D-AP5 (Synonyms: D-2-Amino-5-Phosphonovaleric acid; D-APV) |
| Catalog No.GC16315 |
D-AP5은 선택적 N-methyl-D-aspartate (NMDA) 수용체 앙티아고니스트로, Kd 값이 1.4μM이다.
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-AP5은 선택적 N-methyl-D-aspartate (NMDA) 수용체 앙티아고니스트로, Kd 값이 1.4μM이다.
D-AP5은 NMDA 수용체의 글루타마트 결합 사이트를 억제한다[2]. 이것은 NMDA 수용체가 신경병리학에서의 역할, 특히 신경 보호에서의 역할을 연구하는 데 사용될 수 있다[3].
체외 실험에서 D-AP5(30μM)는 피질 뇌기능을 처리하여 엡시낭에서 방출된 글루타마트가 유도한 세포내 Ca2+ 농도 증가를 NMDA 수용체 억제를 통해 현저하게 감소시켰다[4]. D-AP5(20μM)는 쥐 해마 구조의 뉴런을 처리하여 NMDA 유도 칼슘 류입을 현저하게 감소시키고 뉴런 전기활동을 억제하여 뉴런을 흥분 독성 손상으로부터 보호한다[5].
체내 실험에서 D-AP5(0.5µg/µL; 1µL/h)은 14일 동안 Lister 후드 쥐에게 뇌시내 투여를 통해 공간 학습 및 기억 능력을 크게 영향을 미쳤으며, 주로 NMDA 수용체를 통해 중개된 엡시낭적 유연성 메커니즘과 장기간 강화(LTP) 형성을 억제함으로써 이를 달성했다[6]. D-AP5(5-10 nmol/µL; 0.5µL/h)은 쥐에게 뇌시내 투여를 통해 해마 CA1 영역의 LTP 형성을 현저하게 억제하여 기억 손상으로 이어졌다[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.
| 세포 실험 [1]: | |
|
세포 라인 |
피질 아스트로글리아 |
|
제조 방법 |
격동제가 적용된 2분 전에 세포에 D-AP5(30μM)가 추가되었으며, 이어서 전기 생리학적 기록을 진행하였다. |
|
반응 조건 |
30μM; 2 분 |
|
응용 분야 |
D-AP5는 뉴로전에서 방출된 글루타마트가 인한 세포 내 Ca2+ 농도 증가를 현저하게 감소시킨다. |
|
동물 실험 [2]: |
|
|
동물 모형 |
수컷 리스터 후드 쥐 |
|
제조 방법 |
D-AP5는 14일 동안 0.5 µg/µL의 용량과 1 µL/h의 지속적인 유율로 만성 뇌졸로 유동 펌프를 통해 투여되었다. 이 만성 투여는 더 긴 기간 동안 일정한 약물 농도를 유지한다. |
|
제형 |
0.5µg/µL ,1µL/h의 속도로; i.c.v. |
|
응용 분야 |
D-AP5의 만성 투여는 쥐의 공간 학습 및 기억 능력을 현저하게 영향을 미쳤다. |
|
References: [1] Palygin O, Lalo U, Verkhratsky A, 등. 염이형 NMDA 및 P2X1/5 수용체가 피질 아스트로글리아에서 뉴로전 유도된 Ca2+ 신호를 조절한다[J]. 셀 칼시엄, 2010, 48(4): 225-231. [2] Morris R G M, Steele R J, Bell J E, 등. N‐methyl‐d‐aspartate 수용체, 학습 및 기억: NMDA 수용체 길항제 d-AP 5의 만성 뇌졸 내 유동은 공간 학습의 신경 기전에 직접적으로 작용한다[J]. 유럽 뇌 과학 저널, 2013, 37(5): 700-717. |
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| 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 | |||
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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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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.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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