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GSK1016790A

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
GSK1016790A
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
PubChemCID
ChemSpider
ChEBI
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC28H32Cl2N4O6S2
Molar mass655.61 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 (akaGSK101) is a drug developed byGlaxoSmithKline which acts as a potent and selectiveagonist for theTRPV4 receptor. It has been used to study the role of TRPV4 receptors in the function ofsmooth muscle tissue, particularly that lining blood vessels,lymphatic system, and thebladder.[1][2][3][4][5]

References

[edit]
  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.
TRPA
Activators
Blockers
TRPC
Activators
Blockers
TRPM
Activators
Blockers
TRPML
Activators
Blockers
TRPP
Activators
Blockers
TRPV
Activators
Blockers
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