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Fig. 1 · Structure
Cat. No.
A10544
CAS No.
635318-11-5
Formula
C7H9NO6S
Mol. Weight
235.2

Documents & Downloads

LY404039

mGluR Agonist

LY-404039 is a drug used in scientific research that acts as a selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. It has anxiolytic and antipsychotic effects in animal studies, but without causing sedation. Early human trials using a prodrug form of LY-404,039 called LY-214,0023 have also given encouraging results.

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Biological Activity

Target & Activity

Target Activity Value
Rat neurons expressing native mGlu2/3 Ki 88 nM
Recombinant human mGlu3 Ki 92 nM
Recombinant human mGlu2 Ki 149 nM

In Vitro Studies

Rat primary astrocytes were incubated with 100 µM LY404039 for 48 h in a design involving DETA/NO. The percentage of TUNEL-positive cells was lower with DETA/NO plus LY404039 than with DETA/NO alone. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

TUNEL-positive cells in primary astrocytes

Cell-based study · rat primary astrocytes [1]

Model: rat primary astrocytes. Treatment: 100 µM. Result: DETA/NO: 6.28±1.207; DETA/NO+LY404039: 4.87±0.623.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Percentage of TUNEL positive cells ± SEMPercentage of TUNEL positive cells 1 mM DETA/NO + 100 µM LY404039: Percentage of TUNEL positive cells ± SEM = 4.87±0.623[1]

Literature-Reported Treatment Conditions

Treatment concentration
100 µM
Exposure duration
48 h
Method
incubated
Co-treatment
Other interventions in this design: DETA/NO 1 mM. Compound effect isolated by the comparison: DETA/NO+LY404039 vs DETA/NO.
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: LY404039

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Treatments (S20); Materials and Methods > Microscopic determination of DNA fragmentation by terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay (S32, S33, S34, S35); Results > The Akt pathway (S92, S95); Figure 1 legend (S102); Table 1 (T1.h1, T1.r1)

Percentage of TUNEL positive cells ± SEM: Percentage of TUNEL positive cells ± SEM; comparator: DETA/NO — Materials and Methods > Treatments (S20); Table 1 (T1.h1, T1.r1)

In Vivo Studies

In male adult Sprague Dawley rats, acute oral LY404039 consistently decreased P1 amplitude to the second stimulus and lowered the S2/S1 ratio for P1 amplitude. In food-restricted male Lister-Hooded rats, subcutaneous LY404039 left functional checking unaffected in the Baseline vs. Dose vs. Rebaseline comparison. [2,3]

Second-Stimulus Amplitude in Rats

Animal study · male, adult Sprague Dawley rats [2]

In male adult Sprague Dawley rats, acute oral administration of LY404039 at 10 mg/kg consistently decreased P1 amplitude to the second stimulus.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
P1 amplitude to the second stimulusReported result LY404039 at the highest dose consistently decreased P1 amplitude to the second stimulus.[2]

Conditions shared by the study groups

Route
oral administration
Treatment course
acute administration
Vehicle
H2O + 1NaOH
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
LY404039 10 mg/kgvehicle (6)LY404039 at the highest dose consistently decreased P1 amplitude to the second stimulus.[2]
LY404039 10 mg/kg
Model: male, adult Sprague Dawley rats
Methods and source locations

Compound reported in the paper: LY404039

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Material and Methods > 1. Animal husbandry (S4); Material and Methods > 5. Drugs (S50); Results > 4. Effects of PQ-10 and LY404039 on the P1, N1 and P2 S2/S1 ratios > Peak amplitudes (S90); Fig 4 legend (S132)

P1 amplitude to the second stimulus: P1 amplitude to the second stimulus; comparator: vehicle (6) — Results > 4. Effects of PQ-10 and LY404039 on the P1, N1 and P2 S2/S1 ratios > Peak amplitudes (S90)

LY404039 10 mg/kg · Material and Methods > 5. Drugs (S50); Results > 4. Effects of PQ-10 and LY404039 on the P1, N1 and P2 S2/S1 ratios > Peak amplitudes (S90); Fig 4 legend (S132)

Functional Checking in Rats

Animal study · male Lister-Hooded rats [3]

Food-restricted male Lister-Hooded rats received LY404039 at 0.3 mg/kg subcutaneously 30 min prior to behavioural testing. Functional checking was unaffected in the Baseline vs. Dose vs. Rebaseline comparison.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
functional Observing Lever Presses (OLPs)Reported result Functional checking was similarly unaffected by the 0.3 mg/kg dose of LY404039 [Session: F(2,68) = 2.31, p =.11][3]

