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Azo‐Propofols: Photochromic Potentiators of GABA A Receptors
Author(s) -
Stein Marco,
Middendorp Simon J.,
Carta Valentina,
Pejo Ervin,
Raines Douglas E.,
Forman Stuart A.,
Sigel Erwin,
Trauner Dirk
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201205475
Subject(s) - potentiator , photochromism , gabaa receptor , chemistry , receptor , chloride channel , neurotransmitter , inhibitory postsynaptic potential , glutamate receptor , biophysics , neuroscience , pharmacology , biochemistry , biology , photochemistry
Shine and rise! GABA A receptors are ligand‐gated chloride ion channels that respond to γ‐aminobutyric acid (GABA), which is the major inhibitory neurotransmitter of the mammalian central nervous system. Azobenzene derivatives of propofol, such as compound 1 (see scheme), increase GABA‐induced currents in the dark form and lose this property upon light exposure and thus function as photochromic potentiators. Compound 1 can be employed as a light‐dependent general anesthetic in translucent tadpoles.