Recent advances in TRPV4 agonists and antagonists.

Basic Information

ID: ALA4627288

Journal: Bioorg Med Chem Lett

Title: Recent advances in TRPV4 agonists and antagonists.

Authors: Lawhorn BG, Brnardic EJ, Behm DJ.

Abstract: TRPV4 is a ubiquitously expressed, non-selective cation channel activated by a range of stimuli including hypotonicity, temperature, pH, stretch and endogenous ligands. Agents that modulate TRPV4 are sought as potential therapeutics for the treatment of many diseases including osteoarthritis, respiratory illnesses, gastrointestinal disorders, pain and congestive heart failure. In recent years, significant advances in TRPV4 drug discovery have been realized as at least seven novel TRPV4 agonist or antagonist templates were reported and the first selective TRPV4 antagonist was evaluated in early clinical trials.

CiteXplore: 32063431

DOI: 10.1016/j.bmcl.2020.127022

Patent ID: