Piperazine, 1-[(4-chloro-2-nitrophenyl)sulfonyl]-4-(phenylmethyl)- 1-[(4-Chloro-2-nitrophenyl)sulfonyl]-4-(phenylmethyl)piperazine
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RN 1747, a selective TRPV4 agonist (EC50= 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively), represents the first drug-like TRPV4 antagonist with selectivity over closely related TRP channels. The activities of these compounds were characterized using two different systems: Ca2+ influx assay with human, mouse and rat TRPV4-expressing HEK293 cells and electrophysiology in hTRPV4-transfected Xenopus oocytes. Importantly, RN-1734 antagonized both ligand-gated activation and hypotonicity-induced opening of TRPV4 in both types of assay.
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