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Titolo:
The open channel blocking drug, IEM-1460, reveals functionally distinct alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptors in rat brain neurons
Autore:
Samoilova, MV; Buldakova, SL; Vorobjev, VS; Sharonova, IN; Magazanik, LG;
Indirizzi:
Russian Acad Sci, IM Sechenov Evolutionary Physiol & Biochem Inst, St Petersburg 196140, Russia Russian Acad Sci St Petersburg Russia 196140 t Petersburg 196140, Russia Russian Acad Med Sci, Brain Res Inst, Moscow, Russia Russian Acad Med SciMoscow Russia Sci, Brain Res Inst, Moscow, Russia
Titolo Testata:
NEUROSCIENCE
fascicolo: 1, volume: 94, anno: 1999,
pagine: 261 - 268
SICI:
0306-4522(1999)94:1<261:TOCBDI>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
CA2+-PERMEABLE AMPA RECEPTORS; CALCIUM-PERMEABLE AMPA; SUBUNIT MESSENGER-RNAS; HIPPOCAMPAL-NEURONS; KAINATE RECEPTORS; CA2+ PERMEABILITY; CEREBELLAR SLICES; PURKINJE-CELLS; BASAL GANGLIA; SPIDER TOXIN;
Keywords:
adamantane derivatives; native ionotropic glutamate receptors; non-competitive antagonism;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
44
Recensione:
Indirizzi per estratti:
Indirizzo: Samoilova, MV Russian Acad Sci, IM Sechenov Evolutionary Physiol & BiochemInst, St Petersburg 196140, Russia Russian Acad Sci St Petersburg Russia196140 96140, Russia
Citazione:
M.V. Samoilova et al., "The open channel blocking drug, IEM-1460, reveals functionally distinct alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptors in rat brain neurons", NEUROSCIENC, 94(1), 1999, pp. 261-268

Abstract

The properties of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptors were examined in various cell types isolated from young rat hippocampus, striatum and cerebellum using patch-clamp and fast application techniques. A dicationic adamantane derivative, IEM-1460, reversibly inhibited kainate-induced currents. In the presence of 100 mu M IEM-1460, kainatecurrents in striatal giant cholinergic interneurons and hippocampal non-pyramidal neurons were inhibited by 95% and 81%, respectively, at V-h= - 70 mV. Striatal GABAergic principal cells, hippocampal pyramidal neurons and cerebellar Purkinje cells had low sensitivity to IEM-1460 (inhibition by 4-15%). Analysis of averaged data from the cell types studied revealed a highlysignificant positive correlation (r=0.93, P < 0.01) between percentage inhibition by 100 mu M IEM-1460 and relative calcium permeability of AMPA receptors, P-Ca/P-Na. Also, within each brain structure, the sensitivity of IEM-1460 block was lower the stronger the outward rectification of kainate currents. Some hippocampal neurons exhibited intermediate sensitivity to IEM-1460. Kainate currents were suppressed by 40% in the presence of 100 mu M IEM-1460. Meanwhile, AMPA receptors in this cell type had low calcium permeability (P-Ca/P-Na = 0.13) and demonstrated outwardly rectifying kainate currents. The interrelation of different properties of AMPA receptors considering their assembly is discussed. The data obtained suggest that IEM-1460 may be a convenient and promising marker of native AMPA receptor assembly: it selectively inhibits Ca2+-permeable, GluR2-1acking AMPA receptors. (C) 1999 IBRO. Published by Elsevier Science Ltd.

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Documento generato il 06/04/20 alle ore 02:14:24