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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
1988-5-3
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pubmed:abstractText |
The effects of the calcium entry blockers verapamil (V), diltiazem (D), nifedipine (NF) and nicardipine (NC) have been studied on calcium concentration-effect curves elicited in depolarized (K+, 40 mmol/l) and in serotonin-exposed (6 mumol/l) rat middle cerebral arteries (RMCA) in order to compare the relative potencies of the blockers against these two calcium channel activating mechanisms. In control conditions, Ca2+ sensitivity expressed as pD2 and maximal active wall tension (AWT) were not significantly different in depolarized and in 5-HT-exposed vessels: pD2: 3.39 +/- 0.08 vs 3.50 +/- 0.06 and AWT: 0.93 +/- 0.15 mN.mm-1 vs 0.90 +/- 0.16 mN.mm-1 respectively. V, D, NF and NC displaced Ca2+ control curves to the right and depressed the maximum contractile response in the two experimental conditions, which suggests a noncompetitive type of antagonism. All the blockers were more potent inhibitors of Ca2+-induced contractions in depolarized than in serotonin-exposed middle cerebral arteries. The IC50 values (concentration of blockers producing a 50% inhibition of maximal control contractile response) were (nmol/l): V = 20, D = 120, NF = 0.4, NC = 1 and V = 400, D = 10,000, NF = 20, NC = 7 in depolarized and serotonin-exposed arteries respectively. From these IC50 values, the relative order of potency of the CEB's was not the same in the two experimental conditions suggesting that while serotonin and K+ both promote the entry of Ca2+ into vascular smooth muscle cells of RMCA, they either activate a different gating mechanism associated with a single common channel or perhaps distinct channels.(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 |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Diltiazem,
http://linkedlifedata.com/resource/pubmed/chemical/Nicardipine,
http://linkedlifedata.com/resource/pubmed/chemical/Nifedipine,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Verapamil
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0028-1298
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
336
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
670-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3444482-Animals,
pubmed-meshheading:3444482-Calcium,
pubmed-meshheading:3444482-Calcium Channel Blockers,
pubmed-meshheading:3444482-Cerebral Arteries,
pubmed-meshheading:3444482-Diltiazem,
pubmed-meshheading:3444482-Female,
pubmed-meshheading:3444482-Nicardipine,
pubmed-meshheading:3444482-Nifedipine,
pubmed-meshheading:3444482-Rats,
pubmed-meshheading:3444482-Rats, Inbred Strains,
pubmed-meshheading:3444482-Serotonin,
pubmed-meshheading:3444482-Vascular Resistance,
pubmed-meshheading:3444482-Verapamil
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pubmed:year |
1987
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pubmed:articleTitle |
Compared effects of calcium entry blockers on calcium-induced tension in rat isolated cerebral and peripheral resistance vessels.
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pubmed:affiliation |
Université Louis Pasteur, Laboratoire de Pharmacodynamie (CNRS UA 600), Strasbourg, France.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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