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Updated: May 18, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Azo-propofols: photochromic potentiators of GABA(A) receptors
Marco Stein1, Simon J Middendorp, Valentina Carta
1Department of Chemistry, Ludwig-Maximilians-Universität, München and Center of Integrated Protein Science, 81377 Munich, Germany.
Abstract:
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.
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