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几种药物溶剂的药效学活性研究。2. 甘油、N-(β-羟乙基) - 乳酰胺、聚乙二醇400

[Studies on the pharmacodynamic activity of several drug solvents. 2. Glycerin, N-(beta-hydroxyethyl)-lactamide, polyethylene glycol 400].

作者信息

Budden R, Kühl U G, Buschmann G

出版信息

Arzneimittelforschung. 1978;28(9):1579-86.

PMID:582559
Abstract

The drug solvents glycerin, N-(beta-hydroxyethyl)-lactamide, and polyethylene glycol 400 (Lutrol 9) were examined for their pharmacodynamic properties in the following tests: i.p. toxicity, "sign pattern", inclined screen test, balance rod test, and potentiation of hexobarbitone sleeping time in mice, spasmolytic activity in the guinea pig isolated ileum, and cardiovascular studies in anaesthetized rats, cats, and dogs including the i.v. toxicity. In mice and rats glycerin exhibited the highest tocicity as well as the greatest activity in potentiating hexobarbitone sleeping time. In the isolated ileum the solvents showed unspecific spasmolytic activities with histamine, carbachol, and BaCl2 as spasmogens. After i.v. administration in rats, cats, and dogs the solvents caused cardiovascular effects even in very low doses. Based on the pharmacodynamic properties, doses are recommended for each solvent which should not be exceeded without control experiments in the laboratory routine. These tolerable doses do not only depend on the species but also on the test concerned.

摘要

对药物溶剂甘油、N-(β-羟乙基)-乳酰胺和聚乙二醇400(Lutrol 9)进行了以下试验以研究其药效学性质:腹腔注射毒性、“体征模式”、倾斜筛试验、平衡杆试验以及对小鼠戊巴比妥睡眠时间的增强作用、对豚鼠离体回肠的解痉活性,以及对麻醉大鼠、猫和狗的心血管研究,包括静脉注射毒性。在小鼠和大鼠中,甘油表现出最高的毒性以及在增强戊巴比妥睡眠时间方面最大的活性。在离体回肠中,这些溶剂对以组胺、卡巴胆碱和氯化钡作为致痉剂时表现出非特异性解痉活性。在大鼠、猫和狗静脉注射后,这些溶剂即使在非常低的剂量下也会引起心血管效应。基于药效学性质,针对每种溶剂推荐了剂量,在实验室常规操作中若无对照实验,不应超过这些剂量。这些可耐受剂量不仅取决于物种,还取决于相关试验。

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