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LY-487379 is a positive allosteric modulator of the metabotropic glutamate receptor mGluR2. EC50 = 1.7 μM. LY-487379 shows no intrinsic agonist or antagonist activity at hmGluR2 and has no activity at human mGluR3. LY-487379 markedly potentiates glutamate-stimulated [35S]GTPγS binding in a concentration-dependent manner at hmGluR2, shifting the glutamate dose-response curve leftward by 3-fold and increasing the maximum levels of [35S]GTPγS stimulation. LY-487379 has anxiolytic effects in fear-potentiated startle. This activity profile is useful in all symptom domains of schizophrenia.
| Molecular Weight | 488.91 |
| Formula | C21H19F3N2O4SHCl |
| CAS Number | 353229-59-1 |
| Solubility (25°C) | DMSO: ≥20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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