D-AP5
(Synonyms: (R)-(-)-2-氨基-5-膦酰戊酸,D-2-Amino-5-Phosphonovaleric acid; D-APV) 目录号 : GC16315D-AP5是一种选择性N-甲基-D-天门冬胺酸（NMDA）受体拮抗剂，Kd 值为1.4μM。
Cas No.:79055-68-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines | cortical astrocytes |
Preparation method | D-AP5(30μM) was added to cells 2 minutes before agonist application, followed by electrophysiological recordings. |
Reaction Conditions | 30μM; 2 min |
Applications | D-AP5 significantly reduces the increase in intracellular Ca2+ concentration caused by synaptically released glutamate. |
Animal experiment [2]: | |
Animal models | Male Lister hooded rats |
Preparation method | D-AP5 was infused via a chronic intracerebroventricular syringe pump for 14 days at a dose of 0.5 µg/µL and a continuous infusion rate of 1 µL/h. This chronic infusion maintains a constant drug concentration over a longer period of time. |
Dosage form | 0.5µg/µL at a rate of 1µL/h; i.c.v. |
Applications | Chronic infusion of D-AP5 significantly affected the spatial learning and memory abilities of rats. |
References: [1] Palygin O, Lalo U, Verkhratsky A, et al. Ionotropic NMDA and P2X1/5 receptors mediate synaptically induced Ca2+ signalling in cortical astrocytes[J]. Cell calcium, 2010, 48(4): 225-231. [2] Morris R G M, Steele R J, Bell J E, et al. N‐methyl‐d‐aspartate receptors, learning and memory: chronic intraventricular infusion of the NMDA receptor antagonist d‐AP 5 interacts directly with the neural mechanisms of spatial learning[J]. European Journal of Neuroscience, 2013, 37(5): 700-717. | |
D-AP5 is a selective N-methyl-D-aspartate (NMDA) receptor antagonist with a Kd value of 1.4μM[1]. D-AP5 inhibits the glutamate binding site of the NMDA receptor[2]. It can be used to study the role of NMDA receptors in neuropathology, particularly in neuroprotection[3].
In vitro, D-AP5 (30μM) treatment of cortical astrocytes significantly reduces the increase in intracellular Ca2+ concentration induced by synaptically released glutamate by inhibiting NMDA receptors[4]. D-AP5 (20μM) treatment of mouse hippocampal neurons significantly reduces NMDA-induced calcium influx and inhibits neuronal electrical activity, thereby protecting neurons from excitotoxic damage[5].
In vivo, D-AP5 (0.5µg/µL;1µL/h) administered via intracerebroventricular infusion to Lister hooded rats for 14 days significantly affected spatial learning and memory abilities, primarily by inhibiting NMDA receptor-mediated synaptic plasticity mechanisms and the formation of long-term potentiation (LTP)[6]. D-AP5 (5-10 nmol/µL; 0.5µL/h) administered via intracerebroventricular infusion in rats significantly inhibited LTP formation in the hippocampal CA1 region, resulting in memory impairment[7].
References:
[1] Evans R H, Francis A A, Jones A W, et al. The effects of a series of ω‐phosphonic α‐carboxylic amino acids on electrically evoked and excitant amino acid‐induced responses in isolated spinal cord preparations[J]. British journal of pharmacology, 1982, 75(1): 65-75.
[2] Choi D W, Koh J, Peters S. Pharmacology of glutamate neurotoxicity in cortical cell culture: attenuation by NMDA antagonists[J]. Journal of Neuroscience, 1988, 8(1): 185-196.
[3] Hwang J Y, Kim Y H, Ahn Y H, et al. N-Methyl-D-aspartate receptor blockade induces neuronal apoptosis in cortical culture[J]. Experimental neurology, 1999, 159(1): 124-130.
[4] Palygin O, Lalo U, Verkhratsky A, et al. Ionotropic NMDA and P2X1/5 receptors mediate synaptically induced Ca2+ signalling in cortical astrocytes[J]. Cell calcium, 2010, 48(4): 225-231.
[5] Benveniste M, Mienville J M, Sernagor E, et al. Concentration-jump experiments with NMDA antagonists in mouse cultured hippocampal neurons[J]. Journal of Neurophysiology, 1990, 63(6): 1373-1384.
[6] Morris R G M, Steele R J, Bell J E, et al. N‐methyl‐d‐aspartate receptors, learning and memory: chronic intraventricular infusion of the NMDA receptor antagonist d‐AP 5 interacts directly with the neural mechanisms of spatial learning[J]. European Journal of Neuroscience, 2013, 37(5): 700-717.
[7] Davis S, Butcher S P, Morris R G. The NMDA receptor antagonist D-2-amino-5-phosphonopentanoate (D-AP5) impairs spatial learning and LTP in vivo at intracerebral concentrations comparable to those that block LTP in vitro[J]. Journal of Neuroscience, 1992, 12(1): 21-34.
D-AP5是一种选择性N-甲基-D-天门冬胺酸（NMDA）受体拮抗剂，Kd 值为1.4μM[1]。D-AP5抑制NMDA受体的谷氨酸结合位点[2]。D-AP5可用于研究NMDA受体在神经病理学中的作用，特别是在神经保护方面[3]。
在体外，D-AP5（30μM）处理皮质星形胶质细胞，通过抑制NMDA受体，显著降低了由突触释放的谷氨酸引起的胞内Ca2+浓度的升高[4]。D-AP5（20μM）处理小鼠海马神经元细胞，显著减少了NMDA诱导的钙流入，并抑制神经元电活动，从而保护神经元免受过度兴奋性损伤[5]。
在体内，D-AP5（0.5µg/µL;1µL/h）通过脑室内输注治疗Lister hooded大鼠，持续14天后显著影响了大鼠的空间学习和记忆能力，主要通过抑制NMDA受体介导的突触可塑性机制来实现，抑制了长时程增强（LTP）的形成[6]。D-AP5（5-10 nmol/µL;0.5µL/h）通过脑室内输注治疗大鼠，显著抑制了海马CA1区的LTP形成，表现出记忆功能损伤[7]。
| Cas No. | 79055-68-8 | SDF | |
| 别名 | (R)-(-)-2-氨基-5-膦酰戊酸,D-2-Amino-5-Phosphonovaleric acid; D-APV | ||
| 化学名 | (R)-2-amino-5-phosphonopentanoic acid | ||
| Canonical SMILES | OP(O)(CCC[C@H](C(O)=O)N)=O | ||
| 分子式 | C5H12NO5P | 分子量 | 197.13 |
| 溶解度 | PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.0728 mL | 25.364 mL | 50.7279 mL |
| 5 mM | 1.0146 mL | 5.0728 mL | 10.1456 mL |
| 10 mM | 0.5073 mL | 2.5364 mL | 5.0728 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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