Literature DB >> 22344244

Teaching an old GABA receptor new tricks.

James R Trudell1, Edward Bertaccini, M Bruce Maciver.   

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.

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Year:  2012        PMID: 22344244      PMCID: PMC4444214          DOI: 10.1213/ANE.0b013e31824a0b3c

Source DB:  PubMed          Journal:  Anesth Analg        ISSN: 0003-2999            Impact factor:   5.108


  26 in total

1.  A placebo- and midazolam-controlled phase I single ascending-dose study evaluating the safety, pharmacokinetics, and pharmacodynamics of remimazolam (CNS 7056): Part II. Population pharmacokinetic and pharmacodynamic modeling and simulation.

Authors:  Hugh R Wiltshire; Gavin J Kilpatrick; Gary S Tilbrook; Keith M Borkett
Journal:  Anesth Analg       Date:  2012-01-16       Impact factor: 5.108

Review 2.  Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes.

Authors:  Uwe Rudolph; Frédéric Knoflach
Journal:  Nat Rev Drug Discov       Date:  2011-07-29       Impact factor: 84.694

3.  Alpha5GABAA receptors mediate the amnestic but not sedative-hypnotic effects of the general anesthetic etomidate.

Authors:  Victor Y Cheng; Loren J Martin; Erin M Elliott; John H Kim; Howard T J Mount; Franco A Taverna; John C Roder; John F Macdonald; Amit Bhambri; Neil Collinson; Keith A Wafford; Beverley A Orser
Journal:  J Neurosci       Date:  2006-04-05       Impact factor: 6.167

4.  Microsecond simulations indicate that ethanol binds between subunits and could stabilize an open-state model of a glycine receptor.

Authors:  Samuel Murail; Björn Wallner; James R Trudell; Edward Bertaccini; Erik Lindahl
Journal:  Biophys J       Date:  2011-04-06       Impact factor: 4.033

5.  Stereoselective effects of etomidate optical isomers on gamma-aminobutyric acid type A receptors and animals.

Authors:  S L Tomlin; A Jenkins; W R Lieb; N P Franks
Journal:  Anesthesiology       Date:  1998-03       Impact factor: 7.892

6.  Anesthetics affect the uptake but not the depolarization-evoked release of GABA in rat striatal synaptosomes.

Authors:  J Mantz; J B Lecharny; V Laudenbach; D Henzel; G Peytavin; J M Desmonts
Journal:  Anesthesiology       Date:  1995-02       Impact factor: 7.892

7.  The in vitro and in vivo enantioselectivity of etomidate implicates the GABAA receptor in general anaesthesia.

Authors:  Delia Belelli; Anna-Lisa Muntoni; Simon D Merrywest; Luc J Gentet; Anna Casula; Helen Callachan; Paola Madau; David K Gemmell; Niall M Hamilton; Jeremy J Lambert; Keith T Sillar; John A Peters
Journal:  Neuropharmacology       Date:  2003-07       Impact factor: 5.250

8.  Anesthetics discriminate between tonic and phasic gamma-aminobutyric acid receptors on hippocampal CA1 neurons.

Authors:  Mark C Bieda; Henry Su; M Bruce Maciver
Journal:  Anesth Analg       Date:  2009-02       Impact factor: 5.108

9.  Amnestic concentrations of etomidate modulate GABAA,slow synaptic inhibition in hippocampus.

Authors:  Shuiping Dai; Misha Perouansky; Robert A Pearce
Journal:  Anesthesiology       Date:  2009-10       Impact factor: 7.892

Review 10.  Anxiety over GABA(A) receptor structure relieved by AChBP.

Authors:  Brett A Cromer; Craig J Morton; Michael W Parker
Journal:  Trends Biochem Sci       Date:  2002-06       Impact factor: 13.807

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  4 in total

1.  GABA(A) receptor transmembrane amino acids are critical for alcohol action: disulfide cross-linking and alkyl methanethiosulfonate labeling reveal relative location of binding sites.

Authors:  Cecilia M Borghese; Jessica A Hicks; Daniel J Lapid; James R Trudell; R Adron Harris
Journal:  J Neurochem       Date:  2013-10-28       Impact factor: 5.372

Review 2.  Alcohol dependence: molecular and behavioral evidence.

Authors:  James R Trudell; Robert O Messing; Jody Mayfield; R Adron Harris
Journal:  Trends Pharmacol Sci       Date:  2014-05-25       Impact factor: 14.819

3.  Anesthetic agent-specific effects on synaptic inhibition.

Authors:  M Bruce MacIver
Journal:  Anesth Analg       Date:  2014-09       Impact factor: 5.108

Review 4.  The role of anesthetic drugs in liver apoptosis.

Authors:  Ali Dabbagh; Samira Rajaei
Journal:  Hepat Mon       Date:  2013-08-25       Impact factor: 0.660

  4 in total

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