title: Teaching an old GABA receptor new tricks.
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.
authors.affiliation: Department of Anesthesia, Stanford School of Medicine, 300 Pasteur Dr., Stanford, CA 94305-5117, USA. trudell@stanford.edu
authors.forename: James R
authors.initials: JR
authors.lastname: Trudell
authors.forename: Edward
authors.initials: E
authors.lastname: Bertaccini
authors.forename: M Bruce
authors.initials: MB
authors.lastname: Maciver
mesh_terms: D018686:Anesthetics, Intravenous / Q000009:adverse effects / Q000494:pharmacology*; D000818:Animals; D001569:Benzodiazepines / Q000009:adverse effects / Q000494:pharmacology*; D001665:Binding Sites; D005045:Etomidate / Q000009:adverse effects / Q000031:analogs & derivatives / Q000494:pharmacology*; D058785:GABA-A Receptor Agonists / Q000009:adverse effects / Q000494:pharmacology*; D006801:Humans; D006993:Hypnotics and Sedatives / Q000009:adverse effects / Q000494:pharmacology*; D008958:Models, Molecular; D011487:Protein Conformation; D011963:Receptors, GABA-A / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D013569:Synapses / Q000187:drug effects* / Q000378:metabolism
chemical_list: D018686:Anesthetics, Intravenous; D058785:GABA-A Receptor Agonists; D006993:Hypnotics and Sedatives; D011963:Receptors, GABA-A; D001569:Benzodiazepines; C522201:remimazolam; D005045:Etomidate