LSN2814617 是一种口服有效的、能透过血脑屏障的和选择性的mGlu5(代谢性谷氨酸 5) 正向别构调节剂 (PAM)，其EC50值为 52 nM (Human mGlu5) 和 42 nM (rat mGlu5)。LSN2814617 具有促醒作用。LSN2814617 可用于精神分裂症研究。
| 生物活性 | LSN2814617 is an orally active, potent, brain-penetrant, and selectivemGlu5(metabotropic glutamate 5) positive allosteric modulator (PAM), withEC50values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research[1]. |
| IC50& Target | rat mGluR5 42 ± 9 nM (IC50) | human mGluR5 52 ± 21 nM (IC50) |
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体外研究
(In Vitro) | 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[1].
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体内研究
(In Vivo) | LSN2814617 (0.3-60 mg/kg, Orally, once) displays significant unbound brain exposure and dose-dependent occupancy of the mGlu5 receptor[1].
LSN2814617 (0-10 mg/kg, Orally, once) significantly modulates amphetamine-induced locomotor hyperactivity[1].
LSN2814617 (0-3 mg/kg, Orally, once) markedly increase wakefulness[1].
| Animal Model: | Male Lister Hooded rats (180-250 g, four to eight per cage)[1] | | 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)[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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