2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. LSN2814617

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。

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LSN2814617 Chemical Structure

LSN2814617 Chemical Structure

CAS No. : 1313498-17-7

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LSN2814617 相关抗体

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

LSN2814617 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.
纯度 & 产品资料
参考文献

LSN2814617 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LSN28146171313498-17-7LSN 2814617LSN-2814617mGluRMetabotropic glutamate receptorsGlutamateNMDAN-methyl-d-aspartateSchizophreniaPsychosiswake-promotingInhibitorinhibitorinhibit

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产品名称：
LSN2814617
目录号：
HY-118256
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