(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID Basic information
- Product Name:
- (E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
- Synonyms:
-
- dl-2-amino-4-methyl-5-phosphono-3-*pentenoic acid
- (3E)-2-Amino-4-methyl-5-phosphono-3-pentanoic acid
- (E)-2-Amino-4-methyl-5-phosphonopent-3-enoic acid
- (E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
- CGP 37849
- (E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
- CGP 37849;CGP-37849;CGP37849
- 3-Pentenoic acid, 2-amino-4-methyl-5-phosphono-, (3E)-
- CAS:
- 127910-31-0
- MF:
- C6H12NO5P
- MW:
- 209.14
- Product Categories:
-
- Glutamate receptor
- Glutamate
- Mol File:
- 127910-31-0.mol
(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID Chemical Properties
- 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
(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID Usage And Synthesis
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
Desiccate at +4°C
(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACIDSupplier
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(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID(127910-31-0)Related Product Information
- (2R,3E)-2-Amino-4-methyl-5-phosphono-3-pentenoic acid
- 2-amino-4-methyl-5-phosphono-3-pentenoic acid
- (2R,3E)-2-Amino-4-methyl-5-phosphono-3-pentenoic acid 1-ethyl ester
- (2S,3E)-2-Amino-4-methyl-5-phosphono-3-pentenoic acid
- (2S,3E)-2-Amino-4-methyl-5-phosphono-3-pentenoic acid 1-ethyl ester
- 2-AMINO-3-BUTENOIC ACID
- ALLYLPHOSPHONIC ACID
- CGP 39653, [PROPYL-2,3,3H]-
- (E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
- (E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID ETHYL ESTER,(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID ETHYLESTHER