1377615-44-5
1377615-44-5 structure
- Name: LY3020371 hydrochloride
- Chemical Name: LY3020371 hydrochloride
- CAS Number: 1377615-44-5
- Molecular Formula: C15H16ClF2NO5S
- Molecular Weight: 395.81
- Catalog: Signaling Pathways GPCR/G Protein mGluR
- Create Date: 2019-09-08 07:19:16
- Modify Date: 2025-08-25 10:39:39
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LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM[1]. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo[2].
| Name | LY3020371 hydrochloride |
|---|
| Description | LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM[1]. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo[2]. |
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| Related Catalog | |
| Target |
mGluR2:5.3 nM (Ki) mGluR3:2.5 nM (Ki) |
| In Vitro | LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity (hmGlu2 Ki=5.26 nM; hmGlu3 Ki=2.50 nM)[1]. LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC50=16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC50=6.21 nM)[1]. LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca2+ oscillations (IC50=34 nM) and in an intact hippocampal slice preparation (IC50=46 nM)[1]. |
| In Vivo | LY3020371 hydrochloride (LY3020371.HCl) (Intravenous injection; 3-15 mg/kg) in rats leads to cerebrospinal fluid drug levels that are expected to effectively block mGlu2/3receptors[1]. LY3020371 hydrochloride (LY3020371) (intraperitoneal injection; 3 mg/kg, 10 mg/kg; 2 hours) has clear wake promoting effects, resulting in a large reduction in NREM sleep in the Wistar rats during the light phase[3]. |
| References |
| Molecular Formula | C15H16ClF2NO5S |
|---|---|
| Molecular Weight | 395.81 |