(2R,4R)-APDC
目录号 : GC11379
(2R,4R)-APDC 是一种选择性 II 族代谢型谷氨酸受体 (mGluRs) 激动剂。
Cas No.:169209-63-6
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
| Kinase experiment [1]: | |
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Binding assays |
Radioligand binding to NMDA, AMPA, kainate, and metabotropic glutamate receptors was performed utilizing [3H]CGS19755, [3H]AMPA, [3H]kainate, and [3H]glutamate as the radioligands, respectively. Measure the cyclic adenosine monophosphate (cAMP) and tritiated inositol monophosphates ([3H]IP) levels in rat cerebral cortical slices. |
| Cell experiment [2]: | |
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Cell lines |
Human mGluR2 expressing CHO cell |
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Preparation method |
The solubility of this compound is up 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. |
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Reacting condition |
(2R,4R)-APDC were added and incubated for 20 min at 37°C. |
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Applications |
2R,4R-APDC inhibited forskolin-stimulated CAMP formation in human mGluR2 expressing cells with greater potency than lS,3R-ACPD, but unlike lS,3R-ACPD, (2R,4R)-APDC showed no obvious activation of phosphoinostide hydrolysis in human mGluR.lcc expressing cells.. |
| Animal experiment [1]: | |
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Animal models |
Female Wistar rats were anesthetized with pentobarbitone Na, and a lumbar laminectomy was performed to allow insertion of a seven-barrel glass microelectrode into the gray matter of the spinal cord. Action potential firing rate of single neurons was recorded continuously in response to timed intermittent ejection of AMPA (10 mM in 200 mM NaCl, pH 7.4) from one barrel of the electrode. |
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Dosage form |
When consistent submaximal responses were established, (2R,4R)-APDC at 25 mM in 175 mM NaCl, pH 7.4 were ejected on different cells. |
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Application |
(2R,4R)-APDC caused a robust enhancement of AMPA responses on AMPA evoked responses in intact rat spinal cord neurons. |
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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. |
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References: [1] Monn JA, et al. Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: identification of a potent, highly selective, and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase. J Med Chem. 1996 Jul 19;39(15):2990-3000. [2] Schoepp DD, et al. Selective inhibition of forskolin-stimulated cyclic AMP formation in rat hippocampus by a novel mGluR agonist, 2R,4R-4-aminopyrrolidine-2,4- dicarboxylate. Neuropharmacology. 1995 Aug;34(8):843-50. | |
EC50: 0.4 μM
2R,4R-APDC is a highly selective and relatively potent group II metabotropic glutamate receptor agonist for human mGlu2. L-Glutamate (Glu) is EAA neurotransmitter in the mammalian CNS. Its effects are mediated by a variety of presynaptic and postsynaptic neuronal receptors.
In vitro: 2R,4R-APDC blocked forskolin-stimulated cAMP with none of the other activities of lS,3R-ACPD. forskolin-stimulated cAMP formation in human mGluR2 expressing cells with about three-fold greater potency than lS,3R-ACPD were also inhibited by 2R,4R-APDC, which, unlike lS,3R-ACPD, exhibited no appreciable activation of phosphoinostide hydrolysis in human mGluR. Thus, 2R,4R-APDC should be a useful pharmacological tool to explore the functions of mGluRs coupled to inhibition of adenylate cyclase [1]. The effects of four isomers of APDC were investigated at glutamate receptors in vitro. (2R,4R)-APDC, an aza analog of the nonselective mGluR agonist (1S,3R)-ACPD possessed relatively high affinity for metabotropic glutamate receptors (mGluRs) with no effects on radioligand binding to NMDA, AMPA, or kainate receptors up to 100 íM. None of the other APDC isomers exhibited significant mGluR binding affinity, indicating that this interaction is highly stereospecific [2].
In vivo: Both (1S,3R)-ACPD and (2R,4R)-APDC were effectively attenuating forskolin-stimulated cAMP formation in the adult rat cerebral cortex; however, while (1S,3R)-ACPD was also effectively stimulating basal tritiated inositol monophosphate production of the neonatal rat cerebral cortex, (2R,4R)-APDC was not effectively stimulating phosphoinositide hydrolysis in this tissue preparation. An augmentation of AMPA-induced excitation was produced by microelectrophoretic application of either (1S,3R)-ACPD or (2R,4R)-APDC to intact rat spinal neurons [2].
Clinical trial: Clinical study has been conducted.
References:
[1] Schoepp DD, Johnson BG, Salhoff CR, Valli MJ, Desai MA, Burnett JP, Mayne NG, Monn JA. Selective inhibition of forskolin-stimulated cyclic AMP formation in rat hippocampus by a novel mGluR agonist, 2R,4R-4-aminopyrrolidine-2,4- dicarboxylate. Neuropharmacology. 1995 Aug;34(8):843-50.
[2] Monn JA, Valli MJ, Johnson BG, Salhoff CR, Wright RA, Howe T, Bond A, Lodge D, Spangle LA, Paschal JW, Campbell JB, Griffey K, Tizzano JP, Schoepp DD. Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: identification of a potent, highly selective, and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase. J Med Chem. 1996 Jul 19; 39 (15):2990-3000.
| Cas No. | 169209-63-6 | SDF | |
| 化学名 | (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid | ||
| Canonical SMILES | OC([C@]1(C[C@H](C(O)=O)NC1)N)=O | ||
| 分子式 | C6H10N2O4 | 分子量 | 174.16 |
| 溶解度 | Soluble to 100 mM in Water | 储存条件 | Desiccate at RT |
| 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 | 5.7418 mL | 28.7092 mL | 57.4185 mL |
| 5 mM | 1.1484 mL | 5.7418 mL | 11.4837 mL |
| 10 mM | 0.5742 mL | 2.8709 mL | 5.7418 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。