Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
13
pubmed:dateCreated
1998-10-15
pubmed:abstractText
Previous work indicated that hyperstimulation of muscarinic receptors brings about profound changes not only in the density of the muscarinic receptors, but also of the beta-adrenoceptors in rat heart atria in vivo. We have now investigated whether a similar receptor cross-regulation occurs in cardiomyocytes in vitro. Cardiomyocytes from 3-4 day old rats were exposed to chemical agents on days 5-6 in culture. Densities of muscarinic and beta-adrenergic receptors were measured according to the binding of N-[3H]methylscopolamine and [ H]CGP 12177, respectively, to cell surface membranes and cell homogenates. Exposure of cells to the muscarinic agonist carbachol (1 mmol/l) brought about a profound decrease in the number of muscarinic receptors. The number of beta-adrenoceptors displayed biphasic changes, being augmented after 24 h (by 20-45% on the cell surface and by 29% in the homogenate) and diminished after 48 h and 72 h (after 48 h, decrease by 44-75% on the cell surface and by 36% in the homogenate). These effects of carbachol were not prevented by dimethylaminopropyl-bis-indolylmaleimide, the inhibitor of protein kinase C. Exposure of cells to the beta-adrenoceptor agonist isoprenaline (0.1 mmol/l) strongly diminished the number of beta-adrenoceptors on the cell surface and in the homogenate. The density of muscarinic receptors on the cell surface was diminished by 24-43% after 24 h exposure to isoprenaline and unchanged after 48 h, whereas the concentration of muscarinic receptors in the homogenate was unchanged after 24 h and increased by 20% after 48 h. The isoprenaline-induced decrease in the density of cell surface muscarinic receptors could not be simulated by forskolin and was not abolished by the protein kinase A inhibitors Rp-cAMPS and HA-1004. Dibutyryl cyclic AMP diminished the density of cell surface muscarinic receptors more than that of the beta-adrenergic receptors. Our data reveal a novel phenomenon of a biphasic change (an increase followed by a loss) in the density of beta-adrenoceptors during exposure of cardiocytes to carbachol. Activation of beta-adrenoceptors brings about less conspicuous changes in the density of muscarinic receptors. The observed phenomena of receptor cross-regulation cannot be explained by simple activations of protein kinases A and C.
pubmed:grant
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/Adrenergic beta-Antagonists, http://linkedlifedata.com/resource/pubmed/chemical/Bucladesine, http://linkedlifedata.com/resource/pubmed/chemical/CGP 12177, http://linkedlifedata.com/resource/pubmed/chemical/Carbachol, http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP, http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors, http://linkedlifedata.com/resource/pubmed/chemical/Forskolin, http://linkedlifedata.com/resource/pubmed/chemical/Indoles, http://linkedlifedata.com/resource/pubmed/chemical/Isoproterenol, http://linkedlifedata.com/resource/pubmed/chemical/Isoquinolines, http://linkedlifedata.com/resource/pubmed/chemical/Maleimides, http://linkedlifedata.com/resource/pubmed/chemical/Muscarinic Agonists, http://linkedlifedata.com/resource/pubmed/chemical/N-(2-guanidinoethyl)-5-isoquinolines..., http://linkedlifedata.com/resource/pubmed/chemical/N-Methylscopolamine, http://linkedlifedata.com/resource/pubmed/chemical/Propanolamines, http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic, http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides, http://linkedlifedata.com/resource/pubmed/chemical/Thionucleotides, http://linkedlifedata.com/resource/pubmed/chemical/Tritium, http://linkedlifedata.com/resource/pubmed/chemical/adenosine-3',5'-cyclic..., http://linkedlifedata.com/resource/pubmed/chemical/bisindolylmaleimide I
pubmed:status
MEDLINE
pubmed:issn
0024-3205
pubmed:author
pubmed:issnType
Print
pubmed:volume
63
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1169-82
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed-meshheading:9763212-Adrenergic beta-Agonists, pubmed-meshheading:9763212-Adrenergic beta-Antagonists, pubmed-meshheading:9763212-Animals, pubmed-meshheading:9763212-Binding, Competitive, pubmed-meshheading:9763212-Binding Sites, pubmed-meshheading:9763212-Bucladesine, pubmed-meshheading:9763212-Carbachol, pubmed-meshheading:9763212-Cells, Cultured, pubmed-meshheading:9763212-Cyclic AMP, pubmed-meshheading:9763212-Enzyme Inhibitors, pubmed-meshheading:9763212-Female, pubmed-meshheading:9763212-Forskolin, pubmed-meshheading:9763212-Indoles, pubmed-meshheading:9763212-Isoproterenol, pubmed-meshheading:9763212-Isoquinolines, pubmed-meshheading:9763212-Kinetics, pubmed-meshheading:9763212-Male, pubmed-meshheading:9763212-Maleimides, pubmed-meshheading:9763212-Muscarinic Agonists, pubmed-meshheading:9763212-Myocardium, pubmed-meshheading:9763212-N-Methylscopolamine, pubmed-meshheading:9763212-Propanolamines, pubmed-meshheading:9763212-Protein Kinase C, pubmed-meshheading:9763212-Radioligand Assay, pubmed-meshheading:9763212-Rats, pubmed-meshheading:9763212-Rats, Wistar, pubmed-meshheading:9763212-Receptors, Adrenergic, alpha, pubmed-meshheading:9763212-Receptors, Muscarinic, pubmed-meshheading:9763212-Sulfonamides, pubmed-meshheading:9763212-Thionucleotides, pubmed-meshheading:9763212-Tritium
pubmed:year
1998
pubmed:articleTitle
Heterologous regulation of muscarinic and beta-adrenergic receptors in rat cardiomyocytes in culture.
pubmed:affiliation
Institute of Physiology, Academy of Sciences of the Czech Republic, Prague.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't