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编 号：F743137
分子式：C25H21ClFNO2S
分子量：453.96
分子式：C25H21ClFNO2S
分子量：453.96
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CAS No: 1207965-40-9
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生物活性：
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.
体内研究：
GPR52 agonist-1 (compound 7m) (3, 10, and 30 mg/kg; PO; single dosage) attenuates Methamphetamine-induced hyperlocomotion in mice.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.Animal Model:Male ICR mice (7-8 weeks; subcutaneously injected with 2 mg/kg Methamphetamine after 60 min administration)
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.
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.
体内研究：
GPR52 agonist-1 (compound 7m) (3, 10, and 30 mg/kg; PO; single dosage) attenuates Methamphetamine-induced hyperlocomotion in mice.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.Animal Model:Male ICR mice (7-8 weeks; subcutaneously injected with 2 mg/kg Methamphetamine after 60 min administration)
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.
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