Photoswitchable Nav, Cav and Kv channel blocker. Blocks channels in the trans conformation. Switches conformation from cis to trans at 500 nm and trans to cis at 380 nm. Normally membrane impermeant, but enters nociceptive neurons via ion channels activated by noxious stimuli, particularly TRPV1. Exhibits optically reversible local anesthesia in rats.
Mourot et al (2012) Rapid optical control of nociception with an ion-channel photoswitch. Nat.Methods 9 396 PMID:22343342 |Banghart MR et al (2009) Photochromic blockers of voltage-gated potassium channels. Angew.Chem.Int.Ed. 48 9097 PMID:19882609