LY3027788 hydrochloride

Modify Date: 2025-08-22 19:00:01

LY3027788 hydrochloride Structure
LY3027788 hydrochloride structure
Common Name LY3027788 hydrochloride
CAS Number 1377615-55-8 Molecular Weight 628.04
Density N/A Boiling Point N/A
Molecular Formula C25H32ClF2NO11S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of LY3027788 hydrochloride


LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy[1][2].

 Names

Name LY3027788 hydrochloride

 LY3027788 hydrochloride Biological Activity

Description LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy[1][2].
Related Catalog
Target

mGluR2

mGluR3

In Vitro LY3027788 (4.8-27 mg/kg; a single p.o.) produces antidepressant-like decreases in immobility times in the forced-swim test in mice[1]. LY3027788 (4.8-16 mg/kg; a single p.o.) enhances the locomotor stimulant effects of quinpirole at the dose of 16 mg/kg in the locomotor activity assay in mice[1]. LY3027788 (10-30 mg/kg; a single p.o.) dose dependently increases the wake time of rats without engendering rebound hypersomnolence[1]. LY3027788 (a single p.o.) leads to the rapid and dose-proportionate appearance of the pharmacologically active species LY3020371 in plasma of both mouse (4.8-27 mg/kg) and rat (3-30 mg/kg)[1].
In Vivo LY3027788 (4.8-27 mg/kg; a single p.o.) produces antidepressant-like decreases in immobility times in the forced-swim test in mice[1]. LY3027788 (4.8-16 mg/kg; a single p.o.) enhances the locomotor stimulant effects of quinpirole at the dose of 16 mg/kg in the locomotor activity assay in mice[1]. LY3027788 (10-30 mg/kg; a single p.o.) dose dependently increases the wake time of rats without engendering rebound hypersomnolence[1]. LY3027788 (a single p.o.) leads to the rapid and dose-proportionate appearance of the pharmacologically active species LY3020371 in plasma of both mouse (4.8-27 mg/kg) and rat (3-30 mg/kg)[1]. Animal Model: Male Sprague-Dawley mice (20-25 g)[1] Dosage: 4.8, 16, 27 mg/kg Administration: A single p.o. (60 minutes prior to testing) Result: Potent and efficacious with a minimal effective dose of 16 mg/kg in the mouse forced-swim assay. The ED60 was 8.2 mg/kg.
References

[1]. 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 Antagonists, for the Treatment of Depression. J Pharmacol Exp Ther. 2017 Apr;361(1):68-86.

[2]. 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.

 Chemical & Physical Properties

Molecular Formula C25H32ClF2NO11S
Molecular Weight 628.04
InChIKey FUEQYOZWBYVZQM-GSLULZTOSA-N
SMILES CC(C)OC(=O)OCOC(=O)C1C2C(O)C(CSc3ccc(F)c(F)c3)C(N)(C(=O)OCOC(=O)OC(C)C)C12.Cl
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