Aryl propanolamines; comparison of activity at human β_3 receptors, rat β_3 receptors and rat atrial receptors mediating tachycardia

摘要

1. The in vitro activity of four aryl propanolamines was compared to two prototypic β_3 receptor agonists, CGP 12177 and CL316243 at the human β_3 receptor, the rat β_3 receptor in the stomach fundus and receptors mediating atrial tachycardia. 2. L-739,574 was the most potent (EC_50 = 9 nM) and selective agonist at the human β_3 receptor with high maximal response (74/100 of the maximal response to isoproterenol).