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          Institute: MPI für medizinische Forschung     Collection: Abteilung Molekulare Neurobiologie     Display Documents



ID: 22436.0, MPI für medizinische Forschung / Abteilung Molekulare Neurobiologie
Impact of β and γ variants on ligand binding properties of g-aminobutyric acidA receptors
Translation of Title:Impact of β and γ variants on ligand binding properties of g-aminobutyric acidA receptors
Authors:Lüddens, H.; Seeburg, Peter H.; Korpi, Esa R.
Language:English
Date of Publication (YYYY-MM-DD):1994-05
Title of Journal:Molecular Pharmacology
Journal Abbrev.:Mol. Pharmacol.
Volume:45
Issue / Number:5
Start Page:810
End Page:814
Review Status:Peer-review
Audience:Experts Only
Intended Educational Use:No
Abstract / Description:We expressed in cultured cells recombinant gamma-aminobutyric acid type A (GABAA) receptors of the subunit compositions alpha 1 beta j gamma k and alpha 5 beta j gamma k (j = 1, 2, or 3 and k = 2 or 3). A comparison of ligand-binding properties revealed a functional role for individual beta variants, which depended on the alpha subunit in the GABAA receptor. Recombinant alpha 5 beta x gamma 2/3 receptors recognized the cage convulsant t-butylbicyclophosphoro[35S]thionate, as well as the benzodiazepine (BZ) receptor inverse agonist [3H]Ro 15-4513, only with the beta 3 variant. In contrast, the exchange of beta variants in alpha 1 beta x gamma 2 receptors imparted differential modulation of t-butyl-bicyclophosphoro[35S]thionate binding by BZ receptor ligands. The BZ site of gamma 3-containing receptors was partially independent of the accompanying alpha and beta variants. alpha 1/5 beta 3 gamma 3 receptors were zolpidem insensitive but distinguished from alpha 5 beta 3 gamma 2 receptors by high affinity for the partial BZ receptor agonist CI 218,872. The distinct affinities of recombinant receptors for CI 218,872 suggested that the alpha 5 beta 3 gamma 2 receptor is the dominant zolpidem-insensitive GABAA receptor in the brain. Hence, alpha 5 beta 3 gamma 3 recpetors are not a major fraction of the native zolpidem-insensitive receptors, even though their genes are colocalized on mouse chromosome 7 and on human chromosome 15.
External Publication Status:published
Document Type:Article
Communicated by:Wulf Kaiser
Affiliations:MPI für medizinische Forschung/Abteilung Molekulare Neurobiologie/
Identifiers:URI:http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=... [Abstract]
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