LY354740, Eglumegad

For research purposes only

Cat. No BA94673145

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Description of biological activity

The compound is highly potent agonists for group 2/3 metabotropic glutamate receptors mGluR. (EC50 = 0.055 ± 0.017 μM for group 2 mGluR in the rat cerebral cortical slice preparation, suppression of forskolin-stimulated cAMP formation) possessing no activity at other glutamate receptor sites at concentrations up to 100 μM. Importantly, the mGluR agonist effects of the compound are evident following oral administration in mice in both the elevated plus maze model of anxiety (ED50 = 0.5 mg/kg) and in the ACPD-induced limbic seizure model (ED50 = 45.6 mg/kg) [J. Med. Chem. 1997, 40, 528-537]. mGlu2/3 receptors are targets for the treatment of anxiety, schizophrenia, convulsive disorders, Parkinson’s disease, pain, and neurodegeneration.

Therapeutic area

CNS Disorders

Biological target category

Glutamate receptors

TECHNICAL INFORMATION

(+)-(1S,2S,5R,6S)-2-aminobicyclo [3.1.0]hexane-2,6-dicarboxylic acid the compound is highly potent agonists for group 2/3 metabotropic glutamate receptors mGluR.

IUPAC Name: (+)-(1S,2S,5R,6S)-2-aminobicyclo [3.1.0]hexane-2,6-dicarboxylic acid

Chemical Formula: C8H11NO4

SMILES: N[C@]1(CC[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O

CAS Number: 176199-48-7

Molecular Weight: 185.179

Purity: > 96% chemical purity (LCMS)
>98% ee (NMR of a derivative)

Appearance: a white solid

Solubility: deionized water: soluble8 mg/mL(Aldrich) 10mM/1mL in DMSO(medchemexpress)

STORAGE AND HANDLING

Storage: Store at room temperature

Stability: Stable under normal conditions.

Shipping Conditions: Shipped at room temperature.

1H-NMR spectrum (click to enlarge)

REFERENCES

1. Neuropsychopharmacology 2004, 29, 502-513
2. J. Med. Chem. 2007, 50, 233-240
3. Synthesis 2006, 16, 2659-2664
4. Eur. J. Pharmacol. 2006, 544, 77-81

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