Teaching an old GABA receptor new tricks

Anesth Analg. 2012 Aug;115(2):270-3. doi: 10.1213/ANE.0b013e31824a0b3c. Epub 2012 Feb 17.

Abstract

The accompanying articles in this issue of the journal's special collection describe attempts to improve on the dynamics of distribution and reduce side effects of analogs of etomidate and benzodiazepines. Both classes of drugs have their principal sites of action on γ-aminobutyric acid type A receptors, although at very different binding sites and by different mechanisms of action. Herein, we review the structure of γ-aminobutyric acid type A receptors and describe the location of the 2 likely binding sites. In addition, we describe how these drugs can interact with the nervous system at a systems level. We leave it to other reviewers to discuss whether these new drugs offer true clinical improvements.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Anesthetics, Intravenous / adverse effects
  • Anesthetics, Intravenous / pharmacology*
  • Animals
  • Benzodiazepines / adverse effects
  • Benzodiazepines / pharmacology*
  • Binding Sites
  • Etomidate / adverse effects
  • Etomidate / analogs & derivatives
  • Etomidate / pharmacology*
  • GABA-A Receptor Agonists / adverse effects
  • GABA-A Receptor Agonists / pharmacology*
  • Humans
  • Hypnotics and Sedatives / adverse effects
  • Hypnotics and Sedatives / pharmacology*
  • Models, Molecular
  • Protein Conformation
  • Receptors, GABA-A / chemistry
  • Receptors, GABA-A / drug effects*
  • Receptors, GABA-A / metabolism
  • Synapses / drug effects*
  • Synapses / metabolism

Substances

  • Anesthetics, Intravenous
  • GABA-A Receptor Agonists
  • Hypnotics and Sedatives
  • Receptors, GABA-A
  • Benzodiazepines
  • remimazolam
  • Etomidate