Interaction of anticonvulsants with the barbiturate-benzodiazpine-gaba receptor complex
(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.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/c61c4696-68ad-4ed1-befd-a81ba1fea539
- author
- Leeb-Lundberg, Frederik LU ; Snowman, Adele and Olsen, Richard W.
- publishing date
- 1981-06-10
- 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}}, }