D-AP5
(Synonyms: (R)-(-)-2-氨基-5-膦酰戊酸,D-2-Amino-5-Phosphonovaleric acid; D-APV) 目录号 : GC16315A selective NMDA antagonist
Cas No.:79055-68-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
Neonatal slices, juvenile slices |
Preparation method |
Soluble to 100 mM in sterile water. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
100 μM |
Applications |
In neonatal slices, a 5 Hz/3 min train of stimuli did not induce LTD of field EPSPs in the presence of 100 μM D-AP5. In juvenile slices, a 5 Hz/3 min train of stimuli did not induce LTD of field EPSPs in the presence of 100 μM D-AP5. In the presence of 100 μM D-AP5, voltage-clamping the cells at -80 mV during the induction protocol prevented the induction of mGluR-LTD. |
Animal experiment [2,3]: | |
Animal models |
Rats |
Dosage form |
0–50 mM |
Application |
In rats, D-AP5 (0–50 mM) via osmotic minipumps impaired spatial learning in a linear dose-dependent manner, highly correlated with its corresponding impairment of hippocampal LTP. No concentration of D-AP5 was observed to block LTP without affecting learning. Acute intrahippocampal infusion of radiolabelled D-AP5 revealed relatively restricted diffusion and was used to estimate whole-tissue hippocampal drug concentrations. Chronic i.c.v. infusions of D-AP5 caused a delay-dependent impairment of memory. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Oliet S H R, Malenka R C, Nicoll R A. Two distinct forms of long-term depression coexist in CA1 hippocampal pyramidal cells[J]. Neuron, 1997, 18(6): 969-982. [2]. 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. [3]. Steele R J, Morris R G M. Delay‐dependent impairment of a matching‐to‐place task with chronic and intrahippocampal infusion of the NMDA‐antagonist D‐AP5[J]. Hippocampus, 1999, 9(2): 118-136. |
D-AP5 is a selective N-methyl-D-aspartate (NMDA) receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors.[1] Whereas D-AP5 is the active (−)-stereoisomer, its (+)-isomer (L-AP5) demonstrates considerably less potent NMDA receptor antagonist activity.1 AP5 has been widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.[2]
Reference:
[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. Br. J. Pharmacol. 75(1), 65-75 (1982).
[2]. Morris, R.J. Synaptic plasticity and learning: Selective impairment of learning rats and blockade of long-term potentiation in vivo by the N-methyl-D-aspartate receptor antagonist AP5. J. Neurosci. 9(9), 3040-3057 (1989).
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 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
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 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% 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,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。