(E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
| 中文名称 | (E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID |
|---|---|
| 中文同义词 | (E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸;化合物 T7720;化合物 CGP 37849;CGP 37849,COMPETITIVE NMDA拮抗剂;(E)-2-氨基-4-甲基-5-膦酰基戊-3-烯酸 |
| 英文名称 | (E)-(+/-)-2-Amino-4-methyl-5-phosphono-3-pentenoic acid |
| 英文同义词 | 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;CGP 37849;CGP-37849;CGP37849;3-Pentenoic acid, 2-amino-4-methyl-5-phosphono-, (3E)-;CGP 37849, competitive NMDA antagonist |
| CAS号 | 127910-31-0 |
| 分子式 | C6H12NO5P |
| 分子量 | 209.14 |
| EINECS号 | |
| 相关类别 | Glutamate receptor;Glutamate |
| Mol文件 | 127910-31-0.mol |
| 结构式 |  |
(E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID 性质
| 沸点 | 523.1±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.506±0.06 g/cm3(Predicted) |
| 储存条件 | Desiccate at +4°C |
| 溶解度 | 在水中的溶解度为≥2mg/mL（加热） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 1.83±0.10(Predicted) |
| 颜色 | 白色至米色 |
| 水溶解性 | H2O: 100mM |
| InChI | 1S/C6H12NO5P/c1-4(3-13(10,11)12)2-5(7)6(8)9/h2,5H,3,7H2,1H3,(H,8,9)(H2,10,11,12)/b4-2+ |
| InChIKey | BDYHNCZIGYIOGJ-DUXPYHPUSA-N |
| SMILES | C\C(CP(O)(O)=O)=C/C(N)C(O)=O |
In the hippocampal slice in vitro, CGP 37849 selectively and reversibly antagonizes NMDA-evoked increases in CA1 pyramidal cell firing rate. In slices bathed in medium containing low Mg 2+ levels, concentrations of CGP 37849 up to 10 μM suppresses burst firing evoked in CA1 neurones by stimulation of Schaffer collateral-commissural fibres without affecting the magnitude of the initial population spike.
CGP 37849 potently (
K
i
of 220 nM) and competitively inhibits NMDA-sensitive l-[
3
H]-glutamate binding to postsynaptic density (PSD) fractins from rat brain. CGP 37849 inhibits the binding of the selective NMDA receptor antagonist, [
3
H]-(±)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonate (CPP), with a
K
i
of 35 nM.
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.
Oral administration to mice of CGP 37849 suppresses maximal electroshock-induced seizures in mice with an
ED
50
of 21 mg/kg.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-107702 | (E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID CGP 37849 | 127910-31-0 | 1mg | 1550元 |
| 2026/06/05 | HY-107702 | (E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID CGP 37849 | 127910-31-0 | 5mg | 3850元 |