| pubmed-article:15834439 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15834439 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
| pubmed-article:15834439 | lifeskim:mentions | umls-concept:C1524059 | lld:lifeskim |
| pubmed-article:15834439 | lifeskim:mentions | umls-concept:C0031327 | lld:lifeskim |
| pubmed-article:15834439 | lifeskim:mentions | umls-concept:C0001392 | lld:lifeskim |
| pubmed-article:15834439 | lifeskim:mentions | umls-concept:C0061465 | lld:lifeskim |
| pubmed-article:15834439 | lifeskim:mentions | umls-concept:C1527240 | lld:lifeskim |
| pubmed-article:15834439 | lifeskim:mentions | umls-concept:C0671540 | lld:lifeskim |
| pubmed-article:15834439 | pubmed:issue | 5 | lld:pubmed |
| pubmed-article:15834439 | pubmed:dateCreated | 2005-7-1 | lld:pubmed |
| pubmed-article:15834439 | pubmed:abstractText | 1. Antagonizing glutamatergic neurotransmission by blockade of AMPA-type glutamate receptors (GluR) is a promising pharmacological strategy for neuroprotection in neurodegenerative diseases and acute treatment of stroke. 2. We investigated the interaction of the adamantane derivative IEM-1460 with human wild-type and mutant AMPA-type GluR channels. Different recombinant homooligomeric human AMPA-type GluR channels and a rat nondesensitizing mutant GluR (GluR2 L504Y) channel were expressed in HEK293 cells and investigated using the patch-clamp technique in combination with ultrafast agonist application. 3. When IEM-1460 was coapplied with glutamate, an open channel block mechanism was observed at slow desensitizing GluR2 flip (>/=0.1 mM IEM-1460) and nondesensitizing GluR2 L504Y channels (>/=1 microM IEM-1460). 4. A competitive block of AMPA-type channels was observed with IC(50) values for the dose block curves of 0.1 mM IEM-1460 at human unmutated and 10 microM IEM-1460 at mutant GluR channels. 5. Nondesensitizing GluR2 L504Y channels were used to further characterize the block mechanism. After equilibration with the agonist, a current decay upon coapplication of glutamate and IEM-1460 was observed. The recovery from block was independent of the glutamate and IEM-1460 concentration. The extent of current inhibition as well as the time constant of current decay upon addition of the blocker to the test solution were dependent on agonist concentration; this strongly points to an additional competitive-like block mechanism of IEM-1460 at human AMPA-type GluR channels. 6. The data were interpreted in the frame of a molecular scheme with two binding sites of IEM-1460 at the receptor, one at the unliganded resting and the other at the fully liganded open state of the channels. | lld:pubmed |
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| pubmed-article:15834439 | pubmed:language | eng | lld:pubmed |
| pubmed-article:15834439 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15834439 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:15834439 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:15834439 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15834439 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:15834439 | pubmed:issn | 0007-1188 | lld:pubmed |
| pubmed-article:15834439 | pubmed:author | pubmed-author:KrampflKlausK | lld:pubmed |
| pubmed-article:15834439 | pubmed:author | pubmed-author:BuflerJohanne... | lld:pubmed |
| pubmed-article:15834439 | pubmed:author | pubmed-author:SchlesingerFr... | lld:pubmed |
| pubmed-article:15834439 | pubmed:author | pubmed-author:TammenaDerkD | lld:pubmed |
| pubmed-article:15834439 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15834439 | pubmed:volume | 145 | lld:pubmed |
| pubmed-article:15834439 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15834439 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15834439 | pubmed:pagination | 656-63 | lld:pubmed |
| pubmed-article:15834439 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:meshHeading | pubmed-meshheading:15834439... | lld:pubmed |
| pubmed-article:15834439 | pubmed:year | 2005 | lld:pubmed |
| pubmed-article:15834439 | pubmed:articleTitle | Two mechanisms of action of the adamantane derivative IEM-1460 at human AMPA-type glutamate receptors. | lld:pubmed |
| pubmed-article:15834439 | pubmed:affiliation | Neurological Department of the Medical School of Hannover, Karl-Neuberg Str. 1, 30623 Hannover, Germany. Schlesinger.Friedrich@mh-hannover.de | lld:pubmed |
| pubmed-article:15834439 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:15834439 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:15834439 | lld:pubmed |
