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莫西沙星和吉米沙星通过 ATP 敏感性钾通道介导其抗痉挛作用:一项体外生物测定研究。

Moxifloxacin and gemifloxacin mediates its antispasmodic profile via ATP-sensitive potassium channels: An in-vitro bioassay study.

机构信息

Department of Pharmacy, Shaheed Benazir Bhutto University Sheringal, Dir Upper, Khyber Pakhtunkhwa, Pakistan/ Department of Pharmacology, Institute of Basic Medical Sciences, Khyber Medical University, Peshawar, KP, Pakistan.

Department of Pharmacy, Shaheed Benazir Bhutto University Sheringal, Dir Upper, Khyber Pakhtunkhwa, Pakistan.

出版信息

Pak J Pharm Sci. 2021 Sep;34(5(Supplementary)):1983-1988.

PMID:34836870
Abstract

Moxifloxacin and gemifloxacin were tested on isolated rabbits' jejunal preparations as little is known about its effects on gastrointestinal tissues. Moxifloxacin and gemifloxacin were tested in concentrations 0.01-10μg/mL for possible effect(s) on isolated rabbits' jejunal preparations. The drugs were applied on spontaneous, on low K (20mM)-induced contractions and on high K (80mM)-induced contractions. Response was plotted as % of its respective controls. EC50 for Moxifloxacin and Gemifloxacin on spontaneous (without Glibenclamide) contractions are 2.83±0.5μg/mL and 1.11±0.2μg/mL, respectively. Moxifloxacin and Gemifloxacin relaxed the low K+ (20mM) -induced contractions, which were inhibited in presence of Glibenclamide (3μM). Our result indicates that the relaxant activity of Moxifloxacin and Gemifloxacin is mediated possibly through activation of ATP-sensitive potassium channels (KATP). The relaxant effect of Moxifloxacin and Gemifloxacin is predominantly mediated by activation of ATP-Sensitive potassium channels (K), which could be cause of one of relaxing mechanisms.

摘要

莫西沙星和吉米沙星在离体兔空肠标本上进行了测试,因为人们对其在胃肠道组织中的作用知之甚少。在 0.01-10μg/mL 的浓度下,对莫西沙星和吉米沙星进行了测试,以观察它们对离体兔空肠标本可能产生的影响。药物应用于自发性收缩、低钾(20mM)诱导收缩和高钾(80mM)诱导收缩。将反应绘制成相对于各自对照的百分比。莫西沙星和吉米沙星对自发性(无格列本脲)收缩的 EC50 分别为 2.83±0.5μg/mL 和 1.11±0.2μg/mL。莫西沙星和吉米沙星可松弛低钾(20mM)诱导的收缩,在格列本脲(3μM)存在下,该收缩被抑制。我们的结果表明,莫西沙星和吉米沙星的舒张活性可能是通过激活三磷酸腺苷敏感钾通道(KATP)介导的。莫西沙星和吉米沙星的舒张作用主要通过激活三磷酸腺苷敏感钾通道(K)介导,这可能是其舒张机制之一。

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