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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1 Pt 1
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pubmed:dateCreated |
1987-3-2
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pubmed:abstractText |
To examine the coupling of cardiac cell-surface beta-adrenergic receptors to adenylate cyclase activation and contractile response, we studied this receptor-effector response system in monolayers of spontaneously contracting chick embryo ventricular cells under physiological conditions. The hydrophilic ligand 3H-CGP12177 identified uniformly high-agonist affinity beta-adrenergic receptors (isoproterenol KD = 15 +/- 9 nM). Isoproterenol-stimulated cyclic AMP (cAMP) accumulation with 50% effective concentration at (EC50) = 12.1 nM and augmented contractile response with EC50 = 6 nM under identical conditions. One micromolar isoproterenol induced receptor loss from the cell surface with t1/2 = 13.2 min; under identical conditions cAMP content declined with t1/2 = 13.5 min and contractile response with t1/2 = 20.7 min. After agonist removal cAMP response recovered with t1/2 = 15.7 min and receptors with t1/2 = 24.7 min. Sixty minutes after agonist removal there was recovery of 52% of maximal cAMP responsiveness and 82% of the initial number of receptors; receptor occupancy was associated with 78% of initial contractile response. Agonist affinity for cell-surface receptors was changed only modestly by agonist exposure. We conclude that for this system there is relatively close coupling between high-affinity receptors, adenylate cyclase stimulation, and contractile response.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenylate Cyclase,
http://linkedlifedata.com/resource/pubmed/chemical/CGP 12177,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Isoproterenol,
http://linkedlifedata.com/resource/pubmed/chemical/Propanolamines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0002-9513
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
252
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
C47-54
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:3028146-Adenylate Cyclase,
pubmed-meshheading:3028146-Animals,
pubmed-meshheading:3028146-Binding, Competitive,
pubmed-meshheading:3028146-Cell Membrane,
pubmed-meshheading:3028146-Cells, Cultured,
pubmed-meshheading:3028146-Chick Embryo,
pubmed-meshheading:3028146-Cyclic AMP,
pubmed-meshheading:3028146-Heart Ventricles,
pubmed-meshheading:3028146-Homeostasis,
pubmed-meshheading:3028146-Isoproterenol,
pubmed-meshheading:3028146-Kinetics,
pubmed-meshheading:3028146-Myocardial Contraction,
pubmed-meshheading:3028146-Myocardium,
pubmed-meshheading:3028146-Propanolamines,
pubmed-meshheading:3028146-Receptors, Adrenergic, beta
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pubmed:year |
1987
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pubmed:articleTitle |
Adenylate cyclase regulation in intact cultured myocardial cells.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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