NMDA (N-methyl-D-aspartate) receptor

谷氨酸诱导的 Arc/Arg3.1 蛋白水平增加被 DL-AP5 (100 μM) 部分抑制 [5]。 DL-AP5 可降低 Arc/Arg3.1 的 NMDA 诱导上调 [5]。

DL-AP5（0-10 μg/大鼠，Intra-CA1）极大地减弱了 NMDA 的作用 [3]。 DL-AP5（0-10 nmol，脑室内注射）促进食物消耗的剂量依赖性增加[4]。 DL-AP5（5 nmol，脑室内注射）可减弱脑室内注射生长素释放肽引起的食物消耗减少[4]。

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本试验旨在研究脑室内注射DL-AP5 （n-甲基-d -天冬氨酸（NMDA）受体拮抗剂）和谷氨酸对饥饿素诱导的3 h缺食（FD3）肉仔鸡摄食行为的影响。首先在鸡右侧脑室手术植入引导管。实验1，分别在脑室内注射0、2.5、5、10 nmol DL-AP5。实验2，在注射胃饥饿素0.6 nmol之前，先给鸡注射5 nmol DL-AP5。实验3，在谷氨酸300 nmol后，再饲喂0.6 nmol胃饥饿素，注射后3 h测定累积采食量。本研究结果表明，脑室内注射DL-AP5可增加FD3肉鸡的摄食量（P≤0.05），且呈剂量依赖性。谷氨酸预处理能增强脑室注射胃饥饿素引起的摄食量减少，DL-AP5能减弱这种作用（P≤0.05）。这些结果表明，胃饥饿素和谷氨酸能系统（通过NMDA受体）对肉仔鸡的摄食量有相互作用。[4]

Animal/Disease Models: Male Wistar rat (180-230 g) [3]
Doses: 1, 3.2 and 10 μg/rat
Route of Administration: Inject into the dorsal hippocampus (within CA1) immediately after electric shock, one time
Experimental Results:Significant reduction There was a significant interaction effect of NMDA (10-2 μg/rat, within CA1).

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Animal/Disease Models: Broiler chicken (FD3) (3 hrs (hrs (hours)) fast, n=8 per group) [4]
Doses: 0, 2.5, 5 and 10 nmol; volume of 10 µL
Route of Administration: intracerebroventricular injection
Experimental Results: dose causing food consumption The dependence increased, being significant for the 5 and 10 nmol doses.

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Animal/Disease Models: broiler rooster (fasted for 3 hrs (hrs (hours)) (FD3), n=8 per group) [4]
Doses: 5 nmol
Route of Administration: intracerebroventricular injection, followed by ghrelin (0.6 nmol)
Experimental Results: Attenuated by Intracerebroventricular injection of ghrelin.

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To determine the involvement of glutamate NMDA receptor in the brain in ghrelin-induced eating response, effects of centrally administered DL-AP5 and glutamate on ghrelin-induced eating response were determined in chickens. Injections were made with a 29-gauge, thin-walled stainless-steel injection cannula which extends 1.0 mm beyond the guide cannula. This injection cannula was connected to a 10-μl Hamilton syringe connected to a 60 cm length of PE-20 tubing. Solutions were injected over a period of 60 s. Another 60-s period was allowed to permit the solution to diffuse from the tip of the cannula into the ventricle. All experimental procedures were performed between 9 a.m. and 2 p.m. Before the injections, the birds were removed from their individual cages, restricted by hand, and after injections were put back into their cages. Birds were handled and mock-injected daily during the 5 days recovery period to habituate them to the injection procedure. Three hours before the beginning of the experiments, animals were deprived of food but with water ad lib. Immediately after injections, the birds were returned to their cages. Fresh food was supplied at the time of injection, and cumulative feed intake (grams) was recorded at 15, 30, 60, 120, and 180 min after injection. Placement of the guide cannula into the ventricle was verified by the presence of cerebrospinal fluid and intracerebroventricular injection of methylene blue and anatomically slicing the frozen brain tissue at the end of the experiments.[4]
Experiment 1 was designed to examine the effect of intracerebroventricular injections of different DL-AP5 doses on cumulative feed intake in 3-h food-deprived (FD3, n = 8 for each group) chickens. For this purpose, the birds received 0, 2.5, 5, and 10 nmol of DL-AP5 in a volume of 10 μl. Control group was injected with 10 μl of 0.9% NaCl solution.[4]
In experiment 2, birds of each group received two injections. The first injection consisted of either 0 or 5 nmol DL-AP5 in a volume of 5 μl. The second injection consisted of either 0 or 0.6 nmol ghrelin in a volume of 5 μl, 15 min after the first injection as described in Table 1 (n = 7–9 for each group).[4]

[1]. Neurokinin and NMDA antagonists (but not a kainic acid antagonist) are antinociceptive in the mouse formalin model. Pain. 1991;44(2):179-185.

[2]. N-methyl-D-aspartate receptors of ganglion cells in rabbit retina. J Neurophysiol. 1990;63(1):16-30.

[3]. Jafari-Sabet M. NMDA receptor blockers prevents the facilitatory effects of post-training intra-dorsal hippocampal NMDA and physostigmine on memory retention of passive avoidance learning in rats. Behav Brain Res. 2006 Apr 25;169(1):120-7.

[4]. The effects of DL-AP5 and glutamate on ghrelin-induced feeding behavior in 3-h food-deprived broiler cockerels. J Physiol Biochem. 2011 Jun;67(2):217-23.

[5]. Glutamate-induced rapid induction of Arc/Arg3.1 requires NMDA receptor-mediated phosphorylation of ERK and CREB. Neurosci Lett. 2017 Nov 20;661:23-28.

2-amino-5-phosphonopentanoic acid is the 5-phosphono derivative of 2-aminopentanoic acid; acts as an N-methyl-D-aspartate receptor antagonist. It has a role as a NMDA receptor antagonist. It is functionally related to a phosphonic acid and a 2-aminopentanoic acid.
2-Azaniumyl-5-phosphonopentanoate has been reported in Euglena gracilis with data available.

C5H12NO5P

197.1262

197.045

C, 30.47; H, 6.14; N, 7.11; O, 40.58; P, 15.71

76326-31-3

D-AP5;79055-68-8;L-AP5;79055-67-7

1216

White to off-white solid powder

1.5±0.1 g/cm3

482.1±55.0 °C at 760 mmHg

245.4±31.5 °C

0.0±2.6 mmHg at 25°C

1.536

-2.32

130.66

4

6

5

12

200

0

VOROEQBFPPIACJ-UHFFFAOYSA-N

InChI=1S/C5H12NO5P/c6-4(5(7)8)2-1-3-12(9,10)11/h4H,1-3,6H2,(H,7,8)(H2,9,10,11)

2-amino-5-phosphonopentanoic acid

76326-31-3; DL-AP5; 2-Amino-5-phosphonopentanoic acid; DL-2-Amino-5-phosphonopentanoic acid; 5-Phosphononorvaline; 2-AMINO-5-PHOSPHONOVALERATE; 2-Amino-5-phosphovaleric acid; 2-Amino-5-phosphonovaleric Acid;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~33.33 mg/mL (~169.08 mM)

配方 1 中的溶解度: 50 mg/mL (253.64 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。