1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. LY3027788

LY3027788 

Cat. No.: HY-117606
Handling Instructions

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

For research use only. We do not sell to patients.

LY3027788 Chemical Structure

LY3027788 Chemical Structure

CAS No. : 1377615-76-3

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Description

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

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.
Molecular Weight

591.58

Formula

C₂₅H₃₁F₂NO₁₁S

CAS No.

1377615-76-3

SMILES

O=C([[email protected]@]1(N)[[email protected]]2([H])[[email protected]@H](C(OCOC(OC(C)C)=O)=O)[[email protected]]2([H])[[email protected]](O)[[email protected]]1CSC3=CC=C(F)C(F)=C3)OCOC(OC(C)C)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

LY3027788LY 3027788LY-3027788mGluRMetabotropic glutamate receptorsLY3020371mGlu2/3prodrugantidepressantInhibitorinhibitorinhibit

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LY3027788
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HY-117606
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