Article
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
Journal of medicinal chemistry - 23 Dec 1994
Wieland H A, Lüddens H
Abstract excerpt
Benzodiazepines (BZ) exert their effects through GABAA receptors, which belong to the superfamily of ligand-gated ion channels. Coexpression of recombinant alpha, beta, and gamma subunits in a cell culture system mimics the BZ binding sites. The alpha variants largely determine the nature of the BZ binding site in such alpha i beta j gamma k heteromultimers (i = 1-6; j = 1-3; k = 1-3). Notably, the alpha 1 and...
Topics
- Amino Acid Sequence
- Azides
- Base Sequence
- Benzodiazepines
- Binding Sites
- Diazepam
- GABA Agonists
- Humans
- Molecular Sequence Data
- Mutation
- Receptors, GABA-A