1. GPCR/G Protein
    Neuronal Signaling
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  3. LY3020371

LY3020371 

Cat. No.: HY-131289
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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.

For research use only. We do not sell to patients.

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
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Storage

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

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Keywords:

LY3020371LY 3020371LY-3020371mGluRMetabotropic glutamate receptorsglutamatemGluR2/3depressionInhibitorinhibitorinhibit

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