GSK1018921

From WikiMD's Wellness Encyclopedia



GSK1018921 is a chemical compound that has been studied for its potential effects on the transient receptor potential vanilloid 4 (TRPV4) ion channel. TRPV4 is a member of the transient receptor potential channel family, which is involved in various physiological processes, including osmoregulation, mechanosensation, and thermosensation.

Mechanism of Action[edit | edit source]

GSK1018921 acts as a potent and selective agonist of the TRPV4 channel. By binding to TRPV4, GSK1018921 induces the opening of the channel, allowing the influx of calcium ions (Ca²⁺) into the cell. This influx of calcium can trigger various downstream signaling pathways, leading to physiological responses such as vasodilation, modulation of pain perception, and regulation of cellular volume.

Pharmacological Effects[edit | edit source]

Studies have shown that GSK1018921 can induce vasodilation in isolated blood vessels, suggesting its potential use in conditions where increased blood flow is beneficial. Additionally, its role in modulating pain perception has been explored, with research indicating that TRPV4 activation can influence nociceptive pathways.

Research and Development[edit | edit source]

GSK1018921 has been primarily used as a research tool to study the function of TRPV4 channels in various biological systems. Its high selectivity and potency make it an ideal candidate for investigating the physiological and pathological roles of TRPV4.

Clinical Implications[edit | edit source]

While GSK1018921 has not been developed as a therapeutic drug, its ability to modulate TRPV4 activity has implications for the treatment of diseases such as pulmonary edema, neuropathic pain, and bladder dysfunction. Further research is needed to explore its potential therapeutic applications and safety profile.

Safety and Toxicity[edit | edit source]

As with many research compounds, the safety and toxicity profile of GSK1018921 in humans is not well-established. Preclinical studies are necessary to determine its potential side effects and safe dosage ranges.

Also see[edit | edit source]


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Contributors: Prab R. Tumpati, MD