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
^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.
PMID18499743.
S2CID517735.
^Vincent F, Duncton MA (2011). "TRPV4 agonists and antagonists". Current Topics in Medicinal Chemistry. 11 (17): 2216–26.
doi:
10.2174/156802611796904861.
PMID21671873.
^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.
PMID32126273.
S2CID212406213.
^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.
PMID32706268.
S2CID220731478.