pubmed-article:8581286 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:8581286 | lifeskim:mentions | umls-concept:C0037492 | lld:lifeskim |
pubmed-article:8581286 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
pubmed-article:8581286 | lifeskim:mentions | umls-concept:C0168759 | lld:lifeskim |
pubmed-article:8581286 | pubmed:issue | 5 | lld:pubmed |
pubmed-article:8581286 | pubmed:dateCreated | 1996-3-20 | lld:pubmed |
pubmed-article:8581286 | pubmed:abstractText | 1. Besipirdine (HP 749) is a compound undergoing clinical trials for efficacy in treating Alzheimer's disease. Among other pharmacological effects, besipirdine inhibits voltage-dependent sodium and potassium channels. This paper presents a pharmacological study of the interaction of besipirdine with voltage-dependent sodium channels. 2. Besipirdine inhibited [3H]-batrachotoxin binding (IC50 = 5.5 +/- 0.2 microM) in a rat brain vesicular preparation and concentration-dependently inhibited veratridine (25 microM)-stimulated increases in intracellular free sodium ([Na+]i) and calcium ([Ca2+]i) in primary cultured cortical neurones of rat. 3. Besipirdine (30-100 microM) concentration-dependently inhibited (up to 100%) veratridine-stimulated release of [3H]-noradrenaline (NA) from rat cortical slices. 4. When examined in greater detail, besipirdine was found to inhibit [3H]-batrachotoxin binding in vesicular membranes competitively. However, when examined in rat brain synaptosomes, we found that the antagonism by besipirdine was not competitive; that is, the maximal stimulation of [Ca2+]i induced by veratridine decreased with increasing concentrations of besipirdine. 5. These results show that besipirdine is an inhibitor of voltage-sensitive sodium channels and appears to bind to a site close to the batrachotoxin/veratridine binding site. | lld:pubmed |
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pubmed-article:8581286 | pubmed:language | eng | lld:pubmed |
pubmed-article:8581286 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8581286 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:8581286 | pubmed:month | Nov | lld:pubmed |
pubmed-article:8581286 | pubmed:issn | 0007-1188 | lld:pubmed |
pubmed-article:8581286 | pubmed:author | pubmed-author:SmithC PCP | lld:pubmed |
pubmed-article:8581286 | pubmed:author | pubmed-author:TangLL | lld:pubmed |
pubmed-article:8581286 | pubmed:author | pubmed-author:HugerF PFP | lld:pubmed |
pubmed-article:8581286 | pubmed:author | pubmed-author:KongsamutSS | lld:pubmed |
pubmed-article:8581286 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:8581286 | pubmed:volume | 116 | lld:pubmed |
pubmed-article:8581286 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:8581286 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:8581286 | pubmed:pagination | 2468-72 | lld:pubmed |
pubmed-article:8581286 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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pubmed-article:8581286 | pubmed:year | 1995 | lld:pubmed |
pubmed-article:8581286 | pubmed:articleTitle | Effects of besipirdine at the voltage-dependent sodium channel. | lld:pubmed |
pubmed-article:8581286 | pubmed:affiliation | Department of Biological Research, Hoechst Roussel Pharmaceuticals, Inc., Somerville, NJ 08876, USA. | lld:pubmed |
pubmed-article:8581286 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:8581286 | pubmed:publicationType | In Vitro | lld:pubmed |