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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
1998-5-28
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pubmed:abstractText |
The effect of the Aconitum alkaloids aconitine, 3-acetylaconitine, lappaconitine, and N-desacetyllappaconitine to inhibit [3H]noradrenaline uptake was investigated in rat hippocampal synaptosomes. Aconitine and 3-acetylaconitine, which are known to activate sodium channels, had comparable inhibitory potencies and yielded Ki (inhibitor constant) values of 230 +/- 66 nM and 316 +/- 96 nM, respectively. In contrast, lappaconitine and N-desacetyllappaconitine failed to inhibit [3H]noradrenaline uptake. When either lappaconitine or N-desacetyllappaconitine was applied in combination with aconitine, [3H]noradrenaline uptake was not affected. The sodium channel blocker tetrodotoxin enhanced [3H]noradrenaline uptake, whereas uptake was completely blocked in sodium-free incubation medium. The inhibitory action of aconitine and 3-acetylaconitine on [3H]noradrenaline uptake was blocked by addition of tetrodotoxin. Patch clamp studies performed on cultured rat hippocampal neurons revealed an inhibitory action of lappaconitine and N-desacetyllappaconitine on whole cell sodium currents. It is concluded that the blockade of [3H]noradrenaline uptake evoked by aconitine and 3-acetylaconitine is mediated indirectly by an increased sodium concentration in the synaptosomes.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/3-acetylaconitine,
http://linkedlifedata.com/resource/pubmed/chemical/Aconitine,
http://linkedlifedata.com/resource/pubmed/chemical/N-deacetyllappaconitine,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/lappaconitine
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0006-2952
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
55
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
883-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9586961-Aconitine,
pubmed-meshheading:9586961-Animals,
pubmed-meshheading:9586961-Hippocampus,
pubmed-meshheading:9586961-Male,
pubmed-meshheading:9586961-Norepinephrine,
pubmed-meshheading:9586961-Patch-Clamp Techniques,
pubmed-meshheading:9586961-Plants, Medicinal,
pubmed-meshheading:9586961-Pyramidal Cells,
pubmed-meshheading:9586961-Radioligand Assay,
pubmed-meshheading:9586961-Rats,
pubmed-meshheading:9586961-Rats, Wistar,
pubmed-meshheading:9586961-Structure-Activity Relationship,
pubmed-meshheading:9586961-Synaptosomes,
pubmed-meshheading:9586961-Tritium
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pubmed:year |
1998
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pubmed:articleTitle |
Different effects on [3H]noradrenaline uptake of the Aconitum alkaloids aconitine, 3-acetylaconitine, lappaconitine, and N-desacetyllappaconitine in rat hippocampus.
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pubmed:affiliation |
Department of Pharmacy and Pharmacology of Natural Compounds, University of Ulm, Germany.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro
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