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Block of open channels of recombinant AMPA receptors and native AMPA/kainate receptors by adamantane derivatives.
Magazanik LG
,
Buldakova SL
,
Samoilova MV
,
Gmiro VE
,
Mellor IR
,
Usherwood PN
.
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1. The effects of two adamantane derivatives, 1-trimethylammonio-5-(1-adamantane-methyl-ammoniopentane dibromide) (IEM-1460) and 1-ammonio-5-(1-adamantane-methylammoniopentane dibromide) (IEM-1754) on kainate-induced currents were studied in Xenopus oocytes expressing recombinant ionotropic glutamate receptors and in freshly isolated neurones from rat hippocampal slices. 2. The adamantane derivatives caused use- and voltage-dependent block of open channels of recombinant AMPA receptors. This antagonism was dependent on receptor subunit composition; channels gated by recombinant, homomeric GluR1 and GluR3 receptors exhibited a higher sensitivity to block than those gated by receptors containing edited GluR2 subunits. In the former cases, IEM-1460 had an IC50 of 1.6 microM at a holding potential (Vh) of -80 mV and IEM-1754 was 3.8 times less potent than IEM-1460. In contrast, 100 microM IEM-1460 inhibited responses to 100 microM kainate of receptors containing edited GluR2 subunits by only 7.8 +/- 2.4% (n = 5 oocytes at a Vh of -80 mV. 3. Native AMPA/kainate receptors in isolated hippocampal cells were inhibited by adamantane derivatives in a use- and voltage-dependent manner. This antagonism was dependent on cell type: pyramidal neurones were less sensitive to IEM-1460 (IC50 = 1617 microM at Vh = -80 mV) than interneurones (IC50 = 1.6 microM at Vh = -80 mV). IEM-1460 and IEM-1754 were equipotent when applied to pyramidal neurones, but IEM-1754 was less potent (approximately 3 times) than IEM-1460 when applied to interneurones. 4. It is concluded that the presence of the edited GluR2 subunit in recombinant AMPA receptors and native AMPA/kainate receptors inhibits channel block by organic cations and that adamantane derivatives are potentially valuable tools for identifying classes of AMPA/kainate receptors and their roles in synaptic transmission.
Antonov,
Argiopine blocks glutamate-activated single-channel currents on crayfish muscle by two mechanisms.
1989, Pubmed
Antonov,
Argiopine blocks glutamate-activated single-channel currents on crayfish muscle by two mechanisms.
1989,
Pubmed
Antonov,
Novel adamantane derivatives act as blockers of open ligand-gated channels and as anticonvulsants.
1995,
Pubmed
Blaschke,
A single amino acid determines the subunit-specific spider toxin block of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor channels.
1993,
Pubmed
,
Xenbase
Bochet,
Subunit composition at the single-cell level explains functional properties of a glutamate-gated channel.
1994,
Pubmed
Brackley,
Selective antagonism of native and cloned kainate and NMDA receptors by polyamine-containing toxins.
1993,
Pubmed
,
Xenbase
Burnashev,
Divalent ion permeability of AMPA receptor channels is dominated by the edited form of a single subunit.
1992,
Pubmed
Clark,
Block of locust muscle glutamate receptors by delta-philanthotoxin occurs after receptor activations.
1982,
Pubmed
Dingledine,
Structural determinants of barium permeation and rectification in non-NMDA glutamate receptor channels.
1992,
Pubmed
,
Xenbase
Geiger,
Relative abundance of subunit mRNAs determines gating and Ca2+ permeability of AMPA receptors in principal neurons and interneurons in rat CNS.
1995,
Pubmed
Green,
Polyamine amides are neuroprotective in cerebellar granule cell cultures challenged with excitatory amino acids.
1996,
Pubmed
Götz,
Functional properties of AMPA and NMDA receptors expressed in identified types of basal ganglia neurons.
1997,
Pubmed
Hollmann,
Cloned glutamate receptors.
1994,
Pubmed
Hume,
Identification of a site in glutamate receptor subunits that controls calcium permeability.
1991,
Pubmed
,
Xenbase
Iino,
Permeation of calcium through excitatory amino acid receptor channels in cultured rat hippocampal neurones.
1990,
Pubmed
Iino,
Voltage-dependent blockage of Ca(2+)-permeable AMPA receptors by joro spider toxin in cultured rat hippocampal neurones.
1996,
Pubmed
Isa,
Distribution of neurones expressing inwardly rectifying and Ca(2+)-permeable AMPA receptors in rat hippocampal slices.
1996,
Pubmed
Isa,
Spermine mediates inward rectification of Ca(2+)-permeable AMPA receptor channels.
1995,
Pubmed
Jonas,
Differences in Ca2+ permeability of AMPA-type glutamate receptor channels in neocortical neurons caused by differential GluR-B subunit expression.
1994,
Pubmed
Jonas,
Molecular mechanisms controlling calcium entry through AMPA-type glutamate receptor channels.
1995,
Pubmed
Kerry,
Single channel studies of non-competitive antagonism of a quisqualate-sensitive glutamate receptor by argiotoxin636--a fraction isolated from orb-web spider venom.
1988,
Pubmed
Koh,
Ca(2+)-permeable AMPA and NMDA receptor channels in basket cells of rat hippocampal dentate gyrus.
1995,
Pubmed
Koh,
Block of native Ca(2+)-permeable AMPA receptors in rat brain by intracellular polyamines generates double rectification.
1995,
Pubmed
Köhler,
Determinants of Ca2+ permeability in both TM1 and TM2 of high affinity kainate receptor channels: diversity by RNA editing.
1993,
Pubmed
Leranth,
AMPA receptors in the rat and primate hippocampus: a possible absence of GluR2/3 subunits in most interneurons.
1996,
Pubmed
McBain,
Heterogeneity of synaptic glutamate receptors on CA3 stratum radiatum interneurones of rat hippocampus.
1993,
Pubmed
Neely,
Trapping of an open-channel blocker at the frog neuromuscular acetylcholine channel.
1986,
Pubmed
Petralia,
Light and electron immunocytochemical localization of AMPA-selective glutamate receptors in the rat brain.
1992,
Pubmed
Randle,
Tetrabutylammonium induces a voltage-dependent block of kainate current in Xenopus oocytes injected with rat brain mRNA.
1990,
Pubmed
,
Xenbase
Sudan,
The action of philanthotoxin-343 and photolabile analogues on locust (Schistocerca gregaria) muscle.
1995,
Pubmed
Tsubokawa,
Ca(2+)-dependent non-NMDA receptor-mediated synaptic currents in ischemic CA1 hippocampal neurons.
1994,
Pubmed
Vorobjev,
Vibrodissociation of sliced mammalian nervous tissue.
1991,
Pubmed
Vorobjev,
A simple perfusion system for patch-clamp studies.
1996,
Pubmed
Wenthold,
Evidence for multiple AMPA receptor complexes in hippocampal CA1/CA2 neurons.
1996,
Pubmed
Wisden,
Mammalian ionotropic glutamate receptors.
1993,
Pubmed
