GYY4137, a novel water-soluble, H2S-releasing molecule

Rose, Peter, Dymock, Brian W. and Moore, Philip K. (2015) GYY4137, a novel water-soluble, H2S-releasing molecule. Methods in Enzymology. Hydrogen Sulfide in Redox Biology, Part A, 554 . pp. 143-167. ISSN 0076-6879

GYY4137, a novel water-soluble, H2S-releasing molecule
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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.

Keywords:hydrogen sulfide, unclassified drug, vasodilator agent, morpholin 4 ium 4 methoxyphenyl(morpholino)phosphinodithioate, aging, antiinflammatory activity, apoptosis, Article, biological activity, cardiovascular system, cell aging, cell cycle progression, chemical reaction, drug synthesis, G1 phase cell cycle checkpoint, G2 phase cell cycle checkpoint, genital system, human, in vitro study, in vivo study, inflammation, nonhuman, oxidative stress, physical chemistry, priority journal, senescence, signal noise ratio, thrombocyte function, vascular smooth muscle, bmjgoldcheck, NotOAChecked
Subjects:C Biological Sciences > C700 Molecular Biology, Biophysics and Biochemistry
Divisions:College of Science > School of Life Sciences
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ID Code:16944
Deposited On:17 Mar 2015 10:34

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