Article
Mutations affecting the glycine receptor agonist transduction mechanism convert the competitive antagonist, picrotoxin, into an allosteric potentiator.
The Journal of biological chemistry - 9 Jun 1995
Lynch J W, Rajendra S, Barry P H, Schofield P R
Abstract excerpt
Contrary to its effects on the gamma-aminobutyric acid type A receptor, picrotoxin antagonism of the alpha 1 subunit of the human glycine receptor is shown to be competitive, not use-dependent, and nonselective between the picrotoxin components, picrotin, and picrotoxinin. Competitive antagonism and non-use dependence are consistent with picrotoxin binding to a site in the extracellular domain. The mutations...
Topics
- Allosteric Regulation
- Dose-Response Relationship, Drug
- Humans
- Mutation
- Picrotoxin
- Receptors, Glycine
- Sesterterpenes
- Structure-Activity Relationship