Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
1986-5-30
|
| pubmed:abstractText |
On the isolated electrically driven muscle strip of human right atrial appendages the beta-adrenoceptor subtypes mediating the positive inotropic effects of isoprenaline, dobutamine and procaterol were characterized using the beta 1-selective antagonist bisoprolol and the beta 2-selective antagonist ICI 118,551. The three agonists induced concentration-dependent increases in force of contraction with an order of potency: procaterol (pD2-value: 8.03) greater than isoprenaline (pD2-value: 7.73) greater than dobutamine (pD2-value: 5.44). In saturating concentrations all three agonists produced the same maximum of developed tension. ICI 118,551 (10(-9)--10(-7) mol/l) and bisoprolol (10(-9)--10(-7) mol/l) were nearly equipotent in antagonizing the positive inotropic effects of isoprenaline and dobutamine. However, the slopes of the Schild-plots for both antagonists against both agonists were significantly less than 1.0 indicating interaction with beta 1- and beta 2-adrenoceptors. On the other hand, ICI 118,551 (10(-10)--10(-8) mol/l) was approximately 100 times more potent than bisoprolol (10(-8)--10(-6) mol/l) in antagonizing the positive inotropic effect of the highly selective beta 2-agonist procaterol. In addition, the slopes of the Schild-plots for antagonism of ICI 118,551 and bisoprolol against procaterol were not significantly different from unity indicating interaction with a homogeneous class of beta-adrenoceptors. The pA2-value for ICI 118,551 was 9.49, for bisoprolol it amounted to 6.99.(ABSTRACT TRUNCATED AT 250 WORDS)
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Bisoprolol,
http://linkedlifedata.com/resource/pubmed/chemical/Dobutamine,
http://linkedlifedata.com/resource/pubmed/chemical/Ethanolamines,
http://linkedlifedata.com/resource/pubmed/chemical/ICI 118551,
http://linkedlifedata.com/resource/pubmed/chemical/Isoproterenol,
http://linkedlifedata.com/resource/pubmed/chemical/Procaterol,
http://linkedlifedata.com/resource/pubmed/chemical/Propanolamines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Feb
|
| pubmed:issn |
0028-1298
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
332
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
142-7
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:2871495-Adrenergic beta-Agonists,
pubmed-meshheading:2871495-Adult,
pubmed-meshheading:2871495-Aged,
pubmed-meshheading:2871495-Bisoprolol,
pubmed-meshheading:2871495-Dobutamine,
pubmed-meshheading:2871495-Dose-Response Relationship, Drug,
pubmed-meshheading:2871495-Ethanolamines,
pubmed-meshheading:2871495-Female,
pubmed-meshheading:2871495-Heart Atria,
pubmed-meshheading:2871495-Humans,
pubmed-meshheading:2871495-Isoproterenol,
pubmed-meshheading:2871495-Male,
pubmed-meshheading:2871495-Middle Aged,
pubmed-meshheading:2871495-Myocardial Contraction,
pubmed-meshheading:2871495-Myocardium,
pubmed-meshheading:2871495-Procaterol,
pubmed-meshheading:2871495-Propanolamines,
pubmed-meshheading:2871495-Receptors, Adrenergic, beta,
pubmed-meshheading:2871495-Stimulation, Chemical
|
| pubmed:year |
1986
|
| pubmed:articleTitle |
Human myocardial beta-adrenoceptors: demonstration of both beta 1- and beta 2-adrenoceptors mediating contractile responses to beta-agonists on the isolated right atrium.
|
| pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|