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/ 多巴胺受体 / Pramipexole 2HCl/盐酸普拉克索

Pramipexole 2HCl/盐酸普拉克索 {[allProObj[0].p_purity_real_show]}

货号：A115399 同义名： (S)-Pramipexole (hydrochloride); SND919

Pramipexole 2HCl is an dopamine agonist and can inhibit multiple dopamine receptors including dopamine D2S receptor, dopamine D2L receptor, dopamine D3 receptor, and dopamine D4 receptor with respectively Ki values of 3.9, 2.2, 0.5 and 5.1 nM.

Pramipexole 2HCl/盐酸普拉克索 化学结构 CAS号：104632-25-9
Pramipexole 2HCl/盐酸普拉克索 化学结构
CAS号：104632-25-9
Pramipexole 2HCl/盐酸普拉克索 3D分子结构
CAS号：104632-25-9
Pramipexole 2HCl/盐酸普拉克索 化学结构 CAS号：104632-25-9
Pramipexole 2HCl/盐酸普拉克索 3D分子结构 CAS号：104632-25-9
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Pramipexole 2HCl/盐酸普拉克索 纯度/质量文件 产品仅供科研

货号：A115399 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 D1 receptor ↓ D2 receptor ↓ D3 receptor ↓ D4 receptor ↓ D5 receptor ↓ DAT ↓ Dopamine receptor ↓ 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

 		98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

 		99%
Tetrahydroberberine +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 98% (HPLC)
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole HCl ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

 		98%
Levosulpiride ✔ 99+%
Pridopidine ✔ 95%
Metoclopramide ✔ ✔ 99+%
Molindone HCl ✔ 99%
Sulpiride ✔ 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		99%
Phenothiazine ✔ 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

 		+++

Dopamine D2 receptor, Ki: 3.0 nM

 		++++

Dopamine D3 receptor, Ki: 0.83 nM

 		98%
Rotundine ++

D1 receptor, IC50: 166 nM

 		+

D2 receptor, IC50: 1.47 μM

 		+

D3 receptor, IC50: 3.25 μM

 		98%
Domperidone ✔ 99+%
ONC206 ✔ 99%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

 		++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		98%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		99%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

 		++++

D5 dopamine receptor, Ki: 0.3 nM

 		98%
MPP+ iodide ✔ 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

 		97%
Benztropine mesylate ++

DAT, IC50: 118 nM

 		98%
Azaperone ✔ 98%
Ziprasidone HCl ✔ 98+%
Paliperidone ✔ 98%
Alizapride HCl ✔ 99+%
Amisulpride ✔ 98%
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Clozapine N-oxide ✔ 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Pramipexole 2HCl/盐酸普拉克索 生物活性

描述 Pramipexole (Dihydrochloride) is a nonergolinic dopamine agonist, with high affinity for the D2 subfamily of dopamine receptors. Pramipexole is efficacious for the symptomatic treatment of early Parkinson's Disease (PD) and its early use, before that of levodopa can delay the emergence of levodopa-related motor complication[3]. Pramipexole is a potent dopamine autoreceptor agonist. Two measurements of receptor activation for dopamine D2, D3, and D4 receptors show that pramipexole is most potent for activation of D3 receptors[4]. Post-stroke treatment with pramipexole reduced levels of mitochondrial ROS and Ca2+ after ischemia. Pramipexole elevated the mitochondrial membrane potential and mitochondrial oxidative phosphorylation. Thus, post-stroke administration of pramipexole induces the neurological recovery through mitochondrial pathways in ischemia/reperfusion injury[5]. P-CNs (Pramipexole dihydrochloride loaded chitosan nanoparticles) enhanced antioxidant status in the form of increased superoxide dismutase and catalase activities, along with increased dopamine level in the brain significantly[6]. Half of the patients stopped the pramipexole an average of 2 months after starting it. For all patients, depressed mood, and the total profile of depressive symptoms improved significantly within 4 weeks and remained significantly improved for as long as 36 weeks[7].

Pramipexole 2HCl/盐酸普拉克索 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00614575 - Completed - -
NCT00614575 - Completed - -
NCT00144209 Restless Legs Syndrome Phase 3 Completed - Switzerland ... 展开 >> Boehringer Ingelheim Investigational Site Basel, Switzerland, 4025 Boehringer Ingelheim Investigational Site Basel, Switzerland, 4031 Boehringer Ingelheim Investigational Site Bern, Switzerland, 3000 Boehringer Ingelheim Investigational Site Lugano, Switzerland, CH-6900 Boehringer Ingelheim Investigational Site Zurich, Switzerland, 8091 Boehringer Ingelheim Investigational Site Zurzach, Switzerland, 5330 收起 <<

Pramipexole 2HCl/盐酸普拉克索 参考文献

[1]Pathare DB, Jadhav AS, Shingare MS. Validated chiral liquid chromatographic method for the enantiomeric separation of Pramipexole dihydrochloride monohydrate. J Pharm Biomed Anal. 2006 Jun 16;41(4):1152-6.

[2]Mierau J, Schneider FJ, et al. Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. Eur J Pharmacol. 1995 Jun 23;290(1):29-36.

[3]Perez-Lloret S, Rey MV, Ratti L, Rascol O. Pramipexole for the treatment of early Parkinson's disease. