Chemistry:GSK1016790A

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Short description: Chemical compound
GSK1016790A
GSK1016790A structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEBI
Chemical and physical data
FormulaC28H32Cl2N4O6S2
Molar mass655.61 g·mol−1
3D model (JSmol)

GSK1016790A (aka GSK101) is a drug developed by GlaxoSmithKline which acts as a potent and selective agonist for the TRPV4 receptor. It has been used to study the role of TRPV4 receptors in the function of smooth muscle tissue, particularly that lining blood vessels, lymphatic system, and the bladder.[1][2][3][4][5]

References

  1. "N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I". The Journal of Pharmacology and Experimental Therapeutics 326 (2): 432–42. August 2008. doi:10.1124/jpet.108.139295. PMID 18499743. 
  2. "TRPV4 agonists and antagonists". Current Topics in Medicinal Chemistry 11 (17): 2216–26. 2011. doi:10.2174/156802611796904861. PMID 21671873. 
  3. "Therapeutic potential of blood flow mimetic compounds in preventing endothelial dysfunction and atherosclerosis". Pharmacological Research 155: 104737. May 2020. doi:10.1016/j.phrs.2020.104737. PMID 32126273. 
  4. "Therapeutic potential of pharmacological agents targeting TRP channels in CNS disorders". Pharmacological Research 159: 105026. September 2020. doi:10.1016/j.phrs.2020.105026. PMID 32562815. 
  5. "TRPV4 channels' dominant role in the temperature modulation of intrinsic contractility and lymph flow of rat diaphragmatic lymphatics". American Journal of Physiology. Heart and Circulatory Physiology 319 (2): H507–H518. August 2020. doi:10.1152/ajpheart.00175.2020. PMID 32706268.