D-AP5 (Synonyms: D-2-Amino-5-Phosphonovaleric acid; D-APV) |
| Catalog No.GC16315 |
D-AP5 is a selective N-methyl-D-aspartate (NMDA) receptor antagonist with a Kd value of 1.4μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 79055-68-8
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 79055-68-8 | SDF | |
| Synonyms | D-2-Amino-5-Phosphonovaleric acid; D-APV | ||
| Chemical Name | (R)-2-amino-5-phosphonopentanoic acid | ||
| Canonical SMILES | OP(O)(CCC[C@H](C(O)=O)N)=O | ||
| Formula | C5H12NO5P | M.Wt | 197.13 |
| Solubility | PBS (pH 7.2): 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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