Identification | Back Directory | [Name]
(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID | [CAS]
127910-31-0 | [Synonyms]
CGP 37849 CGP 37849;CGP-37849;CGP37849 dl-2-amino-4-methyl-5-phosphono-3-*pentenoic acid (E)-2-Amino-4-methyl-5-phosphonopent-3-enoic acid (3E)-2-Amino-4-methyl-5-phosphono-3-pentanoic acid (E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID 3-Pentenoic acid, 2-amino-4-methyl-5-phosphono-, (3E)- (E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID | [Molecular Formula]
C6H12NO5P | [MDL Number]
MFCD00153906 | [MOL File]
127910-31-0.mol | [Molecular Weight]
209.14 |
Chemical Properties | Back Directory | [Boiling point ]
523.1±60.0 °C(Predicted) | [density ]
1.506±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at +4°C | [solubility ]
H2O: ≥2mg/mL (warmed) | [form ]
powder | [pka]
1.83±0.10(Predicted) | [color ]
white to beige | [Water Solubility ]
H2O: 100mM |
Hazard Information | Back Directory | [Uses]
CGP 37849 is a potent antagonist at NMDA receptors which results in anticonvulsant activity (1). In addition, it may antagonize NMDA-antagonistic induced antianxiety effects (2). | [Biological Activity]
Potent, selective and competitive NMDA receptor antagonist (K i = 35 nM). Anticonvulsive following oral administration in vivo . | [in vivo]
CGP 37849 potently (Ki of 220 nM) and competitively inhibits NMDA-sensitive l-[3H]-glutamate binding to postsynaptic density (PSD) fractins from rat brain. CGP 37849 inhibits the binding of the selective NMDA receptor antagonist, [3H]-(±)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonate (CPP), with a Ki of 35 nM[1].
In vivo, oral administration to rats of CGP 37849 selectively blocks firing in hippocampal neurones induced by ionophoretically-applied NMDA, without affecting the responses to quisqualate or kainate[1].
Oral administration to mice of CGP 37849 suppresses maximal electroshock-induced seizures in mice with an ED50 of 21 mg/kg[1]. | [IC 50]
NMDA Receptor | [storage]
Store at -20°C |
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