当前位置: X-MOL 学术 › › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
GYY4137, a novel water-soluble, H2S-releasing molecule.
Methods in Enzymology Pub Date : 2015 , DOI: 10.1016/bs.mie.2014.11.014
Peter Rose , Brian W. Dymock , Philip K. Moore

Hydrogen sulfide (H2S) is now recognized as the so called "third gasotransmitter" taking its place alongside nitric oxide and carbon monoxide. In recent years, H2S has been reported to exhibit a diverse range of pharmacological effects in biological systems. Much of this evidence is derived from a combination of conventional pharmacological and genetic approaches coupled with the use of chemical compounds such as sodium hydrosulfide, a rapid H2S releasing donor. Developments in the design of new drug entities which attempt to take into account physicochemical properties, targeting to specific cellular organelles, triggering of H2S release upon specific chemical reactions in the cell, and controlling the release of H2S over extended periods of time have been described. For most of these molecules, little or no work has been conducted to determine their biological activity or possible therapeutic effects. It is therefore not clear whether such molecules have therapeutic potential which highlights the need for further in vivo studies. One exception to the general rule is GYY4137 (morpholin-4-ium 4-methoxyphenyl(morpholino) phosphinodithioate), a slow releasing H2S donor, which has been evaluated for activity in a range of pharmacological models both in vitro and in vivo. GYY4137 was first reported to release H2S and exhibit vasodilator activity over 5 years ago and, to date, GYY4137 is becoming increasingly employed as a pharmacological "tool" to explore the biological functions of H2S.

中文翻译:

GYY4137,一种新型的可释放H2S的水溶性分子。

硫化氢(H2S)现在被认为是所谓的“第三种气体递质”,与一氧化氮和一氧化碳并存。近年来,据报道,H 2 S在生物系统中表现出各种各样的药理作用。许多证据来自常规药理学和遗传学方法的结合,再加上使用诸如硫化氢钠(一种快速释放H2S的供体)之类的化合物。已经描述了尝试考虑理化特性,靶向特定细胞器,在细胞中发生特定化学反应后触发H2S释放以及控制H2S释放的新药实体设计中的发展。对于大多数这些分子,很少或没有工作来确定其生物学活性或可能的治疗效果。因此,尚不清楚此类分子是否具有治疗潜力,从而凸显了对进一步体内研究的需求。一般规则的一个例外是GYY4137(吗啉-4- 4- 4-甲氧基苯基(吗啉代)膦二硫代乙酸盐),一种缓慢释放的H2S供体,已对其在体外和体内的一系列药理模型中的活性进行了评估。据报道,GYY4137在5年前释放H2S并表现出血管舒张活性,迄今为止,GYY4137被越来越多地用作探索H2S生物学功能的药理“工具”。因此,尚不清楚此类分子是否具有治疗潜力,从而凸显了对进一步体内研究的需求。一般规则的一个例外是GYY4137(吗啉-4- 4- 4-甲氧基苯基(吗啉代)膦二硫代乙酸盐),一种缓慢释放的H2S供体,已对其在体外和体内的一系列药理模型中的活性进行了评估。据报道,GYY4137在5年前释放H2S并表现出血管舒张活性,迄今为止,GYY4137被越来越多地用作探索H2S生物学功能的药理“工具”。因此,尚不清楚此类分子是否具有治疗潜力,从而凸显了对进一步体内研究的需求。一般规则的一个例外是GYY4137(吗啉-4- 4- 4-甲氧基苯基(吗啉代)膦二硫代乙酸盐),一种缓慢释放的H2S供体,已对其在体外和体内的一系列药理模型中的活性进行了评估。据报道,GYY4137在5年前释放H2S并表现出血管舒张活性,迄今为止,GYY4137被越来越多地用作探索H2S生物学功能的药理“工具”。已在体外和体内多种药理模型中评估了其活性。据报道,GYY4137在5年前释放H2S并表现出血管舒张活性,迄今为止,GYY4137被越来越多地用作探索H2S生物学功能的药理“工具”。已在体外和体内一系列药理模型中评估了其活性。据报道,GYY4137在5年前释放H2S并表现出血管舒张活性,迄今为止,GYY4137被越来越多地用作探索H2S生物学功能的药理“工具”。
更新日期:2017-01-31
down
wechat
bug