1377615-75-2
1377615-75-2 structure
- Name: LY3020371
- Chemical Name: LY3020371
- CAS Number: 1377615-75-2
- Molecular Formula: C15H15F2NO5S
- Molecular Weight: 359.35
- Catalog: Signaling Pathways GPCR/G Protein mGluR
- Create Date: 2020-11-28 16:21:11
- Modify Date: 2024-01-14 15:25:02
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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[1][2].
| Name | LY3020371 |
|---|
| 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]. |
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| Related Catalog | |
| Target |
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. |
| References |
| Molecular Formula | C15H15F2NO5S |
|---|---|
| Molecular Weight | 359.35 |