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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1-2
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pubmed:dateCreated |
1992-12-18
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pubmed:abstractText |
Receptor binding assays have shown that diaminodecane (DA-10) reduced binding of open channel blockers to the N-methyl-D-aspartate (NMDA) subtype of postsynaptic glutamate receptor through an interaction with the polyamine regulatory site. Because the action of DA-10 was opposite to that of the polyamine agonist spermine and was reversed by polyamine antagonists, DA-10 has been classified as an inverse agonist at the polyamine site. Using whole-cell voltage-clamp and single-channel recordings from cultured rat cortical neurons, we show that at negative holding potentials DA-10 (1-300 microM) reduced NMDA receptor whole cell current (IC50 = 34 microM) and produced a flickery block of NMDA single-channel currents. The flickery block of NMDA single channels was voltage-dependent and not reversed by the polyamine antagonist diethylenetriamine (DET). Potential mechanisms for the flickery block of NMDA single channel currents are discussed.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0304-3940
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
144
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
111-5
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:1279482-Animals,
pubmed-meshheading:1279482-Diamines,
pubmed-meshheading:1279482-Female,
pubmed-meshheading:1279482-Ion Channels,
pubmed-meshheading:1279482-Kinetics,
pubmed-meshheading:1279482-N-Methylaspartate,
pubmed-meshheading:1279482-Neurons,
pubmed-meshheading:1279482-Oocytes,
pubmed-meshheading:1279482-Polyamines,
pubmed-meshheading:1279482-Pregnancy,
pubmed-meshheading:1279482-Rats,
pubmed-meshheading:1279482-Receptors, N-Methyl-D-Aspartate,
pubmed-meshheading:1279482-Spermine
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pubmed:year |
1992
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pubmed:articleTitle |
The polyamine diaminodecane (DA-10) produces a voltage-dependent flickery block of single NMDA receptor channels.
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pubmed:affiliation |
Neuroscience Program, University of Michigan, Ann Arbor.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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