Cyclothiazide decreases [3H]AMPA binding to rat brain membranes: evidence that AMPA receptor desensitization increases agonist affinity
| Autor: | José Ambros-Ingerson, Markus Kessler, Alex Quan, Randy A. Hall, Gary Lynch |
|---|---|
| Předmět: |
Agonist
medicine.medical_specialty medicine.drug_class medicine.medical_treatment Sodium Chloride Symporter Inhibitors AMPA receptor Benzothiadiazines Tritium Radioligand Assay Internal medicine medicine Animals Receptors AMPA Receptor Diuretics Molecular Biology alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Desensitization (medicine) Membranes Liaison Chemistry General Neuroscience Glutamate receptor Temperature Brain Rats Endocrinology Membrane nervous system Solubility Biophysics Cyclothiazide Neurology (clinical) Developmental Biology medicine.drug |
| Zdroj: | Scopus-Elsevier |
| Popis: | The effects of cyclothiazide, a drug which blocks AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor desensitization, were tested on binding of [3HAMPA to rat brain membranes. Cyclothiazide reduced [3HAMPA binding by lowering the apparent affinity of the AMPA receptor. The magnitude of the decrease was temperature dependent and greater for membrane-bound than for solubilized receptors. These data provide evidence that desensitization increases the affinity of the AMPA receptor for agonists and indicate that a significant percentage of AMPA receptors in conventional equilibrium binding assays are in a desensitized state. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|