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Beschreibung

A rhodanine derivative that acts as a reversible, photoactivated (lambdamax = 415 nm), and highly TrpA1-selective channel activator and enables light-induced primary murine DRG calcium response in a TrpA1-dependent and HC-030031- (Cat. No. 648485) blockable manner, allowing light-induced activation only in hTrpA1-expressing, but not TrpV1- or TrpM8-expressing, HEK293T transfectants. Its in vivo efficacy is demonstrated in light-induced zebrafish motor activity (EC50/ECmax = 2 µ,M/3 µ,M) and low power 405 nm laser-induced head twitch response in mice (0.3 µ,mol Optovin/20 uL DMSO/ear applied atopically). Exhibits little or no inhibitory activity toward hERG or a panel of 50 human and rodent CNS receptors, channels, and transporters., A rhodanine derivative that acts as a reversible, photoactivated (lambdamax = 415 nm), and highly TrpA1-selective channel activator, presumably by a light-activated cysteine alkylation mechanism via the alpha,beta-unsaturated alkene group of Optovin rhodanine moiety, and enables light-induced primary murine DRG calcium response in a TrpA1-dependent and HC-030031- (Cat. No. 648485) blockable manner, allowing light-induced activation only in hTrpA1-expressing, but not TrpV1- or TrpM8-expressing, HEK293T transfectants. Its in vivo efficacy is demonstrated in light-induced zebrafish motor activity (EC50/ECmax = 2 µ,M/3 µ,M, with >1.6 µ,W/min 387-405 nm excitation) and low power 405 nm laser-induced head shake/twitch response in mice (0.3 µ,mol Optovin/20 uL DMSO/ear applied atopically before laser illumination). Exhibits little or no inhibitory activity toward hERG or a panel of 50 human and rodent CNS receptors, channels, and transporters.