PW0787

PW0787 is a potent, selective, orally bioavailable, and brain-penetrant allosteric agonist of the orphan G protein-coupled receptor GPR52 (EC50 = 135 nM). Developed by researchers at the University of Texas Medical Branch, PW0787 activates Gs/olf-mediated cAMP signaling by binding to an allosteric site near extracellular loop 2 (ECL2) of GPR52. In preclinical studies, PW0787 has been shown to excite dopamine D2 pathway medium spiny neurons (D2 MSNs) in the nucleus accumbens and functionally oppose dopamine D2 receptor signaling. In animal models, PW0787 dose-dependently suppresses amphetamine-induced hyperlocomotion, demonstrating antipsychotic-like activity. It is being investigated as a potential therapeutic candidate for central nervous system disorders, including schizophrenia and substance use disorders.

Other names

1-(6-(3-fluoro-5-(trifluoromethyl)benzyl)pyrimidin-4-yl)-N-(2-hydroxyethyl)indoline-4-carboxamidecompound 12ccompound12ccompound-12c