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Submit Review(2R,4R)-APDC
说明： Highly selective group II agonist
化学名： (2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylate
纯度： ≥98% (HPLC)
生物活性 for (2R,4R)-APDC
(2R,4R)-APDC is a highly selective and relatively potent group II metabotropic glutamate receptor agonist. EC50 values are 0.4, 0.4, > 100, > 100, > 300 and > 300 μM for human mGlu2, mGlu3, mGlu1, mGlu5, mGlu4 and mGlu7 receptors respectively. Centrally active following systemic administration in vivo.
许可信息
Sold with the permission of Eli Lilly and Company
技术数据 for (2R,4R)-APDC
| 分子量 | 174.16 |
| 公式 | C6H10N2O4 |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 169209-63-6 |
| PubChem ID | 5310984 |
| InChI Key | XZFMJVJDSYRWDQ-AWFVSMACSA-N |
| Smiles | N[C@]1([C@](O)=O)C[C@H]([C@](O)=O)NC1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for (2R,4R)-APDC
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 100 |
制备储备液 for (2R,4R)-APDC
以下数据基于产品分子量 174.16。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 5.74 mL | 28.71 mL | 57.42 mL |
| 5 mM | 1.15 mL | 5.74 mL | 11.48 mL |
| 10 mM | 0.57 mL | 2.87 mL | 5.74 mL |
| 50 mM | 0.11 mL | 0.57 mL | 1.15 mL |
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产品说明书 for (2R,4R)-APDC
参考文献 for (2R,4R)-APDC
参考文献是支持产品生物活性的出版物。
Monn et al (1996) 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. 39 2990 PMID: 8709133
Schoepp et al (1995) Selective inhibition of forskolin-stimulated cyclic AMP formation in rat hippocampus by a novel mGluR agonist, 2R,4R-4-aminopyrrolidine-2,4-dicarboxylate. Neuropharmacology 34 843 PMID: 8532165
Schoepp et al (1999) Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 38 1431 PMID: 10530808
If you know of a relevant reference for (2R,4R)-APDC, please let us know.
关键词: (2R,4R)-APDC, (2R,4R)-APDC supplier, selective, group, II, agonists, Group, Receptors, mGlu2, mGlu3, mGluR2, mGluR3, Glutamate, Metabotropic, (Metabotropic), 1208, Tocris Bioscience
8 篇 (2R,4R)-APDC 的引用文献
引用文献是使用了 Tocris 产品的出版物。 (2R,4R)-APDC 的部分引用包括：
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236
McIlwrath and Westlund (2015) Pharmacological attenuation of chronic alcoholic pancreatitis induced hypersensitivity in rats. Brain Res 21 836 PMID: 25624717
Carlton et al (2009) Group II metabotropic glutamate receptor activation on peripheral nociceptors modulates TRPV1 function. J Neurosci 1248 86 PMID: 19026992
Ren et al (2012) Intrathecal injection of metabotropic glutamate receptor subtype 3 and 5 agonist/antagonist attenuates bone cancer pain by inhibition of spinal astrocyte activation in a mouse model. Anesthesiology 116 122 PMID: 22123524
Pasquale and Sherman (2013) A modulatory effect of the feedback from higher visual areas to V1 in the mouse. J Neurophysiol 109 2618 PMID: 23446698
Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43 PMID: 22726616
Proudfoot et al (2006) Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr Biol 16 1591 PMID: 16920620
Jiang et al (2006) Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on DArgic neurons through a microtubule-dependent mechanism. J Neurosci 26 4318 PMID: 16624952
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