| Field | Specification |
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| Target | |
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| Molecular weight | |
| Molecular formula | C15H15F2NO5S |
| SMILES | |
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Compound Overview
LY3020371 is a potent, selective antagonist of the metabotropic glutamate (mGlu) 2/3 receptors, with Ki values of 5.26 nM at hmGluR2 and 2.50 nM at hmGluR3. It can be used in depression research[1][2]. It has the molecular formula C15H15F2NO5S and a molecular weight of 359.35 g/mol.
Physical & Chemical Properties
| CAS Number | 1377615-75-2 |
|---|---|
| Molecular Formula | C15H15F2NO5S |
| Molecular Weight | 359.35 g/mol |
| 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 |
| Target | hmGluR2, hmGluR3 |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
hmGluR2 5.26 nM (Ki) |
hmGluR3 2.50 nM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
LY3020371 (0.1 nM-100 μM) displaces the mGlu2/3 agonist ligand [3H]-459477 from its binding sites competitively and with high affinity[1]. LY3020371 (0.1 nM-100 μM) prevents DCG-IV-induced inhibition of forskolin-stimulated cAMP production, with IC50=16.2 nM for mGlu2 and IC50=6.21 nM for mGlu3, in cells expressing the recombinant human receptors[1]. LY3020371 (0.3-30000 nM) antagonizes LY379268-inhibited cAMP formation in a concentration-dependent manner[1]. LY3020371 (1-10000 nM) reverses the LY379268-suppressed, K+-evoked glutamate release, with an IC50 of 86 nM[1]. LY3020371 (0.3-10000 nM) completely blocks the LY379268-suppressed response in a concentration-dependent manner, with an IC50 of 33.9 nM[1].
In Vivo
LY3020371 (0.3-3 mg/kg, a single i.v.) significantly raises how many dopamine cells are spontaneously active in the rat ventral tegmental area (VTA)[2]. Tissue oxygen in the anterior cingulate cortex (ACC) of rats rises dose dependently with LY3020371 (1-10 mg/kg, i.p., weekly for 5 weeks)[2]. In freely moving rats, LY3020371 (10 mg/kg, a single i.p.) elevates monoamine efflux in the medial prefrontal cortex[2]. Cumulative wake time in rats increases dose- and time-dependently with LY3020371 (1-30 mg/kg, a single i.v.), without rebound hypersomnolence[2]. In the rat forced-swim assay, LY3020371 (0.1-10 mg/kg, a single i.v.) shortens the period during which rats stay immobile in the forced-swim test[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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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bioRxiv. 2026 Feb 11.