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rdf:type |
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lifeskim:mentions |
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0047123,
umls-concept:C0049860,
umls-concept:C0056792,
umls-concept:C0205155,
umls-concept:C0813872,
umls-concept:C0936012,
umls-concept:C1167622,
umls-concept:C1413682,
umls-concept:C1522472,
umls-concept:C1551341,
umls-concept:C1552858,
umls-concept:C1552923,
umls-concept:C1552924,
umls-concept:C1705191,
umls-concept:C1882598
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pubmed:issue |
3
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pubmed:dateCreated |
1993-5-13
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pubmed:abstractText |
1. The regional binding of [3H]-(+)-5-methyl-10,11-dihydro-5H-dibenzo (a,d)cyclohepten-5,10-imine maleate ([3H]-(+)-MK 801) to sections of rat brain was measured by an in vitro quantitative autoradiographic technique. A heterogeneous distribution of binding sites was observed. 2. High values of binding were detected in the hippocampal formation and cerebral cortex, while very low binding was found in cerebellum. [3H]-(+)-MK 801 binding was not detectable in white matter tracts or in the brain stem. 3. [3H]-(+)-MK 801 binding was inhibited by increasing concentrations of both 7-chlorokynurenate (1-1000 microM) and ((+)-2-carboxypiperazine-4-yl)propyl-1-phosphonic acid (CPP) (0.1-100 microM). High concentrations of both drugs were able to inhibit completely specific [3H]-(+)-MK 801 binding. 4. IC50 values calculated for both 7-chlorokynurenate and CPP-induced [3H]-(+)-MK 801 binding inhibition were similar in all brain regions analyzed. 5. The inhibitory action of 7-chlorokynurenate and that of CPP on [3H]-(+)-MK 801 binding were reversed by addition of glycine and glutamate respectively. 6. It is concluded that activation of glycine and N-methyl-D-aspartate (NMDA) receptors is obligatory for the binding of [3H]-(+)-MK 801 to occur in all of the brain regions examined in the present study. Furthermore, on the basis of the similar regional sensitivities of [3H]-(+)-MK 801 binding to the inhibitory action of 7-chlorokynurenate and CPP, a single pharmacological classification of the NMDA receptor complex in brain is suggested. The cerebellum was not included in the study due to the very low level of [3H]-(+)-MK 801 binding detected under the experimental conditions used.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-1676144,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-1682157,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-1694710,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-1968086,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2169959,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2188577,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2433595,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2448800,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2536176,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2543272,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2557130,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2566140,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2823273,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2841759,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2842779,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2873045,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-2876750,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-3022881,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-3031504,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-3031525,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-3291999,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-6093256,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-6112965,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-6138738,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-6142499,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-6151863,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8096780-686171
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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 |
Mar
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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 |
108
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
577-82
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8096780-Animals,
pubmed-meshheading:8096780-Autoradiography,
pubmed-meshheading:8096780-Brain,
pubmed-meshheading:8096780-Cerebellum,
pubmed-meshheading:8096780-Dizocilpine Maleate,
pubmed-meshheading:8096780-Glutamates,
pubmed-meshheading:8096780-Glutamic Acid,
pubmed-meshheading:8096780-Glycine,
pubmed-meshheading:8096780-Image Processing, Computer-Assisted,
pubmed-meshheading:8096780-Kynurenic Acid,
pubmed-meshheading:8096780-Male,
pubmed-meshheading:8096780-Piperazines,
pubmed-meshheading:8096780-Rats,
pubmed-meshheading:8096780-Rats, Sprague-Dawley,
pubmed-meshheading:8096780-Receptors, N-Methyl-D-Aspartate
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pubmed:year |
1993
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pubmed:articleTitle |
Inhibition of [3H]-(+)-MK 801 binding to rat brain sections by CPP and 7-chlorokynurenic acid: an autoradiographic analysis.
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pubmed:affiliation |
Glaxo Research Laboratories, Verona, Italy.
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pubmed:publicationType |
Journal Article,
In Vitro
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