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Biochem/physiol Actions
Potent glycine site-selective NMDA receptor antagonist with anticonvulsant efficacy in vivo.
CGP 78608 (PAMQX) is a potent glycine site-selective NMDA receptor antagonist (IC50 = 5 nM by competitive binding against 5 nM [3H]MDL 105,519; IC50 = 3/2.7 μM against AMPA/kainate, >10 μM against CGP39653 (glutamate site) and channel blocker MK-801) that exhibits anticonvulsant efficacy in mice in vivo (electroshock-induced convulsion ED50 = 12 mg/kg i.p.).
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Hygroscopic
| Quality Segment | 100 |
| assay | ≥97% |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (warmed) |
| storage temp. | -10 to -25°C |
| SMILES string | BrC1=CC(NC2=O)=C(C(CN[C@@H](P(O)(O)=O)C)=C1)NC2=O.Cl |
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¥ 5167.58
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