LY3020371 hydrochloride structure
|
Common Name | LY3020371 hydrochloride | ||
|---|---|---|---|---|
| CAS Number | 1377615-44-5 | Molecular Weight | 395.81 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C15H16ClF2NO5S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of LY3020371 hydrochlorideLY3020371 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]. |
|---|---|
| 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 |
| InChIKey | XETSGLSGWGGOTN-JPWNOPPSSA-N |
| SMILES | Cl.NC1(C(=O)O)C(CSc2ccc(F)c(F)c2)C(O)C2C(C(=O)O)C21 |