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ACS Chem Neurosci
2010 Mar 17;13:175-181. doi: 10.1021/cn900037c.
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Kaitocephalin antagonism of glutamate receptors expressed in Xenopus oocytes.
Limon A
,
Reyes-Ruiz JM
,
Vaswani RG
,
Chamberlin AR
,
Miledi R
.
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Kaitocephalin is the first discovered natural toxin with protective properties against excitotoxic-death of cultured neurons induced by N-methyl-d-aspartate (NMDA) or alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA)/kainic acid (kainate, KA) receptors. Nevertheless, the effects of kaitocephalin on the function of these receptors were unknown. In this work we report some pharmacological properties of synthetic (-)-kaitocephalin on rat brain glutamate receptors expressed in Xenopus laevis oocytes and, on the homomeric AMPA-type GluR3 and KA-type GluR6 receptors. Kaitocephalin was found to be a more potent antagonist of NMDA receptors (IC(50) = 75 +/- 9 nM) than of AMPA receptors from cerebral cortex (IC(50) = 242 +/- 37 nM) and from homomeric GluR3 subunits (IC(50) = 502 +/- 55 nM). Moreover, kaitocephalin is a weak antagonist of the KA-type receptor GluR6 (IC(50) ~ 100 muM) and of metabotropic (IC(50) > 100 muM) glutamate receptors expressed by rat brain mRNA.
Bleakman,
Pharmacological discrimination of GluR5 and GluR6 kainate receptor subtypes by (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahyd roisdoquinoline-3 carboxylic-acid.
1996, Pubmed
Bleakman,
Pharmacological discrimination of GluR5 and GluR6 kainate receptor subtypes by (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahyd roisdoquinoline-3 carboxylic-acid.
1996,
Pubmed
Carpenter,
Messenger RNAs coding for receptors and channels in the cerebral cortex of adult and aged rats.
1992,
Pubmed
,
Xenbase
Casabona,
Expression and coupling to polyphosphoinositide hydrolysis of group I metabotropic glutamate receptors in early postnatal and adult rat brain.
1997,
Pubmed
Chen,
The chemical biology of clinically tolerated NMDA receptor antagonists.
2006,
Pubmed
Cull-Candy,
Role of distinct NMDA receptor subtypes at central synapses.
2004,
Pubmed
D'Antoni,
Metabotropic glutamate receptors in glial cells.
2008,
Pubmed
Dingledine,
The glutamate receptor ion channels.
1999,
Pubmed
Egebjerg,
Cloning of a cDNA for a glutamate receptor subunit activated by kainate but not AMPA.
1991,
Pubmed
,
Xenbase
Everts,
Lectin-induced inhibition of desensitization of the kainate receptor GluR6 depends on the activation state and can be mediated by a single native or ectopic N-linked carbohydrate side chain.
1999,
Pubmed
,
Xenbase
Fagni,
Identification and functional roles of metabotropic glutamate receptor-interacting proteins.
2004,
Pubmed
Ferraguti,
Metabotropic glutamate receptors.
2006,
Pubmed
Fucile,
Effects of cyclothiazide on GluR1/AMPA receptors.
2006,
Pubmed
GADDUM,
Quantitative studies of antagonists for 5-hydroxytryptamine.
1955,
Pubmed
Gundersen,
Glutamate and kainate receptors induced by rat brain messenger RNA in Xenopus oocytes.
1984,
Pubmed
,
Xenbase
Hollmann,
Ca2+ permeability of KA-AMPA--gated glutamate receptor channels depends on subunit composition.
1991,
Pubmed
,
Xenbase
Horikoshi,
Regional distribution of metabotropic glutamate response in the rat brain using Xenopus oocytes.
1989,
Pubmed
,
Xenbase
Kalia,
NMDA receptors in clinical neurology: excitatory times ahead.
2008,
Pubmed
Limon,
Properties of GluR3 receptors tagged with GFP at the amino or carboxyl terminus.
2007,
Pubmed
,
Xenbase
Manahan-Vaughan,
A single application of MK801 causes symptoms of acute psychosis, deficits in spatial memory, and impairment of synaptic plasticity in rats.
2008,
Pubmed
Miledi,
Properties of acetylcholine receptors translated by cat muscle mRNA in Xenopus oocytes.
1982,
Pubmed
,
Xenbase
Miledi,
A calcium-dependent transient outward current in Xenopus laevis oocytes.
1982,
Pubmed
,
Xenbase
Monyer,
Developmental and regional expression in the rat brain and functional properties of four NMDA receptors.
1994,
Pubmed
Parker,
Changes in intracellular calcium and in membrane currents evoked by injection of inositol trisphosphate into Xenopus oocytes.
1986,
Pubmed
,
Xenbase
Ragsdale,
Inhibition of rat brain glutamate receptors by philanthotoxin.
1989,
Pubmed
,
Xenbase
Randle,
Competitive inhibition by NBQX of kainate/AMPA receptor currents and excitatory synaptic potentials: importance of 6-nitro substitution.
1992,
Pubmed
,
Xenbase
Schwartz,
Protective autoimmunity against the enemy within: fighting glutamate toxicity.
2003,
Pubmed
Shepherd,
The cell biology of synaptic plasticity: AMPA receptor trafficking.
2007,
Pubmed
Shin-Ya,
Novel antitumor and neuroprotective substances discovered by characteristic screenings based on specific molecular targets.
2005,
Pubmed
Strange,
Functional characterisation of homomeric ionotropic glutamate receptors GluR1-GluR6 in a fluorescence-based high throughput screening assay.
2006,
Pubmed
,
Xenbase
Vaswani,
Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-kaitocephalin.
2009,
Pubmed
Vaswani,
Stereocontrolled total synthesis of (--)-kaitocephalin.
2008,
Pubmed
Verdoorn,
N-methyl-D-aspartate/glycine and quisqualate/kainate receptors expressed in Xenopus oocytes: antagonist pharmacology.
1989,
Pubmed
,
Xenbase
Villmann,
On the hypes and falls in neuroprotection: targeting the NMDA receptor.
2007,
Pubmed
Wong,
The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist.
1986,
Pubmed
