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LY3020371

Catalog No. T38791 CAS 1377615-75-2

LY3020371 is a highly potent and selective antagonist targeting the glutamate (mGlu) 2/3 receptor, showcasing excellent inhibition at Ki values of 5.26 nM and 2.50 nM for hmGluR2 and hmGluR3, respectively. With its remarkable affinity and specificity, LY3020371 serves as a valuable tool in depression research.

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LY3020371, CAS 1377615-75-2

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Description	LY3020371 is a highly potent and selective antagonist targeting the glutamate (mGlu) 2/3 receptor, showcasing excellent inhibition at Ki values of 5.26 nM and 2.50 nM for hmGluR2 and hmGluR3, respectively. With its remarkable affinity and specificity, LY3020371 serves as a valuable tool in depression research.
Targets&IC50	mGluR3 (human):2.50 nM (Ki), mGluR2 (human):5.26 nM (Ki)
In vitro	LY3020371, across a range of 0.1 nM to 100 μM, competitively inhibits the binding of the mGlu2/3 agonist ligand [3 H]-459477 with significant affinity[1]. At the same concentration range, it prevents DCG-IV from inhibiting forskolin-induced cAMP production in cells with recombinant human mGlu2 (IC50=16.2 nM) and mGlu3 (IC50=6.21 nM) receptors[1]. Additionally, LY3020371 demonstrates concentration-dependent antagonism towards LY379268-induced inhibition of cAMP formation across a span of 0.3-30,000 nM[1]. Furthermore, between 1-10,000 nM, it effectively counteracts the suppression of K+-induced glutamate release caused by LY379268, with an optimal effectiveness (IC50) at 86 nM[1]. In a similar concentration range (0.3-10,000 nM), it fully blocks the LY379268-induced suppression response, achieving an IC50 value of 33.9 nM[1].
In vivo	LY3020371, administered intravenously (i.v.) at doses ranging from 0.3 to 3 mg/kg, significantly increases the number of spontaneously active dopamine neurons in the ventral tegmental area (VTA) of rats. When given intraperitoneally (i.p.) at 1 to 10 mg/kg once a week for five weeks, it dose-dependently enhances tissue oxygen levels in the anterior cingulate cortex (ACC) of rats. A single i.p. dose of 10 mg/kg leads to an increase in monoamine efflux in the medial prefrontal cortex of freely moving rats. Moreover, a single i.v. administration of LY3020371 in doses ranging from 1 to 30 mg/kg elevates the cumulative wake time in rats in both a dose- and time-dependent manner, without causing rebound hypersomnolence. Additionally, doses from 0.1 to 10 mg/kg administered i.v. reduce the duration of immobility in the forced-swim test, indicating potential antidepressant activity. In a specific set-up using male Sprague-Dawley rats weighing between 230–350 g, dosages of 0.3, 1, and 3 mg/kg were administered via i.v. daily for five days per week over two weeks, resulting in an increased count of actively firing dopamine neurons in the VTA of anesthetized subjects.

Molecular Weight	359.34
Formula	C15H15F2NO5S
CAS No.	1377615-75-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Witkin JM, In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu 2/3 receptor antagonist. Neuropharmacology. 2017 Mar 15;115:100-114. 2. Witkin JM, et, al. Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 Antagonists, for the Treatment of Depression. J Pharmacol Exp Ther. 2017 Apr;361(1):68-86.

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Keywords

LY3020371 1377615-75-2 LY 3020371 LY-3020371 inhibitor inhibit

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