Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1989-6-2
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
10
pubmed:volume
159
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
125-31
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Interaction of DPI 201-106 with cardiac muscarinic receptors.
pubmed:affiliation
Institut für Pharmakodynamik und Toxikologie, Karl-Franzens-Universität Graz, Austria.
pubmed:publicationType
Journal Article, In Vitro