Literature DB >> 10678761

Propofol increases agonist efficacy at the GABA(A) receptor.

S M O'Shea1, L C Wong, N L Harrison.   

Abstract

Using the whole-cell patch-clamp technique, we have determined that propofol, but not midazolam, increases the efficacy of piperidine-4-sulphonic acid (P4S), a partial agonist at alpha1beta1gamma2s, GABA(A) receptors expressed in HEK 293 cells. These findings are consistent with the idea that propofol facilitates receptor gating, while midazolam increases receptor occupancy by the agonist.

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Year:  2000        PMID： 10678761     DOI： 10.1016/s0006-8993(99)02151-4

Source DB:  PubMed          Journal:  Brain Res        ISSN： 0006-8993            Impact factor:   3.252


  12 in total

1.  Agonist-specific conformational changes in the α1-γ2 subunit interface of the GABA A receptor.

Authors:  Megan M Eaton; You Bin Lim; John Bracamontes; Joe Henry Steinbach; Gustav Akk
Journal:  Mol Pharmacol       Date:  2012-05-09       Impact factor: 4.436

2.  Inverse effects on gating and modulation caused by a mutation in the M2-M3 Linker of the GABA(A) receptor gamma subunit.

Authors:  Sean M O'Shea; Carrie A Williams; Andrew Jenkins
Journal:  Mol Pharmacol       Date:  2009-06-24       Impact factor: 4.436

3.  Analysis of GABAA Receptor Activation by Combinations of Agonists Acting at the Same or Distinct Binding Sites.

Authors:  Daniel J Shin; Allison L Germann; Douglas F Covey; Joe Henry Steinbach; Gustav Akk
Journal:  Mol Pharmacol       Date:  2018-10-18       Impact factor: 4.436

4.  Additivities of compounds that increase the numbers of high affinity [3H]muscimol binding sites by different amounts define more than 9 GABA(A) receptor complexes in rat forebrain: implications for schizophrenia and clozapine research.

Authors:  R F Squires; E Saederup
Journal:  Neurochem Res       Date:  2000-12       Impact factor: 3.996

5.  Structure and dynamics of the GABA binding pocket: A narrowing cleft that constricts during activation.

Authors:  D A Wagner; C Czajkowski
Journal:  J Neurosci       Date:  2001-01-01       Impact factor: 6.167

6.  An allosteric coagonist model for propofol effects on α1β2γ2L γ-aminobutyric acid type A receptors.

Authors:  Dirk Ruesch; Elena Neumann; Hinnerk Wulf; Stuart A Forman
Journal:  Anesthesiology       Date:  2012-01       Impact factor: 7.892

Review 7.  Anesthetic sites and allosteric mechanisms of action on Cys-loop ligand-gated ion channels.

Authors:  Stuart A Forman; Keith W Miller
Journal:  Can J Anaesth       Date:  2011-01-07       Impact factor: 5.063

8.  Endogenous gamma-aminobutyric acid modulates tonic guinea pig airway tone and propofol-induced airway smooth muscle relaxation.

Authors:  George Gallos; Neil R Gleason; Laszlo Virag; Yi Zhang; Kentaro Mizuta; Robert A Whittington; Charles W Emala
Journal:  Anesthesiology       Date:  2009-04       Impact factor: 7.892

9.  The benzodiazepine diazepam potentiates responses of α1β2γ2L γ-aminobutyric acid type A receptors activated by either γ-aminobutyric acid or allosteric agonists.

Authors:  Ping Li; Megan M Eaton; Joe Henry Steinbach; Gustav Akk
Journal:  Anesthesiology       Date:  2013-06       Impact factor: 7.892

10.  Thalamic reticular nucleus induces fast and local modulation of arousal state.

Authors:  Laura D Lewis; Jakob Voigts; Francisco J Flores; L Ian Schmitt; Matthew A Wilson; Michael M Halassa; Emery N Brown
Journal:  Elife       Date:  2015-10-13       Impact factor: 8.140
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