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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
|
pubmed:dateCreated |
1989-6-2
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pubmed:abstractText |
The effects of the new cardiotonic compound, DPI 201-106, on muscarinic responses and muscarinic receptor binding were studied in the guinea pig heart. DPI 201-106 exerted a pronounced anticholinergic action in isolated auricles and a moderate one in papillary muscles, which resembled the pattern of a functional antagonism. However, in competition binding experiments, DPI 201-106 inhibited binding of the specific muscarinic antagonist [3H]NMS with equal potency in atrial and ventricular homogenates (apparent KI = 0.7 mumol/l in atria and 1.2 mumol/l in ventricles). At higher concentrations (greater than 3 mumol/l), DPI 201-106 slowed the dissociation of [3H]NMS from cardiac muscarinic receptors, indicating that DPI 201-106 affects in addition a site allosteric to the muscarinic receptor. It is concluded that DPI 201-106 is able to inhibit cholinergic responses in the heart, not only by a functional antagonism but also by direct interaction with muscarinic receptors.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Atropine,
http://linkedlifedata.com/resource/pubmed/chemical/Carbachol,
http://linkedlifedata.com/resource/pubmed/chemical/DPI 201-106,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
10
|
pubmed:volume |
159
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
125-31
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2707304-Animals,
pubmed-meshheading:2707304-Atropine,
pubmed-meshheading:2707304-Carbachol,
pubmed-meshheading:2707304-Female,
pubmed-meshheading:2707304-Guinea Pigs,
pubmed-meshheading:2707304-Male,
pubmed-meshheading:2707304-Myocardium,
pubmed-meshheading:2707304-Papillary Muscles,
pubmed-meshheading:2707304-Piperazines,
pubmed-meshheading:2707304-Receptors, Muscarinic
|
pubmed:year |
1989
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pubmed:articleTitle |
Interaction of DPI 201-106 with cardiac muscarinic receptors.
|
pubmed:affiliation |
Institut für Pharmakodynamik und Toxikologie, Karl-Franzens-Universität Graz, Austria.
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pubmed:publicationType |
Journal Article,
In Vitro
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