GSK1016790A

Last updated
GSK1016790A
GSK1016790A structure.png
Identifiers
  • N-[(1S)-1-[[4-[(2S)-2-[[(2,4-Dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]benzo[b]thiophene-2-carboxamide
CAS Number
PubChem CID
ChemSpider
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
Formula C28H32Cl2N4O6S2
Molar mass 655.61 g·mol−1
3D model (JSmol)
  • CC(C)C[C@H](NC(C1=CC2=CC=CC=C2S1)=O)C(N3CCN(CC3)C([C@H](CO)NS(=O)(C4=C(Cl)C=C(Cl)C=C4)=O)=O)=O
  • InChI=1S/C28H32Cl2N4O6S2/c1-17(2)13-21(31-26(36)24-14-18-5-3-4-6-23(18)41-24)27(37)33-9-11-34(12-10-33)28(38)22(16-35)32-42(39,40)25-8-7-19(29)15-20(25)30/h3-8,14-15,17,21-22,32,35H,9-13,16H2,1-2H3,(H,31,36)/t21-,22-/m0/s1
  • Key:IVYQPSHHYIAUFO-VXKWHMMOSA-N

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. ↑ Thorneloe KS, Sulpizio AC, Lin Z, Figueroa DJ, Clouse AK, McCafferty GP, et al. (August 2008). "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. doi:10.1124/jpet.108.139295. PMID   18499743. S2CID   517735.
  2. ↑ Vincent F, Duncton MA (2011). "TRPV4 agonists and antagonists". Current Topics in Medicinal Chemistry. 11 (17): 2216–26. doi:10.2174/156802611796904861. PMID   21671873.
  3. ↑ Xu S (May 2020). "Therapeutic potential of blood flow mimetic compounds in preventing endothelial dysfunction and atherosclerosis". Pharmacological Research. 155 104737. doi:10.1016/j.phrs.2020.104737. PMID   32126273. S2CID   212406213.
  4. ↑ Thapak P, Vaidya B, Joshi HC, Singh JN, Sharma SS (September 2020). "Therapeutic potential of pharmacological agents targeting TRP channels in CNS disorders". Pharmacological Research. 159 105026. doi:10.1016/j.phrs.2020.105026. PMID   32562815. S2CID   219959586.
  5. ↑ Solari E, Marcozzi C, Bistoletti M, Baj A, Giaroni C, Negrini D, Moriondo A (August 2020). "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. doi:10.1152/ajpheart.00175.2020. hdl: 11383/2096014 . PMID   32706268. S2CID   220731478.
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