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Effects of propofol on GABA(A) channel conductance in rat-cultured hippocampal neurons

Eghbali, M; Gage, PW and Birnir, Bryndis LU (2003) In European Journal of Pharmacology 468(2). p.75-82
Abstract
Channels were activated, in ripped-off patches from rat-cultured hippocampal neurons, by propofol alone, propofol plus 0.5 muM GABA (gamma-aminobutyric acid) or GABA alone. The propofol-activated currents were chloride-selective, showed outward-rectification and were enhanced by 1 muM diazepam. The maximum propofol-activated channel conductance increased with propofol concentration from less than 15 pS (10 muM) to about 60 pS (500 muM) but decreased to 40 pS in 1 mM propofol. Fitting the data from 10 to 500 muM propofol with a Hill-type equation gave a maximum conductance of 64 pS, an EC50 value of 32 muM and a Hill coefficient of 1.1. Addition of 0.5 muM GABA shifted the propofol EC50 value to 10 muM and increased the maximum channel... (More)
Channels were activated, in ripped-off patches from rat-cultured hippocampal neurons, by propofol alone, propofol plus 0.5 muM GABA (gamma-aminobutyric acid) or GABA alone. The propofol-activated currents were chloride-selective, showed outward-rectification and were enhanced by 1 muM diazepam. The maximum propofol-activated channel conductance increased with propofol concentration from less than 15 pS (10 muM) to about 60 pS (500 muM) but decreased to 40 pS in 1 mM propofol. Fitting the data from 10 to 500 muM propofol with a Hill-type equation gave a maximum conductance of 64 pS, an EC50 value of 32 muM and a Hill coefficient of 1.1. Addition of 0.5 muM GABA shifted the propofol EC50 value to 10 muM and increased the maximum channel conductance to about 100 pS. The Hill coefficient was 0.8. The maximum channel conductance did not increase further when 1 muM diazepam was added together with a saturating propofol concentration and GABA. The results are compared to effects other drugs have on GABA(A) channels conductance. (C) 2003 Elsevier Science B.V All rights reserved. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
benzodiazepine, anaesthetic, inhibition, receptor, extrasynaptic, GABA(A) receptor, GABA (gamma-aminobutyric acid)
in
European Journal of Pharmacology
volume
468
issue
2
pages
75 - 82
publisher
Elsevier
external identifiers
  • wos:000182964500001
  • scopus:0038058757
ISSN
1879-0712
DOI
10.1016/S0014-2999(03)01641-8
language
English
LU publication?
yes
id
0422b1b1-6e15-4a93-8a47-14fd0d6ac828 (old id 310616)
date added to LUP
2007-08-29 13:40:39
date last changed
2017-05-28 03:45:03
@article{0422b1b1-6e15-4a93-8a47-14fd0d6ac828,
  abstract     = {Channels were activated, in ripped-off patches from rat-cultured hippocampal neurons, by propofol alone, propofol plus 0.5 muM GABA (gamma-aminobutyric acid) or GABA alone. The propofol-activated currents were chloride-selective, showed outward-rectification and were enhanced by 1 muM diazepam. The maximum propofol-activated channel conductance increased with propofol concentration from less than 15 pS (10 muM) to about 60 pS (500 muM) but decreased to 40 pS in 1 mM propofol. Fitting the data from 10 to 500 muM propofol with a Hill-type equation gave a maximum conductance of 64 pS, an EC50 value of 32 muM and a Hill coefficient of 1.1. Addition of 0.5 muM GABA shifted the propofol EC50 value to 10 muM and increased the maximum channel conductance to about 100 pS. The Hill coefficient was 0.8. The maximum channel conductance did not increase further when 1 muM diazepam was added together with a saturating propofol concentration and GABA. The results are compared to effects other drugs have on GABA(A) channels conductance. (C) 2003 Elsevier Science B.V All rights reserved.},
  author       = {Eghbali, M and Gage, PW and Birnir, Bryndis},
  issn         = {1879-0712},
  keyword      = {benzodiazepine,anaesthetic,inhibition,receptor,extrasynaptic,GABA(A) receptor,GABA (gamma-aminobutyric acid)},
  language     = {eng},
  number       = {2},
  pages        = {75--82},
  publisher    = {Elsevier},
  series       = {European Journal of Pharmacology},
  title        = {Effects of propofol on GABA(A) channel conductance in rat-cultured hippocampal neurons},
  url          = {http://dx.doi.org/10.1016/S0014-2999(03)01641-8},
  volume       = {468},
  year         = {2003},
}