小说 H2S-释放双功能抗歇斯塔林分子,具有改善的抗和减少镇静作用
Ivi Antoniadou1, Maria Georgiou2, Yannis Dotsikas2
1Biomedical Research Foundation of the Academy of Athens, 4 Soranou Efesiou Str, Athens 115 27, Greece.
结合抗组胺剂与硫化 (H2S) 捐赠者的新混合分子显示了增强的抗 (抗性) 疗效. 这些化合物有效地减少了,与传统抗胰岛素相比,镇静副作用较少.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
- 胃肠病学 胃肠病学
背景情况:
- 硫化 (H2S) 是一种具有已知的抗炎和抗性质的内源性气传递物.
- 抗胰岛素通常用于治疗,但可能有副作用,如镇静.
研究的目的:
- 合成和评估结合抗组胺和H2S释放功能的新型双功能分子.
- 评估这些混合化合物的体外和体外抗疗效和安全性.
主要方法:
- 合成混合分子,其中包括抗组胺剂和释放H2S的药.
- 在体外评估H2S释放使用甲基蓝和酸试验.
- 通过抑制组织因子表达来评估H1阻断活性.
- 在动物模型中对抗和镇静作用的体内测试.
主要成果:
- 所有合成的混合化合物都显示了剂量依赖的H2S释放,并保持了显著的组胺H1阻断活性.
- 两种化合物在抑制基因组胺诱导的方面表现出比原始抗组胺药物 (素, cetirizine) 更高的疗效.
- 混合化合物显示降低了镇静作用,表明安全性得到改善.
结论:
- 双功能分子集成H2S捐赠和抗组胺特性,提供增强的抗作用.
- 释放H2S的部分可能有助于提高这些新型化合物的疗效和减少副作用.
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