LY3020371 hydrochloride 是一种有效的选择性代谢型谷氨酸 2/3 受体 (mGlu2/3) 拮抗剂，K_i 值分别为 5.3 nM 和 2.5 nM。LY3020371 hydrochloride 有效阻断 cAMP 形成，IC₅₀ 值为 16.2 nM。LY3020371 hydrochloride 在体内具有抗抑郁样特性。

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 IC 50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.

Solid

mGluR2 5.3 nM (Ki) mGluR3 2.5 nM (Ki)

LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [H]-459477 with high affinity (hmGlu2 Ki=5.26 nM; hmGlu3 Ki=2.50 nM).
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).
LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca oscillations (IC50=34 nM) and in an intact hippocampal slice preparation (IC50=46 nM).
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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur 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.
[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

In Vitro: DMSO : 250 mg/mL (631.62 mM; Need ultrasonic)配制储备液