| Identification | Back Directory | [Name]
Benzamide, 3-[2-[(3-chloro-5-fluorophenyl)methyl]benzo[b]thien-7-yl]-N-(2-methoxyethyl)- | [CAS]
1207965-40-9 | [Synonyms]
GPR52 agonist-1
3-(2-(3-Chloro-5-fluorobenzyl)benzo[b]thiophen-7-yl)-N-(2-methoxyethyl)benzamide
Benzamide, 3-[2-[(3-chloro-5-fluorophenyl)methyl]benzo[b]thien-7-yl]-N-(2-methoxyethyl)- | [Molecular Formula]
C25H21ClFNO2S | [MOL File]
1207965-40-9.mol | [Molecular Weight]
453.96 |
| Chemical Properties | Back Directory | [Boiling point ]
627.4±55.0 °C(Predicted) | [density ]
1.283±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
14.08±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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: | 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. |
| [References]
[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. DOI:10.1021/jm5002919 |
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