LY404039

SKU: orb1301143

Description

LY404039 (pomaglumetad) is a potent and selective agonist for the human metabotropic glutamate receptors mGlu2 and mGlu3. It has been utilized in preclinical research to investigate the role of these receptors in psychiatric and neurological disorders, including studies in both in vitro systems and animal models.

Research Area

Metabolism Research, Neuroscience

Key Properties

• CAS Number: 635318-11-5
• MW: 235.22
• Purity: 99.92% (May vary between batches)
• Formula: C₇H₉NO₆S
• SMILES: [H][C@@]12[C@@H](C(O)=O)[C@]1([H])S(=O)(=O)C[C@@]2(N)C(O)=O
• Target: Glucocorticoid Receptor,GluR
• Solubility: DMSO:Slightly soluble

Bioactivity

• Target IC50:
  mGlu2 (human recombinant):149 nM(Ki)|mGlu2/3 (rat neurons):88 nM(Ki)|mGlu3 (human recombinant):92 nM(Ki)
• In Vivo:
  LY404039 demonstrates higher plasma exposure and better oral bioavailability. LY404039 may be valuable in the treatment of neuropsychiatric disorders, including anxiety and psychosis. In wild-type animals, LY404039 significantly reverses d-amphetamine(AMP)-induced increase in ambulations, distance traveled, and reduced time spent at rest. LY404039 reverses phencyclidine (PCP)-evoked behaviors at 10 mg/kg. The antipsychotic-like effects of LY404039 on PCP and AMP-evoked behavioral activation are absent in mGlu2 and mGlu2/3 but not in mGlu3 receptor-deficient mice. In contrast, clozapine and risperidone inhibit PCP-evoked behaviors in both wild-type and mGlu2/3 receptor-deficient mice. LY404039 reduces responding on the EtOH in the pavlovian spontaneous recovery (PSR) test and reduces the expression of an alcohol deprivation effect (ADE) during relapse, but does not affect EtOH responding under maintenance conditions. LY404039 inhibits the expression of alcohol seeking and relapse behavior without altering alcohol self-administration behavior. Moreover, LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion. LY404039 could inhibit conditioned avoidance responding and also reduces fear-potentiated startle in rats and marble burying in mice. Importantly, LY404039 does not produce sedative effects or motor impairment in the conditioned avoidance task. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Recombinant human mGlu2, Recombinant human mGlu3, Rat neurons expressing native mGlu2/3, pomaglumetad, anxiolytic, antipsychotic, cAMP, GlucocorticoidReceptor, Glucocorticoid Receptor, L-glutamate, Inhibitor, inhibit, LY 404039, LY404039, LY-404039, mGluR, mGlu2, mGlu3, Metabotropic glutamate receptors

Compound Identifiers

PubChem CID

9834591