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Tuesday, 11 September, 2012

Azo-Propofols: Photochromic Potentiators of GABAA Receptors

M. Stein, S. J. Middendorp, V. Carta, E. Pejo, D. E. Raines, S. A. Forman, E. Sigel, and D. Trauner -
Angew. Chem. Int. Edition, doi: 10.1002/anie.201205475, published online: 11 September 2012

GABAA 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 loose 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.

 

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