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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
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pubmed:dateCreated |
1987-8-3
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pubmed:abstractText |
Two dihydropyridine compounds, Bay K8644 (a calcium entry activator) and nifedipine (a calcium entry blocker), were found to inhibit the binding of [3H]phenylisopropyladenosine ([3H]PIA) to A1 adenosine receptors in rat cerebral cortex membranes with comparable potencies (IC50 10-30 microM). Scatchard analyses indicated that both Bay K8644 and nifedipine inhibited the binding of [3H]PIA by increasing the KD but without significant effect on the Bmax. When tested at 100 microM, neither Bay K8644 nor nifedipine showed a significant effect on [3H]-p-aminoclonidine ([3H]PAC; alpha 2-adrenergic receptor), [3H]dihydroalprenolol ([3H]DHA; beta-adrenergic receptor), [3H]spiperone (dopamine receptor), and [3H]nitrobenzylthioinosine [( 3H]NBMPR; nucleoside transporter) binding. In the presence of 10 mM Mg2+, the ability of 2-chloroadenosine (2-Cl-Ad, an A1 adenosine receptor agonist) to displace [3H]PIA binding was increased. Conversely, the potencies of 1,3-diethyl-8-phenylxanthine (DPX; an A1 receptor antagonist), Bay K8644 and nifedipine in inhibiting [3H]PIA binding were unchanged. It is suggested that both Bay K8644 and nifedipine may act as antagonists of adenosine A1 receptors, in addition to their well-known effects on calcium channels.
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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/1,3-diethyl-8-phenylxanthine,
http://linkedlifedata.com/resource/pubmed/chemical/3-Pyridinecarboxylic acid...,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Nifedipine,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylisopropyladenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Purinergic,
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 |
0006-2952
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
36
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2183-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2440436-3-Pyridinecarboxylic acid...,
pubmed-meshheading:2440436-Adenosine,
pubmed-meshheading:2440436-Animals,
pubmed-meshheading:2440436-Cell Membrane,
pubmed-meshheading:2440436-Cerebral Cortex,
pubmed-meshheading:2440436-Male,
pubmed-meshheading:2440436-Nifedipine,
pubmed-meshheading:2440436-Phenylisopropyladenosine,
pubmed-meshheading:2440436-Rats,
pubmed-meshheading:2440436-Rats, Inbred Strains,
pubmed-meshheading:2440436-Receptors, Purinergic,
pubmed-meshheading:2440436-Xanthines
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pubmed:year |
1987
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pubmed:articleTitle |
Inhibition of radioligand binding to A1 adenosine receptors by Bay K8644 and nifedipine.
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pubmed:publicationType |
Journal Article,
Comparative Study
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