| Bioactivity | 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]. |
| Target | pEC50: 7.53 (GPR52) |
| In Vivo | 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: |
| Name | GPR52 agonist-1 |
| CAS | 1207965-40-9 |
| Formula | C25H21ClFNO2S |
| Molar Mass | 453.96 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
GPR52 agonist-1
CAS: 1207965-40-9 F: C25H21ClFNO2S W: 453.96
GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of
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