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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
1996-7-1
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pubmed:abstractText |
A 45Ca2+ influx assay has been used to investigate the pharmacology of stably expressed recombinant human NR1a/NR2A and NR1a/NR2B N-methyl-D-aspartate (NMDA) receptors. Inhibition of glutamate-stimulated 45Ca2+ influx by six glycine-site antagonists and inhibition of glycine-stimulated 45Ca2+ influx by five glutamate-site antagonists revealed no significant differences between affinity values obtained for NR1a/NR2A and NR1a/NR2B receptors. The polyamine site agonist spermine showed differential modulation of glutamate- and glycine-stimulated 45Ca2+ influx for recombinant NMDA receptors, inhibiting and stimulating 45Ca2+ influx into cells expressing NR1a/NR2A receptors (IC50 = 408 microM) and NR1a/NR2B receptors (EC50 = 37.3 microM), respectively. The antagonist ifenprodil was selective for NR1a/NR2B receptors (IC50 = 0.099 microM) compared with NR1a/NR2A receptors (IC50 = 164 microM). The effects of putative polyamine site antagonists, redox agents, ethanol, and Mg2+ and Zn2+ ions were also compared between NR1a/NR2A and NR1a/NR2B receptors. This study demonstrates the use of 45Ca2+ influx as a method for investigating the pharmacology of the numerous modulatory sites that regulate the function of recombinant human NMDA receptors stably expressed in L(tk-) cells.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/1-amino-1,3-dicarboxycyclopentane,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Cycloleucine,
http://linkedlifedata.com/resource/pubmed/chemical/Dithionitrobenzoic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Dithiothreitol,
http://linkedlifedata.com/resource/pubmed/chemical/Excitatory Amino Acid Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Glutamic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Glycine,
http://linkedlifedata.com/resource/pubmed/chemical/Kainic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Neurotoxins,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, N-Methyl-D-Aspartate,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Spermine,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfhydryl Reagents,
http://linkedlifedata.com/resource/pubmed/chemical/alpha-Amino-3-hydroxy-5-methyl-4-iso...
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0022-3042
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
66
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2589-95
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:8632186-Animals,
pubmed-meshheading:8632186-Binding Sites,
pubmed-meshheading:8632186-Calcium,
pubmed-meshheading:8632186-Calcium Radioisotopes,
pubmed-meshheading:8632186-Cycloleucine,
pubmed-meshheading:8632186-Dithionitrobenzoic Acid,
pubmed-meshheading:8632186-Dithiothreitol,
pubmed-meshheading:8632186-Excitatory Amino Acid Agonists,
pubmed-meshheading:8632186-Glutamic Acid,
pubmed-meshheading:8632186-Glycine,
pubmed-meshheading:8632186-Humans,
pubmed-meshheading:8632186-Kainic Acid,
pubmed-meshheading:8632186-L Cells (Cell Line),
pubmed-meshheading:8632186-Ligands,
pubmed-meshheading:8632186-Mice,
pubmed-meshheading:8632186-Neurotoxins,
pubmed-meshheading:8632186-Receptors, N-Methyl-D-Aspartate,
pubmed-meshheading:8632186-Recombinant Proteins,
pubmed-meshheading:8632186-Spermine,
pubmed-meshheading:8632186-Sulfhydryl Reagents,
pubmed-meshheading:8632186-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
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pubmed:year |
1996
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pubmed:articleTitle |
Modulation of 45Ca2+ influx into cells stably expressing recombinant human NMDA receptors by ligands acting at distinct recognition sites.
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pubmed:affiliation |
Merck, Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, England.
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pubmed:publicationType |
Journal Article
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