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编 号：F678659
分子式：C18H20FN5O
分子量：341.38
分子式：C18H20FN5O
分子量：341.38
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CAS No: 1313498-17-7
产品详情
生物活性：
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.
体内研究：
LSN2814617 (0.3-60 mg/kg, Orally, once) displays significant unbound brain exposure and dose-dependent occupancy of the mGlu5 receptor.LSN2814617 (0-10 mg/kg, Orally, once) significantly modulates amphetamine-induced locomotor hyperactivity.LSN2814617 (0-3 mg/kg, Orally, once) markedly increase wakefulness.Animal Model:Male Lister Hooded rats (180-250 g, four to eight per cage)
Dosage:0, 2.5, 5, and 10 mg/kg
Administration:Orally, once, 60 min before amphetamine
Result:Significantly modulated amphetamine hyperactivity, although a trend level decrease in hyperactivity was observed for the highest dose. At the end of the test session, from 75 to 120 min, the 10 mg/kg dose of LSN2814617 significantly increased amphetamine-induced hyperactivity.
Animal Model:Adult male Wistar rats (approximately 270 g)
Dosage:0, 0.3, 1, and 3 mg/kg
Administration:Orally, once
Result:Displayed dose-dependently increase in wakefulness immediately following oral administration; Produced 234 ± 16 min of increased wake for over 7 h in the case of 3 mg/kg. Produced dose-dependent reductions in both NREM and REM sleep.
体外研究：
LSN2814617 (1nM-10 μM) fails to elicit responses alone in rat cortical neurons, and evokes a concentration-dependent increase in the [Ca2+]i response in AV12 cells.
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.
体内研究：
LSN2814617 (0.3-60 mg/kg, Orally, once) displays significant unbound brain exposure and dose-dependent occupancy of the mGlu5 receptor.LSN2814617 (0-10 mg/kg, Orally, once) significantly modulates amphetamine-induced locomotor hyperactivity.LSN2814617 (0-3 mg/kg, Orally, once) markedly increase wakefulness.Animal Model:Male Lister Hooded rats (180-250 g, four to eight per cage)
Dosage:0, 2.5, 5, and 10 mg/kg
Administration:Orally, once, 60 min before amphetamine
Result:Significantly modulated amphetamine hyperactivity, although a trend level decrease in hyperactivity was observed for the highest dose. At the end of the test session, from 75 to 120 min, the 10 mg/kg dose of LSN2814617 significantly increased amphetamine-induced hyperactivity.
Animal Model:Adult male Wistar rats (approximately 270 g)
Dosage:0, 0.3, 1, and 3 mg/kg
Administration:Orally, once
Result:Displayed dose-dependently increase in wakefulness immediately following oral administration; Produced 234 ± 16 min of increased wake for over 7 h in the case of 3 mg/kg. Produced dose-dependent reductions in both NREM and REM sleep.
体外研究：
LSN2814617 (1nM-10 μM) fails to elicit responses alone in rat cortical neurons, and evokes a concentration-dependent increase in the [Ca2+]i response in AV12 cells.
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