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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
1994-3-21
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pubmed:abstractText |
The effect of various blockers of voltage operated calcium channels (VOCCs) was studied on the non-inactivating, plateau phase of KCl-induced intracellular free Ca2+ ([Ca2+]i) elevation in rat cortical and chicken forebrain synaptosomes. In chicken synaptosomes, omega-CgTx GVIA (0.1 nM to 1 microM) and omega-CgTx MVIIA (0.1 nM to 1 microM), both selective blockers of N-type Ca2+ channels, produced a concentration-dependent inhibition of the plateau phase of [Ca2+]i elevation. omega-CgTx GVIA (IC50 value 28 nM) was more potent than omega-CgTx MVIIA (IC50 value 78 nM), but at submaximal concentrations, took longer to reach its maximum effect (20 min for omega-CgTx GVIA; 10 min for omega-CgTx MVIIA). At 1 microM, the highest concentration tested, each toxin blocked > 85% of [Ca2+]i elevation. The effect of omega-CgTx GVIA on the extent and time-course of inhibition of [Ca2+]i elevation was maintained in a Na(+)-free, choline substituted, medium. omega-Aga IVA (300 nM), a selective blocker of P-type calcium channels, inhibited 28 +/- 5% of [Ca2+]i elevation. The effect of a combination of submaximal inhibitory concentrations of omega-CgTx GVIA (100 nM) and omega-Aga IVA (300 nM) was less than additive. In rat synaptosomes, omega-CgTx GVIA (1 microM) and omega-CgTx MVIIA (1 microM), blocked only 18 +/- 5% and 17 +/- 4% of the plateau phase of free Ca2+ elevation, respectively. omega-Aga IVA produced a concentration-dependent inhibition of [Ca2+]i elevation in this preparation. Threshold inhibition was observed at 1 nM, and maximum inhibition (64 +/- 8%) at 1 microM.(ABSTRACT TRUNCATED AT 250 WORDS)
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0028-3908
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
32
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1195-202
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8107973-Animals,
pubmed-meshheading:8107973-Calcium,
pubmed-meshheading:8107973-Calcium Channel Blockers,
pubmed-meshheading:8107973-Calcium Channels,
pubmed-meshheading:8107973-Chickens,
pubmed-meshheading:8107973-Potassium Chloride,
pubmed-meshheading:8107973-Prosencephalon,
pubmed-meshheading:8107973-Rats,
pubmed-meshheading:8107973-Species Specificity,
pubmed-meshheading:8107973-Synaptosomes
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pubmed:year |
1993
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pubmed:articleTitle |
Pharmacological characterisation of the calcium channels coupled to the plateau phase of KCl-induced intracellular free Ca2+ elevation in chicken and rat synaptosomes.
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pubmed:affiliation |
Lilly Research Centre, Windlesham, Surrey, U.K.
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pubmed:publicationType |
Journal Article,
In Vitro
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