Conditions shared by the study groups

Route
subcutaneously
Treatment course
30 min prior to behavioural testing
Vehicle
1 ml/kg water double distilled vehicle injection
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
LY404039 0.3 mg/kgBaseline vs. Dose vs. RebaselineFunctional checking was similarly unaffected by the 0.3 mg/kg dose of LY404039 [Session: F(2,68) = 2.31, p =.11][3]
LY404039 0.3 mg/kg
Model: male Lister-Hooded rats
Methods and source locations

Compound reported in the paper: LY404039

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and methods > Subjects (S1, S5); Materials and methods > Drugs (S59); Materials and methods > Statistical analysis (S67); Results > The mGluR2/3 agonist LY404039 dose-dependently reduced checking behaviour (S115); Fig. 4 legend (S166)

functional Observing Lever Presses (OLPs): functional Observing Lever Presses (OLPs); comparator: Baseline vs. Dose vs. Rebaseline — Results > The mGluR2/3 agonist LY404039 dose-dependently reduced checking behaviour (S115); Fig. 4 legend (S166)

LY404039 0.3 mg/kg · Materials and methods > Drugs (S59); Results > The mGluR2/3 agonist LY404039 dose-dependently reduced checking behaviour (S115)

Stimulus Amplitude Ratio in Rats

Animal study · male, adult Sprague Dawley rats [2]

In male adult Sprague Dawley rats, acute oral administration of LY404039 at 10 mg/kg consistently lowered the S2/S1 ratio for P1 amplitude.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
S2/S1 ratio for the P1 amplitudeReported result LY404039 at the highest dose consistently lowered the S2/S1 ratio effect of p = 0.04[2]

Conditions shared by the study groups

Route
oral administration
Treatment course
acute administration
Vehicle
H2O + 1NaOH
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
LY404039 10 mg/kgvehicle (6)LY404039 at the highest dose consistently lowered the S2/S1 ratio effect of p = 0.04[2]
LY404039 10 mg/kg
Model: male, adult Sprague Dawley rats
Methods and source locations

Compound reported in the paper: LY404039

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Material and Methods > 1. Animal husbandry (S4); Material and Methods > 5. Drugs (S50); Results > 4. Effects of PQ-10 and LY404039 on the P1, N1 and P2 S2/S1 ratios > S2/S1 ratio (S92, S93); Fig 4 legend (S132)

S2/S1 ratio for the P1 amplitude: S2/S1 ratio for the P1 amplitude; comparator: vehicle (6) — Results > 4. Effects of PQ-10 and LY404039 on the P1, N1 and P2 S2/S1 ratios > S2/S1 ratio (S92, S93)

LY404039 10 mg/kg · Material and Methods > 5. Drugs (S50); Results > 4. Effects of PQ-10 and LY404039 on the P1, N1 and P2 S2/S1 ratios > S2/S1 ratio (S93); Fig 4 legend (S132)

Specifications

Manufacturer Adooq Bioscience
Actions Agonist
CAS Number 635318-11-5
Applications mGluR Agonist
Formula C7H9NO6S
Molecular Weight 235.2
SMILES
C1[C@]([C@@H]2[C@H]([C@@H]2S1(=O)=O)C(=O)O)(C(=O)O)N

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Durand D, Carniglia L, Caruso C, et al. Reduced cAMP, Akt activation and p65-c-Rel dimerization: mechanisms involved in the protective effects of mGluR3 agonists in cultured astrocytes. PLoS One (2011). PMID: 21779400 DOI: 10.1371/journal.pone.0022235 Source material
  2. [2] Ahnaou A, Biermans R, Drinkenburg WH. Modulation of mGlu2 Receptors, but Not PDE10A Inhibition Normalizes Pharmacologically-Induced Deviance in Auditory Evoked Potentials and Oscillations in Conscious Rats. PLoS One (2016). PMID: 26808689 DOI: 10.1371/journal.pone.0147365 Source material
  3. [3] McKenzie C, Sloot B, Amorim FE, et al. Agonism at mGluR2 receptors reduces dysfunctional checking on a rodent analogue of compulsive-like checking in obsessive compulsive disorder. Psychopharmacology (Berl) (2025). PMID: 40178609 DOI: 10.1007/s00213-025-06774-2 Source material

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