doi: 10.1016/0006-8993(93)90978-v.
Cyclothiazide decreases [3H]AMPA binding to rat brain membranes: evidence that AMPA receptor desensitization increases agonist affinity
Affiliations
- PMID: 7508813
- DOI: 10.1016/0006-8993(93)90978-v
Item in Clipboard
Cyclothiazide decreases [3H]AMPA binding to rat brain membranes: evidence that AMPA receptor desensitization increases agonist affinity
Brain Res.
.
Abstract
The effects of cyclothiazide, a drug which blocks AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor desensitization, were tested on binding of [3H]AMPA to rat brain membranes. Cyclothiazide reduced [3H]AMPA 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.
Similar articles
-
Cyclothiazide and AMPA receptor desensitization: analyses from studies of AMPA-induced release of [3H]-noradrenaline from hippocampal slices.Br J Pharmacol. 1998 Feb;123(3):473-80. doi: 10.1038/sj.bjp.0701638. Br J Pharmacol. 1998. PMID: 9504388 Free PMC article.
-
Pharmacological characterization of the human ionotropic glutamate receptor subtype GluR3 stably expressed in mammalian cells.J Pharmacol Exp Ther. 1998 Apr;285(1):358-70. J Pharmacol Exp Ther. 1998. PMID: 9536032
-
Effect of cyclothiazide on binding properties of AMPA-type glutamate receptors: lack of competition between cyclothiazide and GYKI 52466.Mol Pharmacol. 1996 Jan;49(1):123-31. Mol Pharmacol. 1996. PMID: 8569697
-
Stable expression of recombinant AMPA receptor subunits: binding affinities and effects of allosteric modulators.J Neurochem. 1997 Jun;68(6):2424-34. doi: 10.1046/j.1471-4159.1997.68062424.x. J Neurochem. 1997. PMID: 9166736
-
In search of novel AMPA potentiators.Recent Pat CNS Drug Discov. 2006 Nov;1(3):239-46. doi: 10.2174/157488906778773661. Recent Pat CNS Drug Discov. 2006. PMID: 18221205 Review.
Cited by
-
Synaptic excitation mediated by AMPA receptors in rat cerebellar slices is selectively enhanced by aniracetam and cyclothiazide.Neurochem Res. 1995 May;20(5):605-9. doi: 10.1007/BF01694543. Neurochem Res. 1995. PMID: 7643966
-
Ultraviolet radiation, thiol reagents, and solubilization enhance AMPA receptor binding affinity via a common mechanism.Neurochem Res. 1996 Aug;21(8):963-8. doi: 10.1007/BF02532347. Neurochem Res. 1996. PMID: 8895851
-
The regulation of AMPA receptor-binding sites.Mol Neurobiol. 1998 Winter;17(1-3):33-58. doi: 10.1007/BF02802023. Mol Neurobiol. 1998. PMID: 9887445 Review.
-
Interactions of 2,3-benzodiazepines and cyclothiazide at AMPA receptors: patch clamp recordings in cultured neurones and area CA1 in hippocampal slices.Br J Pharmacol. 1996 Mar;117(6):1209-21. doi: 10.1111/j.1476-5381.1996.tb16718.x. Br J Pharmacol. 1996. PMID: 8882618 Free PMC article.
-
Modulation of agonist binding to AMPA receptors by 1-(1,4-benzodioxan-6-ylcarbonyl)piperidine (CX546): differential effects across brain regions and GluA1-4/transmembrane AMPA receptor regulatory protein combinations.J Pharmacol Exp Ther. 2009 Dec;331(3):965-74. doi: 10.1124/jpet.109.158014. Epub 2009 Aug 28. J Pharmacol Exp Ther. 2009. PMID: 19717789 Free PMC article.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
