Discovery of the first potent and orally available agonist of the orphan G-protein-coupled receptor 52

…, Y Miyanohana, E Shiraishi, T Harasawa…

Index: Setoh, Masaki; Ishii, Naoki; Kono, Mitsunori; Miyanohana, Yuhei; Shiraishi, Eri; Harasawa, Toshiya; Ota, Hiroyuki; Odani, Tomoyuki; Kanzaki, Naoyuki; Aoyama, Kazunobu; Hamada, Teruki; Kori, Masakuni Journal of Medicinal Chemistry, 2014 , vol. 57, # 12 p. 5226 - 5237

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Citation Number: 6

Abstract

G-protein-coupled receptor 52 (GPR52) is an orphan Gs-coupled G-protein-coupled receptor. GPR52 inhibits dopamine D2 receptor signaling and activates dopamine D1/N- methyl-d-aspartate receptors via intracellular cAMP accumulation, and therefore, GPR52 agonists may have potential as a novel class of antipsychotics. A series of GPR52 agonists with a bicyclic core was designed to fix the conformation of the phenethyl ether moiety of ...