12535855

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Predicate	Object
rdf:type	pubmed:Citation
lifeskim:mentions	umls-concept:C0053799, umls-concept:C0063773, umls-concept:C0068475, umls-concept:C0330390, umls-concept:C1167622, umls-concept:C1707455, umls-concept:C2603343
pubmed:issue	1
pubmed:dateCreated	2003-1-21
pubmed:abstractText	There is an ongoing discussion on whether or not high beta(1)-adrenoceptor selectivity of beta-adrenoceptor antagonists may be favorable in the treatment of patients with heart failure. The present study compared the beta(1)-adrenoceptor selectivity of nebivolol and bisoprolol with that of carvedilol in the human myocardium, using a binding assay in conjunction with either the hydrophilic ligand (+/-)-[3H]4-(3-tertiarybutylamino-2-hydroxypropoxy)-benzimidazole-2-on HCl ([3H]CGP 12.177) or the lipophilic ligand [125I]iodocyanopindolol as radiolabeled compound. Measurements were made using membrane preparations obtained from identical nonfailing donor hearts. beta-adrenoceptor density was found to be slightly higher when [125I]iodocyanopindolol was used compared to [3H]CGP 12.177 (256+/-15 and 213+/-18 fmol/mg protein, respectively). When the highly beta(1)-adrenoceptor-selective compound 2-hydroxy-5-(2-(hydroxy-3-(4((1-methyl-4-trifluoromethyl)-1-H-imidazol-2-yl)-phenoxy)-propyl)-aminoethoxyl)-benzamide (CGP 20.712A) and the highly beta(2)-adrenoceptor-selective compound erythro-(+/-)-1-(7-methylindan-4-yloyl)-3-isopropylaminobutan-2-ol HCl (ICI 118.551) were used in competition experiments, a similar proportion of beta(1)-adrenoceptors was seen for [3H]CGP 12.177 (69.3+/-1.6%) and for [125I]iodocyanopindolol (67.0+/-2.1%). K(i)(beta(1)) and K(i)(beta(2)) were obtained in the presence of 50 nM ICI 118.551 and 300 nM CGP 20.712A. The rank order of beta(1)-adrenoceptor selectivity (K(i)(beta(2))/K(i)(beta(1)) ratio) was nebivolol (for [3H]CGP 12.177 46.1 and for [125I]iodocyanopindolol 22.5)>bisoprolol (13.1 and 6.4)>carvedilol (0.65 and 0.41). To investigate whether in vivo metabolized nebivolol retains high beta(1)-adrenoceptor selectivity, serum specimens were collected before and 2 h after oral administration of 5 mg nebivolol. The samples were used for [125I]iodocyanopindolol binding studies with the myocardial membrane preparations. In these samples, the binding of [125I]iodocyanopindolol to beta(1)-adrenoceptors was inhibited by 46.4+/-5.3%, whereas the binding to beta(2)-adrenoceptors was inhibited by 20.5+/-1.1% compared to that of control samples. It is concluded that nebivolol is approximately 3.5 times more beta(1)-adrenoceptor-selective than bisoprolol in the human myocardium. Furthermore, in vivo metabolized nebivolol retains beta(1)-adrenoceptor selectivity.
pubmed:language	eng
pubmed:journal	http://linkedlifedata.com/resource/pubmed/journal/1254354
pubmed:citationSubset	IM
pubmed:chemical	http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-1 Receptor..., http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-Antagonists, http://linkedlifedata.com/resource/pubmed/chemical/Benzopyrans, http://linkedlifedata.com/resource/pubmed/chemical/Bisoprolol, http://linkedlifedata.com/resource/pubmed/chemical/CGP 12177, http://linkedlifedata.com/resource/pubmed/chemical/Ethanolamines, http://linkedlifedata.com/resource/pubmed/chemical/Iodine Radioisotopes, http://linkedlifedata.com/resource/pubmed/chemical/Iodocyanopindolol, http://linkedlifedata.com/resource/pubmed/chemical/Propanolamines, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-1, http://linkedlifedata.com/resource/pubmed/chemical/Tritium, http://linkedlifedata.com/resource/pubmed/chemical/nebivolol
pubmed:status	MEDLINE
pubmed:month	Jan
pubmed:issn	0014-2999
pubmed:author	pubmed-author:BölckBirgitB, pubmed-author:BrixiusKlaraK, pubmed-author:BundkirchenAndreasA, pubmed-author:NguyenQuangQ, pubmed-author:SchwingerRobert H GRH
pubmed:issnType	Print
pubmed:day	26
pubmed:volume	460
pubmed:owner	NLM
pubmed:authorsComplete	Y
pubmed:pagination	19-26
pubmed:dateRevised	2010-11-18
pubmed:meshHeading	pubmed-meshheading:12535855-Adrenergic beta-1 Receptor Antagonists, pubmed-meshheading:12535855-Adrenergic beta-Antagonists, pubmed-meshheading:12535855-Adult, pubmed-meshheading:12535855-Benzopyrans, pubmed-meshheading:12535855-Binding Sites, pubmed-meshheading:12535855-Bisoprolol, pubmed-meshheading:12535855-Dose-Response Relationship, Drug, pubmed-meshheading:12535855-Ethanolamines, pubmed-meshheading:12535855-Female, pubmed-meshheading:12535855-Humans, pubmed-meshheading:12535855-Iodine Radioisotopes, pubmed-meshheading:12535855-Iodocyanopindolol, pubmed-meshheading:12535855-Male, pubmed-meshheading:12535855-Middle Aged, pubmed-meshheading:12535855-Myocardium, pubmed-meshheading:12535855-Propanolamines, pubmed-meshheading:12535855-Receptors, Adrenergic, beta-1, pubmed-meshheading:12535855-Tritium
pubmed:year	2003
pubmed:articleTitle	Beta 1-adrenoceptor selectivity of nebivolol and bisoprolol. A comparison of [3H]CGP 12.177 and [125I]iodocyanopindolol binding studies.
pubmed:affiliation	Laboratory of Muscle Research and Molecular Cardiology, Clinic III of Internal Medicine, University of Cologne, Joseph-Stelzmann-Strasse 9, 50924 Cologne, Germany.
pubmed:publicationType	Journal Article, Comparative Study, Research Support, Non-U.S. Gov't