GPR52 Agonist

NXE0041178 is an orally active and BBB-penetrant full GPR52 agonist, with a pEC₅₀ of 7.5 for human GPR52 and an EC₅₀ of 27.5 nM (pEC₅₀ = 7.55) for rat GPR52. NXE0041178 shows no significant inhibition on hERG, hNaV1.5 and cytochrome P450 isoforms. NXE0041178 can reduce d-amphetamine-induced hyperactivity in rats. NXE0041178 can be used for research of Neurological disease.

GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC₅₀ value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity.

R-185 is an orally active and brain-penetrant GPR52 agonist. R-185 activates GPR52 to increase intracellular cAMP levels. R-185 can be used for the research of schizophrenia.

PW0729 is a selective GPR52 agonist. PW0729 activates G protein/cAMP signaling pathway, with bias toward this pathway over β-arrestin recruitment, and induces GPR52 desensitization. PW0729 can be used for the research of neuropsychiatric and neurological diseases.