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LY3020371 hydrochloride

Catalog No. T11911 CAS 1377615-44-5

LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. 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.

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LY3020371 hydrochloride Chemical Structure

LY3020371 hydrochloride, CAS 1377615-44-5

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Description	LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. 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.
Targets&IC50	mGluR3:2.5 nM (ki), mGluR2:5.3 nM (ki)
In vitro	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].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].
In vivo	LY3020371 hydrochloride (LY3020371) administered via intraperitoneal injection at doses of 3 mg/kg and 10 mg/kg, 2 hours prior, significantly promotes wakefulness, notably decreasing NREM sleep in Wistar rats during the light phase[3]. Intravenous administration of LY3020371 hydrochloride at a dosage range of 3-15 mg/kg in rats results in cerebrospinal fluid concentrations predicted to efficiently inhibit mGlu2/3 receptors[1].

Molecular Weight	395.81
Formula	C15H16ClF2NO5S
CAS No.	1377615-44-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Witkin JM, et al. In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist. Neuropharmacology. 2017 Mar 15;115:100-114. 2. Witkin JM, et al. Preclinical predictors that the orthosteric mGlu2/3 receptor antagonist LY3020371 will not engender ketamine-associated neurotoxic, motor, cognitive, subjective, or abuse-liability-related effects. Pharmacol Biochem Behav. 2017 Apr;155:43-55. 3. Wood CM, et al. Investigating the role of mGluR2 versus mGluR3 in antipsychotic-like effects, sleep-wake architecture and network oscillatory activity using novel Han Wistar rats lacking mGluR2 expression. Neuropharmacology. 2018 Sep 15;140:246-259.

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Keywords

LY3020371 hydrochloride 1377615-44-5 Neuroscience GluR LY-3020371 Hydrochloride LY 3020371 Hydrochloride LY-3020371 hydrochloride LY3020371 Hydrochloride inhibitor inhibit

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