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LSN2814617
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LSN2814617图片
CAS NO:1313498-17-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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].

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.
分子量

341.38

Formula

C18H20FN5O

CAS 号

1313498-17-7

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.