GPR52 agonist-1

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[1].

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

pEC50: 7.53 (GPR52)[1]

GPR52 agonist-1 (compound 7m) (3, 10, and 30 mg/kg; PO; single dosage) attenuates Methamphetamine-induced hyperlocomotion in mice[1]. GPR52 agonist-1 (0.1 mg/kg, IV and 1 mg/kg, PO; single dosage) exhibits good oral pharmacokinetic profile with an Cmax of 108.1 ng/mL, an AUC0-8h of 613.7 ng·h/mL, and an F (bioavailability) of 73% in mouse[1]. Animal Model: Male ICR mice (7-8 weeks; subcutaneously injected with 2 mg/kg Methamphetamine after 60 min administration)[1] Dosage: 3, 10, and 30 mg/kg Administration: PO; single dosage Result: Attenuated Methamphetamine-induced hyperlocomotion dose-dependently. Did not show significant cataleptogenic effects even at a dose of 100 mg/kg and had a low risk of extrapyramidal side effects.

[1]. Setoh M, et al. Discovery of the first potent and orally available agonist of the orphan G-protein-coupled receptor 52. J Med Chem. 2014 Jun 26;57(12):5226-37.