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- W2033842010 abstract "TRPV4 belongs to the TRPV subfamily of Transient Receptor Potential (TRP) ion channels. This year marks the 10 year anniversary of the discovery of this polymodal ion channel which is activated by a variety of stimuli including warm temperatures, hypotonicity and endogenous lipids. Coupled with a widespread tissue distribution, this activation profile has resulted in a large number of disparate physiological functions for TRPV4. These range from temperature monitoring in skin keratinocytes to osmolarity sensing in kidneys, sheer stress detection in blood vessels and osteoclast differentiation control in bone. As knowledge of its physiological roles has expanded, interest in targeting TRPV4 modulation for therapeutic purposes has arisen and is now focused on several areas. First, as with related TRP channels TRPV1, TRPV3, TRPM8 and TRPA1, TRPV4 antagonism is being considered for inflammatory and neuropathic pain treatment. Recent work conducted using KO mice and agonists 4αPDD and GSK1016790A suggests bladder dysfunctions may also be targeted. Additionally, ventilator-induced lung injury has emerged as another potential indication for TRPV4 antagonists. Herein we review the known small molecule modulators of TRPV4 and relate progress made in identifying potent, selective and bioavailable agonists and antagonists to interrogate this ion channel in vivo. Keywords: 4αPDD, activator, blocker, GSK1016790A, inhibitor, phorbol ester, RN-1747, RN-1734, ruthenium red, TRPV4, polymodal ion channel, temperature monitoring in skin, keratinocytes, osmolarity sensing in kidneys, sheer stress detection in blood vessels" @default.
- W2033842010 created "2016-06-24" @default.
- W2033842010 creator A5007795346 @default.
- W2033842010 creator A5041051375 @default.
- W2033842010 date "2011-09-01" @default.
- W2033842010 modified "2023-10-17" @default.
- W2033842010 title "TRPV4 Agonists and Antagonists" @default.
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- W2033842010 doi "https://doi.org/10.2174/156802611796904861" @default.
- W2033842010 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21671873" @default.
- W2033842010 hasPublicationYear "2011" @default.
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