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依普唑醇抗支气管收缩作用的机制。II. 对豚鼠的体内研究。

Mechanisms of anti-bronchoconstrictive effects of eprozinol. II. In vivo studies on the guinea pig.

作者信息

Labrid C, Duchene-Marullaz P, Rispat G

出版信息

Pharmacology. 1981;23(1):48-55. doi: 10.1159/000137526.

DOI:10.1159/000137526
PMID:7312935
Abstract

The possible interactions of the anti-asthmatic compound, eprozinol, with bronchoconstrictors and adrenergic agents were investigated in the anaesthetised guinea pig by means of the following techniques: (1) study of the inhibition of histamine- and serotonin-induced bronchospasm; (2) investigation of potentiation or antagonism between the anti-bronchoconstrictor effects of eprozinol and isoprenaline; (3) investigation of propranolol-induced blockade of the anti-bronchoconstrictor effects of eprozinol and several reference compounds. In the anaesthetised guinea pig, eprozinol (5 mge . kg-1), isoprenaline (2 micrograms . kg-1) and theophylline (15 mg . kg-1) administered intravenously cause a clear inhibition of the bronchospasm induced by intravenous perfusion of histamine or serotonin, with an intensity not significantly different for all three compounds. The anti-bronchoconstrictor activities of eprozinol and isoprenaline with regard to histamine are directly additive and show absolutely no interference with one another. Propranolol is without effect on in vivo anti-bronchoconstrictor activity of eprozinol on tracheal musculature. It is concluded that the mechanisms brought into play by eprozinol to exert anti-bronchoconstrictor and bronchorelaxant activity, are completely independent of the adrenergic system.

摘要

采用以下技术,在麻醉豚鼠中研究了抗哮喘化合物乙磺半胱氨酸与支气管收缩剂和肾上腺素能药物之间可能的相互作用:(1) 研究对组胺和5-羟色胺诱导的支气管痉挛的抑制作用;(2) 研究乙磺半胱氨酸和异丙肾上腺素抗支气管收缩作用之间的增强或拮抗作用;(3) 研究普萘洛尔对乙磺半胱氨酸和几种参比化合物抗支气管收缩作用的阻断作用。在麻醉豚鼠中,静脉注射乙磺半胱氨酸(5mg·kg-1)、异丙肾上腺素(2μg·kg-1)和茶碱(15mg·kg-1)可明显抑制静脉灌注组胺或5-羟色胺所诱导的支气管痉挛,三种化合物的抑制强度无显著差异。乙磺半胱氨酸和异丙肾上腺素对组胺的抗支气管收缩活性直接相加,且彼此间绝对无干扰。普萘洛尔对乙磺半胱氨酸对气管平滑肌的体内抗支气管收缩活性无影响。得出的结论是,乙磺半胱氨酸发挥抗支气管收缩和支气管舒张活性的机制完全独立于肾上腺素能系统。

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1
Mechanisms of anti-bronchoconstrictive effects of eprozinol. II. In vivo studies on the guinea pig.依普唑醇抗支气管收缩作用的机制。II. 对豚鼠的体内研究。
Pharmacology. 1981;23(1):48-55. doi: 10.1159/000137526.
2
Mechanisms of anti-bronchoconstrictive effects of eprozinol. I. In vitro studies.依普唑醇抗支气管收缩作用的机制。I. 体外研究。
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