Mapping of the benzodiazepine recognition site on GABA(A) receptors.

@article{Sigel2002MappingOT,
  title={Mapping of the benzodiazepine recognition site on GABA(A) receptors.},
  author={Erwin Sigel},
  journal={Current topics in medicinal chemistry},
  year={2002},
  volume={2 8},
  pages={
          833-9
        }
}
  • Erwin Sigel
  • Published 2002 in Current topics in medicinal chemistry
Ligands of the benzodiazepine binding site of the GABAA receptor come in three flavors: positive allosteric modulators, negative allosteric modulators and antagonists, all of which can bind with high affinity. The GABA(A) receptor is a pentameric protein which forms a chloride selective ion channel and ligands of the benzodiazepine binding site stabilize three different conformations of this receptor channel. Classical benzodiazepines exert a positive allosteric effect by increasing the… CONTINUE READING
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