LY3020371 hydrochloride
Names
[ CAS No. ]:
1377615-44-5
[ Name ]:
LY3020371 hydrochloride
Biological Activity
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C15H16ClF2NO5S
[ Molecular Weight ]:
395.81