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rdf:type |
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lifeskim:mentions |
umls-concept:C0002520,
umls-concept:C0025914,
umls-concept:C0026809,
umls-concept:C0030685,
umls-concept:C0079245,
umls-concept:C0140182,
umls-concept:C0205227,
umls-concept:C0380266,
umls-concept:C0391871,
umls-concept:C0680255,
umls-concept:C0813872,
umls-concept:C0870883,
umls-concept:C1176472,
umls-concept:C1280500,
umls-concept:C1283071,
umls-concept:C1512523,
umls-concept:C1963578
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pubmed:issue |
8
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pubmed:dateCreated |
1996-10-10
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pubmed:abstractText |
1. In this study the effect of FPL 12495AA, the desglycinyl metabolite of remacemide hydrochloride and dizocilpine (MK-801), on potassium- and veratridine-stimulated release of neurotransmitter amino acids from mouse cortical slices was investigated. 2. Veratridine (20 microM) and potassium (60 mM) produced a preferential release of glutamate and aspartate. Potassium-stimulated release was calcium-dependent, while veratridine-stimulated release was only partially affected by removal of calcium from the medium. 3. FPL 12495AA significantly inhibited veratridine- and potassium-stimulated release of glutamate and aspartate. Lower concentrations of FPL 12495AA were needed to inhibit veratridine-stimulated release of glutamate (12.5 microM) than potassium-stimulated release (100 microM). 4. Dizocilpine significantly inhibited veratridine- and potassium-stimulated release of glutamate and aspartate at concentrations of 100 microM and above. 5. FPL 12495AA and dizocilpine both have an affinity for the ion channel subsite of the N-methyl-D-aspartate (NMDA) receptor. The reduction of potassium-stimulated release of glutamate and aspartate by FPL 12495AA and dizocilpine is probably due to NMDA receptor blockade. 6. FPL 12495AA inhibited veratridine-stimulated release at a concentration of 12.5 microM while dizocilpine was effective only at a concentration of 100 microM. This difference in efficacy is probably due to the higher affinity of FPL 12495AA compared to dizocilpine at the veratridine-binding site on the sodium channel.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-1361916,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-1388119,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-1506452,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-1660399,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-1731047,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-1963406,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-2843782,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-2853604,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-2894484,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-2897648,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-3311770,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-3529096,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-3757936,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-4153804,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-6103519,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-6104753,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-7508638,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-7532339,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-7895041,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-7911685,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-8102309,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8719781-8449271
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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/Acetamides,
http://linkedlifedata.com/resource/pubmed/chemical/Anticonvulsants,
http://linkedlifedata.com/resource/pubmed/chemical/Aspartic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Dizocilpine Maleate,
http://linkedlifedata.com/resource/pubmed/chemical/Excitatory Amino Acid Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/FPL 12495,
http://linkedlifedata.com/resource/pubmed/chemical/Glutamic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Phenethylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium,
http://linkedlifedata.com/resource/pubmed/chemical/Veratridine,
http://linkedlifedata.com/resource/pubmed/chemical/remacemide
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
116
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3087-92
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8719781-Acetamides,
pubmed-meshheading:8719781-Animals,
pubmed-meshheading:8719781-Anticonvulsants,
pubmed-meshheading:8719781-Aspartic Acid,
pubmed-meshheading:8719781-Cerebral Cortex,
pubmed-meshheading:8719781-Dizocilpine Maleate,
pubmed-meshheading:8719781-Excitatory Amino Acid Antagonists,
pubmed-meshheading:8719781-Female,
pubmed-meshheading:8719781-Glutamic Acid,
pubmed-meshheading:8719781-Male,
pubmed-meshheading:8719781-Mice,
pubmed-meshheading:8719781-Mice, Inbred BALB C,
pubmed-meshheading:8719781-Phenethylamines,
pubmed-meshheading:8719781-Potassium,
pubmed-meshheading:8719781-Veratridine
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pubmed:year |
1995
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pubmed:articleTitle |
The effect of the desglycinyl metabolite of remacemide hydrochloride (FPL 12495AA) and dizocilpine (MK-801) on endogenous amino acid release from mouse cortex.
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pubmed:affiliation |
Department of Pharmacology and Therapeutics, University of Wales College of Medicine, Heath Park, Cardiff.
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pubmed:publicationType |
Journal Article,
In Vitro
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