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Interaction of anticonvulsants with the barbiturate-benzodiazpine-gaba receptor complex

Leeb-Lundberg, Frederik LU ; Snowman, Adele and Olsen, Richard W. (1981) In European Journal of Pharmacology 72(1). p.125-129
Abstract

Unlike the anesthetic barbiturate pentobarbital and the anxiolytic pyrazolopyridine etazolate, which enhance [3H]diazepam binding to rat brain membranes, the anticonvulsant barbiturates phenobarbital and metharbital, and also chlormethiazole, at therapeutic concentrations (10-1000 μM), do not stimulate [3H]diazepam binding, but instead block the enhancement by both pentobarbital and etazolate. The same anticonvulsants at similar concentrations inhibit [3H]α-dihydropicrotoxinin (DHP) binding, suggesting that these anticonvulsants compete for the same receptor sites as pentobarbital and etazolate, designated the barbiturate-picrotoxinin receptor component of the benzodiazepine-GABA receptor complex.

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author
; and
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Anesthetics, Anticonvulsants, Anxiolytics, Cl channels, γ-Aminobutyric acid
in
European Journal of Pharmacology
volume
72
issue
1
pages
125 - 129
publisher
Elsevier
external identifiers
  • pmid:6266847
  • scopus:0019430205
ISSN
0014-2999
DOI
10.1016/0014-2999(81)90309-5
language
English
LU publication?
no
id
c61c4696-68ad-4ed1-befd-a81ba1fea539
date added to LUP
2019-06-12 12:01:03
date last changed
2024-01-01 10:01:56
@article{c61c4696-68ad-4ed1-befd-a81ba1fea539,
  abstract     = {{<p>Unlike the anesthetic barbiturate pentobarbital and the anxiolytic pyrazolopyridine etazolate, which enhance [<sup>3</sup>H]diazepam binding to rat brain membranes, the anticonvulsant barbiturates phenobarbital and metharbital, and also chlormethiazole, at therapeutic concentrations (10-1000 μM), do not stimulate [<sup>3</sup>H]diazepam binding, but instead block the enhancement by both pentobarbital and etazolate. The same anticonvulsants at similar concentrations inhibit [<sup>3</sup>H]α-dihydropicrotoxinin (DHP) binding, suggesting that these anticonvulsants compete for the same receptor sites as pentobarbital and etazolate, designated the barbiturate-picrotoxinin receptor component of the benzodiazepine-GABA receptor complex.</p>}},
  author       = {{Leeb-Lundberg, Frederik and Snowman, Adele and Olsen, Richard W.}},
  issn         = {{0014-2999}},
  keywords     = {{Anesthetics; Anticonvulsants; Anxiolytics; Cl channels; γ-Aminobutyric acid}},
  language     = {{eng}},
  month        = {{06}},
  number       = {{1}},
  pages        = {{125--129}},
  publisher    = {{Elsevier}},
  series       = {{European Journal of Pharmacology}},
  title        = {{Interaction of anticonvulsants with the barbiturate-benzodiazpine-gaba receptor complex}},
  url          = {{http://dx.doi.org/10.1016/0014-2999(81)90309-5}},
  doi          = {{10.1016/0014-2999(81)90309-5}},
  volume       = {{72}},
  year         = {{1981}},
}