LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptorpositive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM)[1].
In HEK293 cells transiently expressing human, dog, rhesus monkey, and mouse D1 receptors, the EC50s of LY3154207 are 2.3 nM, 2.0 nM, 2.5 nM, and 62.1 nM, respectively[1].
[1]. Hao J, Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor. J Med Chem. 2019 Oct 10;62(19):8711-8732.