Louis S N, Nero T L, Iakovidis D, Jackman G P, Louis W J
Department of Clinical Pharmacology and Therapeutics Unit, The University of Melbourne, Austin and Repatriation Medical Centre, Heidelberg, Victoria, Australia.
Eur J Pharmacol. 1999 Feb 19;367(2-3):431-5. doi: 10.1016/s0014-2999(99)00019-9.
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.
LK 204 - 545（（±）-1 - （2 - （3 - （2 - 氰基 - 4 - （2 - 环丙基甲氧基 - 乙氧基）苯氧基） - 2 - 羟基 - 丙基氨基） - 乙基） - 3 - （4 - 羟基 - 苯基）脲）是一种在大鼠中具有高β1/β2选择性的拮抗剂，研究了一系列心脏选择性和非选择性β - 肾上腺素能受体拮抗剂，以比较它们对转染到CHO细胞中的人β1、β2和β3肾上腺素能受体的放射性配体结合亲和力。LK 204 - 545和CGP 20712A在人β - 肾上腺素能受体上表现出最高的β1/β2选择性（分别约为1800和约650）和β1/β3选择性（分别约为17000和约2200），LK 204 - 545的β1/β2选择性比CGP 20712A高约2.75倍，β1/β3选择性高约8倍。LK 204 - 545在转染的人β1 - 肾上腺素能受体和大鼠β1 - 肾上腺素能受体功能模型中具有高效能及其高选择性，使其成为研究β1 - 肾上腺素能受体的有用配体，并表明它可能是人β - 肾上腺素能受体研究的首选配体。
