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Title: LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
Authors: Louis, Simon N S;Nero, Tracy L;Iakovidis, D;Jackman, G P;Louis, William J
Affiliation: Department of Clinical Pharmacology and Therapeutics Unit, The University of Melbourne, Austin and Repatriation Medical Centre, Heidelberg, Victoria, Australia.
Issue Date: 19-Feb-1999
Citation: European Journal of Pharmacology; 367(2-3): 431-5
Abstract: LK 204-545 ((+/-)-1-(2-(3-(2-cyano-4-(2-cyclopropyl-methoxy-ethoxy)phenoxy)-2-hydro xy-propyl-amino)-ethyl)-3-(4-hydrxy-phenyl) urea), an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-selective beta-adrenoceptor antagonists were examined to compare their radioligand binding affinities for human beta1-, beta2- and beta3-adrenoceptors transfected into CHO cells. LK 204-545 and CGP 20712A displayed the highest beta1-/beta2- (approximately 1800 and approximately 650, respectively) and beta1-/beta3-selectivity (approximately 17000 and approximately 2200, respectively) at human beta-adrenoceptors with LK 204-545 being approximately 2.75-fold more beta1-/beta2-selective and approximately 8-fold beta1-/beta3-selective than CGP 20712A. The high potency of LK 204-545 at transfected human beta1-adrenoceptors and in functional models of rat beta1-adrenoceptors together with its high selectivity, identify it as a useful ligand for studying beta1-adrenoceptors and suggest that it may be the preferred ligand for human beta-adrenoceptor studies.
Internal ID Number: 10079020
Type: Journal Article
Subjects: Adrenergic beta-Agonists.metabolism
Adrenergic beta-Antagonists.metabolism.pharmacology
CHO Cells
In Vitro Techniques
Protein Binding
Rats, Sprague-Dawley
Receptors, Adrenergic, beta.metabolism
Receptors, Adrenergic, beta-1.metabolism
Receptors, Adrenergic, beta-2.metabolism
Urea.analogs & derivatives.pharmacology
Appears in Collections:Journal articles

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