Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1998-5-28
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0006-2952
pubmed:author
pubmed:issnType
Print
pubmed:day
15
pubmed:volume
55
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
883-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1998
pubmed:articleTitle
Different effects on [3H]noradrenaline uptake of the Aconitum alkaloids aconitine, 3-acetylaconitine, lappaconitine, and N-desacetyllappaconitine in rat hippocampus.
pubmed:affiliation
Department of Pharmacy and Pharmacology of Natural Compounds, University of Ulm, Germany.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro