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

S M O'Shea, L C Wong, N L Harrison
Author Information
  1. S M O'Shea: Department of Pharmacological and Physiological Sciences, University of Chicago, IL 60637, USA.

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.

Grants

  1. DA07255/NIDA NIH HHS
  2. GM00623/NIGMS NIH HHS
  3. GM45129/NIGMS NIH HHS

MeSH Term

Allosteric Regulation
Anesthetics, Intravenous
Cells, Cultured
Drug Synergism
GABA Agonists
GABA Modulators
Humans
Ion Channel Gating
Kidney
Ligands
Midazolam
Patch-Clamp Techniques
Piperidines
Propofol
Receptors, GABA-A

Chemicals

Anesthetics, Intravenous
GABA Agonists
GABA Modulators
Ligands
Piperidines
Receptors, GABA-A
piperidine-4-sulfonic acid
Midazolam
Propofol