Please use this identifier to cite or link to this item:
|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. firstname.lastname@example.org|
|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|
In Vitro Techniques
Receptors, Adrenergic, beta.metabolism
Receptors, Adrenergic, beta-1.metabolism
Receptors, Adrenergic, beta-2.metabolism
Urea.analogs & derivatives.pharmacology
|Appears in Collections:||Journal articles|
Files in This Item:
There are no files associated with this item.
Items in AHRO are protected by copyright, with all rights reserved, unless otherwise indicated.