A potent photoreactive general anesthetic with novel binding site selectivity for GABA_A receptors.

ABSTRACT: The pentameric γ-aminobutyric acid type A receptors (GABA_ARs) are the major inhibitory ligand-gated ion channels in the central nervous system. They mediate diverse physiological functions, mutations in them are associated with mental disorders and they are the target of many drugs such as general anesthetics, anxiolytics and anti-convulsants. The five subunits of synaptic GABA_ARs are arranged around a central pore in the order β-α-β-α-γ. In the outer third of the transmembrane domain (TMD) drugs may bind to five homologous intersubunit binding sites. Etomidate binds between the pair of β - α subunit interfaces (designated as β⁺/α^-) and R-mTFD-MPAB binds to an α⁺/β^- and an γ⁺/β^- subunit interface (a β

SUBMITTER: Shalabi AR 

PROVIDER: S-EPMC7342775 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature