title: Tuning photochromic ion channel blockers.
abstract: Photochromic channel blockers provide a conceptually simple and convenient way to modulate neuronal activity with light. We have recently described a family of azobenzenes that function as tonic blockers of K(v) channels but require UV-A light to unblock and need to be actively switched by toggling between two different wavelengths. We now introduce red-shifted compounds that fully operate in the visible region of the spectrum and quickly turn themselves off in the dark. Furthermore, we have developed a version that does not block effectively in the dark-adapted state, can be switched to a blocking state with blue light, and reverts to the inactive state automatically. Photochromic blockers of this type could be useful for the photopharmacological control of neuronal activity under mild conditions.
authors.affiliation: Department of Molecular and Cell Biology, University of California, Berkeley, California 94720, USA.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Mourot
authors.forename: Michael A
authors.initials: MA
authors.lastname: Kienzler
authors.forename: Matthew R
authors.initials: MR
authors.lastname: Banghart
authors.forename: Timm
authors.initials: T
authors.lastname: Fehrentz
authors.forename: Florian M E
authors.initials: FM
authors.lastname: Huber
authors.forename: Marco
authors.initials: M
authors.lastname: Stein
authors.forename: Richard H
authors.initials: RH
authors.lastname: Kramer
authors.forename: Dirk
authors.initials: D
authors.lastname: Trauner
mesh_terms: D000818:Animals; D002531:Cerebellum / Q000187:drug effects / Q000378:metabolism; D051668:Delayed Rectifier Potassium Channels / Q000187:drug effects; D004583:Electrons; D055724:Electrophysiological Phenomena; D057809:HEK293 Cells; D006801:Humans; D008839:Microelectrodes; D018408:Patch-Clamp Techniques; D010777:Photochemistry; D026902:Potassium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012997:Solvents; D013056:Spectrophotometry, Ultraviolet; D013237:Stereoisomerism; D013816:Thermodynamics
chemical_list: D051668:Delayed Rectifier Potassium Channels; D026902:Potassium Channel Blockers; D012997:Solvents