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Submit ReviewPG 01037 dihydrochloride
说明： Selective D3 antagonist
化学名： N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride
纯度： ≥98%
生物活性 for PG 01037 dihydrochloride
PG 01037 dihydrochloride is a dopamine D3 receptor antagonist; 133-fold selective for D3 over D2 receptors in vitro (Ki values are 0.70, 93.3 and 375 nM for D3, D2 and D4 receptors respectively). Attenuates abnormal involuntary movements associated with L-DOPA (Cat. No. 3788) in rat models of Parkinson's disease. Inhibits the effects of methamphetamine; attenuates drug-induced behaviors in vivo.
化合物库 for PG 01037 dihydrochloride
PG 01037 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for PG 01037 dihydrochloride
| 分子量 | 554.34 |
| 公式 | C26H26Cl2N4O.2HCl |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥98% |
| CAS Number | 675599-62-9 |
| PubChem ID | 90488894 |
| InChI Key | DACFFMAXBWGOKQ-CZEFNJPISA-N |
| Smiles | ClC(C(Cl)=CC=C4)=C4N(CC3)CCN3C/C=C/CNC(C1=CC=C(C2=NC=CC=C2)C=C1)=O.Cl.Cl |
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 PG 01037 dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 11.09 | 20 温和加热 | |
| DMSO | 55.43 | 100 |
制备储备液 for PG 01037 dihydrochloride
以下数据基于产品分子量 554.34。 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 | 1.8 mL | 9.02 mL | 18.04 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.61 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.8 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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产品说明书 for PG 01037 dihydrochloride
参考文献 for PG 01037 dihydrochloride
参考文献是支持产品生物活性的出版物。
Grundt et al (2005) Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the DA D3 receptor. J.Med.Chem. 48 839 PMID: 15689168
Grundt et al (2007) Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-butyl)arylcarboxamides with functionalized linking chains as novel DA D3 receptor ligands: potential substance abuse therapeutic agents. J.Med.Chem. 50 4135 PMID: 17672446
Kumar et al (2009) Evaluation of the D3 DA receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats. Neuropharmacology 56 944 PMID: 19371585
Mason et al (2010) Characterization of the transport, metabolism, and pharmacokinetics of the DA D3 receptor-delective fluorenyl-and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse. J.Pharm.Exp.Ther. 333 854 PMID: 20228156
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关键词: PG 01037 dihydrochloride, PG 01037 dihydrochloride supplier, PG01037, dopamine, receptors, D3, antagonists, dopaminergic, parkinsons, antiparkinsonian, parkinson's, Receptors, 3887, Tocris Bioscience
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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。
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Addiction Poster
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.