LY3020371
Based on 1 publication(s) in Google Scholar
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.
- CAS No.: 1377615-75-2
- Formula: C15H15F2NO5S
- Molecular Weight:359.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) LY3020371
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Biological Activity
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hmGluR2 5.26 nM (Ki) |
hmGluR3 2.50 nM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (230-350 g)[1]
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Dosage:0.3, 1, 3 mg/kg
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Administration:I.v. daily 5 days per week for 2 weeks
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Result:Increased the number of actively firing dopamine neurons in the VTA of anesthetized rats.
Chemical Information
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CAS No. 1377615-75-2
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Molecular Weight 359.35
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Formula C15H15F2NO5S
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Purity & Documentation
References
[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. [Content Brief]
[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 A [Content Brief]
[3]. Witkin JM, et, al. mGlu2/3 receptor antagonism: A mechanism to induce rapid antidepressant effects without ketamine-associated side-effects. Pharmacol Biochem Behav. 2020 Mar;190:172854. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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