Linked Life Data

2352840

Source:http://linkedlifedata.com/resource/pubmed/id/2352840

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-2
pubmed:dateCreated
1990-7-17
pubmed:abstractText
We have investigated the effect of W-7, a calmodulin (CaM) antagonist, on Ca2+ mobilization in a human salivary epithelial cell line, HSG-PA, after muscarinic receptor stimulation. In a medium containing 1.5 mmol/l Ca2+, W-7 reduced both the maximum peak increase in cytosolic Ca2+ [( Ca2+]i) which follows stimulation by carbachol (Cch, 100 mumol/l) and the sustained nature of the response. Using an experimental approach which allows separate visualization of the intracellular Ca2+ release and extracellular Ca2+ entry phases, W-7 was shown preferentially to inhibit Ca2+ release. At 100 mumol/l W-7, Cch-induced Ca2+ release was completely inhibited, but Cch-induced Ca2+ entry was partially (approximately 40%) maintained. This W-7 residual Ca2+ entry response was abolished when cells were depolarized with high K+ or gramicidin D. W-7 also substantially inhibited Cch-induced inositol trisphosphate (IP3) production (approximately 5%). W-5, a less potent CaM antagonist than W-7, had markedly smaller effects on Cch-induced Ca2+ mobilization and IP3 formation. W-7 (100 mumol/l) completely blocked (comparable to 10 mumol/l atropine) the binding of the muscarinic antagonist [3H] quinuclidinyl benzilate (QNB) to muscarinic receptors on cell membranes, whereas Cch (at 100 mumol/l) had minimal effects on ligand binding. W-7 and W-5 were equipotent in their ability to inhibit [3H] QNB binding. These results suggest that W-7 reduces Ca2+ mobilization in HSG-PA cells by a mechanism which likely involves the antagonism of a CaM regulatory step(s) but may also involve at least a partial blockade of the muscarinic receptor.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0031-6768
pubmed:author
pubmed:issnType
Print
pubmed:volume
416
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
36-42
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
The effect of N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) on muscarinic receptor-induced Ca2+ mobilization in a human salivary epithelial cell line.
pubmed:affiliation
Clinical Investigations and Patient Care Branch, National Institute of Dental Research, National Institutes of Health, Bethesda, MD 20892.
pubmed:publicationType
Journal Article