Linked Life Data

2575531

Source:http://linkedlifedata.com/resource/pubmed/id/2575531

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1990-3-2
pubmed:abstractText
The effects of nebivolol, the racemic mixture of the SRRR and RSSS enantiomers, on beta-adrenoceptor-mediated cAMP accumulation in living cardiac cells were compared to those of beta-adrenoceptor antagonists. Serum-free cultivation of cardiac cells from ventricles of 2 to 3-day-old Wistar rats resulted in a population of contractile cardiac cells almost free of mesenchymal non-myocardial cells. Isoproterenol stimulated beta 1- as well as beta 2-adrenoceptor sites. Selective beta 1- and beta 2-receptor site occlusion, in the presence of an appropriate concentration of the selective beta 2-adrenoceptor antagonist, ICI 118-551, or the selective beta 1-adrenoceptor antagonist, CGP 20712-A, showed that the receptor population consisted of mostly the beta 1-adrenergic subtype. The latter could be specifically stimulated by noradrenaline. Nebivolol and d-nebivolol (SRRR) inhibited noradrenaline-induced cAMP accumulation with IC50 values of 22 and 15 nM, respectively. CGP 20712-A was 10 times more active and atenolol was 7 times less active than nebivolol. Both assays, beta-adrenoceptor binding and cAMP accumulation, evidenced beta-adrenoceptor antagonistic properties only for the d-enantiomer of nebivolol (SRRR). 1-Nebivolol (RSSS) showed no beta-adrenergic activity.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
5
pubmed:volume
172
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
471-9
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Beta-adrenoceptor-mediated cAMP accumulation in cardiac cells: effects of nebivolol.
pubmed:affiliation
Department of Biochemical Pharmacology, Janssen Research Foundation, Beerse, Belgium.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't