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  3. LY3020371

LY3020371 

目录号: HY-131289
产品使用指南

LY3020371 是一种有效和选择性的谷氨酸受体 (mGluR2/3) 拮抗剂,对 hmGluR2 和 hmGluR3 的 Ki 值分别为 5.26 和 2.50 nM。LY3020371 可用于抑郁症的研究。

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LY3020371 Chemical Structure

LY3020371 Chemical Structure

CAS No. : 1377615-75-2

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Description

LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression[1][2].

IC50 & Target[1]

hmGluR2

5.26 nM (Ki)

hmGluR3

2.50 nM (Ki)

In Vitro

LY3020371 (0.1 nM-100 μM) competitively displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity[1].
LY3020371 (0.1 nM-100 μM) blocks DCG-IV-induced inhibition of forskolin-stimulated cAMP production in cells expressing recombinant human mGlu2 (IC50=16.2 nM) and mGlu3 (IC50=6.21 nM) receptors[1].
LY3020371 (0.3-30000 nM) exhibits concentration-dependent antagonism of LY379268-inhibited cAMP formation[1].
LY3020371 (1-10000 nM) reverses LY379268-suppressed, K+-evoked glutamate release, with an IC50 of 86 nM[1].
LY3020371 (0.3-10000 nM) leads to a concentration-dependent and complete blockade of the LY379268-suppressed response, with an IC50 of 33.9 nM[1].

In Vivo

LY3020371 (0.3-3 mg/kg, a single i.v.) significantly increases the number of spontaneously active dopamine cells in the ventral tegmental area (VTA) of rats[2].
LY3020371 (1-10 mg/kg, i.p. once a week for 5 weeks) dose dependently increases tissue oxygen in the anterior cingulate cortex (ACC) of rats[2].
LY3020371 (10 mg/kg, a single i.p.) increases in monoamine efflux in the medial prefrontal cortex of freely moving rats[2].
LY3020371 (1-30 mg/kg, a single i.v.) increases the cumulative wake time of rats in a dose- and time-dependent manner without rebound hypersomnolence[2].
LY3020371 (0.1-10 mg/kg, a single i.v.) decrease the time rats are immobile in the forced-swim test in the rat forced-swim assay[2].

Animal Model: Male Sprague-Dawley rats (230-350 g)[1]
Dosage: 0.3, 1, 3 mg/kg
Administration: I.v. daily 5 days per week for 2 weeks
Result: Increased the number of actively firing dopamine neurons in the VTA of anesthetized rats.
Molecular Weight

359.35

Formula

C₁₅H₁₅F₂NO₅S

CAS No.

1377615-75-2

SMILES

O=C([C@@]1(N)[C@]2([H])[C@@H](C(O)=O)[C@]2([H])[C@H](O)[C@H]1CSC3=CC=C(F)C(F)=C3)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

LY3020371LY 3020371LY-3020371mGluRMetabotropic glutamate receptorsglutamatemGluR2/3depressionInhibitorinhibitorinhibit

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产品名称:
LY3020371
目录号:
HY-131289
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