For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I018732 |
| CAS Number | 1377615-44-5 |
| Synonyms | (1S,2R,3S,4S,5R,6R)-2-amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylic acid;hydrochloride |
| Molecular Formula | C15H16ClF2NO5S |
| Purity | ≥95% |
| InChI | InChI=1S/C15H15F2NO5S.ClH/c16-7-2-1-5(3-8(7)17)24-4-6-12(19)9-10(13(20)21)11(9)15(6,18)14(22)23;/h1-3,6,9-12,19H,4,18H2,(H,20,21)(H,22,23);1H/t6-,9+,10+,11+,12-,15+;/m1./s1 |
| InChIKey | XETSGLSGWGGOTN-JPWNOPPSSA-N |
| SMILES | C1=CC(=C(C=C1SCC2C(C3C(C3C2(C(=O)O)N)C(=O)O)O)F)F.Cl |
| Reference | [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 [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. |
