Source:http://linkedlifedata.com/resource/pubmed/id/10411473
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
14
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pubmed:dateCreated |
1999-8-2
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pubmed:abstractText |
Caffeine and other methylxanthines are known to induce Ca(2+)-release from intracellular stores via the ryanodine receptor. In the present work, a range of caffeine analogues, in which methyl groups at the 1 and 7 positions were replaced with alkyl chains containing different functional groups (oxo, hydroxyl, propargyl, ester, and acids), were synthesized. These compounds were then screened for their ability to potentiate Ca(2+)-release induced by cADPR (an endogenous modulator of ryanodine receptors) in sea urchin egg homogenates. Two of the synthesized methylxanthines, 1, 3-dimethyl-7-(7-hydroxyoctyl)xanthine (37) and 3-methyl-7-(7-oxooctyl)-1-propargylxanthine (66), were shown to be more potent than caffeine in potentiating cADPR-induced Ca(2+)-release, while 1,3-dimethyl-7-(5-ethylcarboxypentyl)xanthine (14) was shown to be more efficacious. The development of new methylxanthine analogues may lead to a better understanding of ryanodine receptor function and could possibly provide novel therapeutic agents.
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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/Adenosine Diphosphate Ribose,
http://linkedlifedata.com/resource/pubmed/chemical/Caffeine,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic ADP-Ribose,
http://linkedlifedata.com/resource/pubmed/chemical/Ryanodine Receptor Calcium Release...,
http://linkedlifedata.com/resource/pubmed/chemical/Xanthines
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
42
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2527-34
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:10411473-Adenosine Diphosphate Ribose,
pubmed-meshheading:10411473-Animals,
pubmed-meshheading:10411473-Caffeine,
pubmed-meshheading:10411473-Calcium,
pubmed-meshheading:10411473-Cyclic ADP-Ribose,
pubmed-meshheading:10411473-Drug Evaluation, Preclinical,
pubmed-meshheading:10411473-Ovum,
pubmed-meshheading:10411473-Ryanodine Receptor Calcium Release Channel,
pubmed-meshheading:10411473-Sea Urchins,
pubmed-meshheading:10411473-Structure-Activity Relationship,
pubmed-meshheading:10411473-Xanthines
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pubmed:year |
1999
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pubmed:articleTitle |
Potentiation of cADPR-induced Ca(2+)-release by methylxanthine analogues.
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pubmed:affiliation |
Department of Biochemical Sciences, University La Sapienza, Via degli Apuli 9, 00185 Rome, Italy.
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pubmed:publicationType |
Journal Article,
In Vitro
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