds.

摘要

在豚鼠中,我们研究了24种胍和脒衍生物对心脏交感神经末梢去甲肾上腺素(NA)的耗竭作用;将这些化学结构相当相似的物质的作用与利血平、胍乙啶、胍生和环拉嗪的作用进行了比较。游离胍基被取代形成咪唑啉或咪唑烷环会降低化合物的活性。如果胍生的苯并二恶烷环“打开”形成儿茶酚二醚,这些物质的活性不会改变。我们还观察到,注射一些被哌嗪取代的胍衍生物后会出现NA耗竭。胍基与芳族取代基之间脂肪链的延长会大大降低化合物的活性。

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