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Submit ReviewPD 168077 maleate
说明： High affinity, selective D4 agonist
化学名： N-[[4-(2-Cyanophenyl)-1-piperazinyl]methyl]-3-methylbenzamide maleate
纯度： ≥98% (HPLC)
生物活性 for PD 168077 maleate
PD 168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM) with > 400-fold selectivity over D2 and > 300-fold selectivity versus D3 subtypes respectively. Induces synaptic translocation of CaMK II to postsynaptic sites in cultured prefrontal cortical neurons. Centrally active in vivo.
技术数据 for PD 168077 maleate
| 分子量 | 450.49 |
| 公式 | C20H22N4O.C4H4O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 630117-19-0 |
| PubChem ID | 11957665 |
| InChI Key | NAEUGRPISCANHO-BTJKTKAUSA-N |
| Smiles | OC(=O)\C=C/C(O)=O.CC1=CC(=CC=C1)C(=O)NCN1CCN(CC1)C1=C(C=CC=C1)C#N |
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 PD 168077 maleate
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 45.05 | 100 |
制备储备液 for PD 168077 maleate
以下数据基于产品分子量 450.49。 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 | 2.22 mL | 11.1 mL | 22.2 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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产品说明书 for PD 168077 maleate
参考文献 for PD 168077 maleate
参考文献是支持产品生物活性的出版物。
Clifford and Waddington (2000) Topographically based search for an "Ethogram" among a series of novel D4 DA receptor agonists and antagonists. Neuropsychopharmacology 22 538 PMID: 10731629
Glase et al (1997) Substituted [(4-phenylpiperazinyl)methyl]benzamides: selective DA D4 agonists. J.Med.Chem. 40 1771 PMID: 9191952
Gu et al (2006) Activation of DA D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol.Pharmacol. 69 813 PMID: 16365279
If you know of a relevant reference for PD 168077 maleate, please let us know.
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关键词: PD 168077 maleate, PD 168077 maleate supplier, High, affinity, selective, D4, agonists, Dopamine, Receptors, dopaminergic, PD168077, maleate, 1065, Tocris Bioscience
7 篇 PD 168077 maleate 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PD 168077 maleate 的部分引用包括：
Dai et al (2017) Is DA transporter-mediated DArgic signaling in the retina a noninvasive biomarker for attention-deficit/ hyperactivity disorder? A study in a novel DA transporter variant Val559 transgenic mouse model. J Neurodev Disord 9 38 PMID: 29281965
Graziane et al (2009) DA D4 Receptors Regulate GABAA Receptor Trafficking via an Actin/Cofilin/Myosin-dependent Mechanism. Circ Res 284 8329 PMID: 19179335
Huang (2017) Neurochemical arguments for the use of DA D4 receptor stimulation to improve cognitive impairment associated with schizophrenia. Pharmacol Biochem Behav 157 16 PMID: 28455126
Guo (2017) DA D4 receptor activation restores CA1 LTP in hippocampal slices from aged mice. Aging Cell 16 1323 PMID: 28975698
Chen et al (2015) Activation of D4 DA receptor decreases angiotensin II type 1 receptor expression in rat renal proximal tubule cells. J Biol Chem 65 153 PMID: 25368031
Negrete-Díaz et al (2019) Pharmacological activation of dopamine D4 receptor modulates morphine-induced changes in the expression of GAD65/67 and GABAB receptors in the basal ganglia. Neuropharmacology 152 22 PMID: 30682345
Yuen et al (2013) Restoration of glutamatergic transmission by DA D4 receptors in stressed animals. J Biol Chem 288 26112 PMID: 23884421
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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