LY3020371 hydrochloride 

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with K_i 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].

LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [³H]-459477 with high affinity (hmGlu2 K_i=5.26 nM; hmGlu3 K_i=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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

395.81

C₁₅H₁₆ClF₂NO₅S

1377615-44-5

Solid

White to off-white

O=C([C@@]1(N)[C@]2([H])[C@@H](C(O)=O)[C@]2([H])[C@H](O)[C@H]1CSC3=CC=C(F)C(F)=C3)O.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [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;155:4  [Content Brief]

  [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.  [Content Brief]