GSK1016790A

GSK1016790A is a potent and selective activator of the transient receptor potential vanilloid 4 (TRPV4) channel, a member of the transient receptor potential (TRP) channel family. This compound was developed by GlaxoSmithKline (GSK), a British multinational pharmaceutical company.

Chemistry

GSK1016790A is a small molecule with the chemical formula C22H23F3N4O. It is a potent and selective activator of the TRPV4 channel, with an EC50 (half maximal effective concentration) of approximately 10 nM.

Pharmacology

The TRPV4 channel is a non-selective cation channel that is sensitive to mechanical and osmotic changes, as well as heat. Activation of this channel by GSK1016790A can lead to various physiological responses, including vasodilation, secretion of cytokines, and changes in cell volume.

Clinical significance

GSK1016790A has been used in preclinical studies to investigate the role of the TRPV4 channel in various diseases, including pulmonary edema, cystic fibrosis, and cancer. However, the compound is not currently approved for use in humans.

See also

• Transient receptor potential channel
• GlaxoSmithKline

References

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