LY3020371_product_DataBase

Bioactivity	LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression[1][2].
Invitro	LY3020371 (0.1 nM-100 μM) competitively displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity[1].LY3020371 (0.1 nM-100 μM) blocks DCG-IV-induced inhibition of forskolin-stimulated cAMP production in cells expressing recombinant human mGlu2 (IC50=16.2 nM) and mGlu3 (IC50=6.21 nM) receptors[1].LY3020371 (0.3-30000 nM) exhibits concentration-dependent antagonism of LY379268-inhibited cAMP formation[1].LY3020371 (1-10000 nM) reverses LY379268-suppressed, K+-evoked glutamate release, with an IC50 of 86 nM[1].LY3020371 (0.3-10000 nM) leads to a concentration-dependent and complete blockade of the LY379268-suppressed response, with an IC50 of 33.9 nM[1].
In Vivo	LY3020371 (0.3-3 mg/kg, a single i.v.) significantly increases the number of spontaneously active dopamine cells in the ventral tegmental area (VTA) of rats[2].LY3020371 (1-10 mg/kg, i.p. once a week for 5 weeks) dose dependently increases tissue oxygen in the anterior cingulate cortex (ACC) of rats[2].LY3020371 (10 mg/kg, a single i.p.) increases in monoamine efflux in the medial prefrontal cortex of freely moving rats[2].LY3020371 (1-30 mg/kg, a single i.v.) increases the cumulative wake time of rats in a dose- and time-dependent manner without rebound hypersomnolence[2].LY3020371 (0.1-10 mg/kg, a single i.v.) decrease the time rats are immobile in the forced-swim test in the rat forced-swim assay[2]. Animal Model:
Name	LY3020371
CAS	1377615-75-2
Formula	C15H15F2NO5S
Molar Mass	359.35
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Witkin JM, In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu 2/3 receptor antagonist. Neuropharmacology. 2017 Mar 15;115:100-114. [2]. Witkin JM, et, al. Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 A [3]. Witkin JM, et, al. mGlu2/3 receptor antagonism: A mechanism to induce rapid antidepressant effects without ketamine-associated side-effects. Pharmacol Biochem Behav. 2020 Mar;190:172854.

PeptideDB

LY3020371

CAS: 1377615-75-2 F: C15H15F2NO5S W: 359.35