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Gating effects on picrotin block of glycine receptors.
- Source :
-
Neuroreport [Neuroreport] 2012 Dec 05; Vol. 23 (17), pp. 1017-20. - Publication Year :
- 2012
-
Abstract
- Picrotoxin is a pore blocker that can differentiate ligand-gated inhibitory chloride channels. Even within one receptor type, such as the glycine receptor, picrotoxin block differs between subunits. The effect of subunit gating properties on block of the inhibitory glycine receptor (GlyR) was explored using heteromeric α subunit expression in voltage-clamped HEK293 cells. The α2 GlyR is more sensitive to picrotin block than the α1 GlyR, and this difference was used to explore whether mutations that interfered with gating of the α2 subunit would also interfere with picrotin block. Two mutations were used: one that decreased the glycine sensitivity of α2 by almost two log units and the other that was unresponsive to glycine. In both cases, the sensitivity to picrotin was essentially unaltered. The results indicated that α2 subunits can determine the picrotin sensitivity of α1α2-heteromeric receptors and that direct gating of the α2 subunit is not required for this picrotin inhibition.
- Subjects :
- Amino Acid Substitution
Animals
Arginine chemistry
Chloride Channels antagonists & inhibitors
Dimerization
Dose-Response Relationship, Drug
HEK293 Cells
Humans
Inhibitory Concentration 50
Lysine chemistry
Mutation, Missense
Patch-Clamp Techniques
Picrotoxin pharmacology
Point Mutation
Protein Structure, Tertiary
Rats
Receptors, Glycine chemistry
Receptors, Glycine genetics
Receptors, Glycine physiology
Recombinant Fusion Proteins antagonists & inhibitors
Recombinant Fusion Proteins chemistry
Recombinant Fusion Proteins physiology
Sesterterpenes
Transfection
Chlorides metabolism
Glycine metabolism
Ion Channel Gating drug effects
Picrotoxin analogs & derivatives
Receptors, Glycine antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1473-558X
- Volume :
- 23
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- Neuroreport
- Publication Type :
- Academic Journal
- Accession number :
- 23079787
- Full Text :
- https://doi.org/10.1097/WNR.0b013e32835a8629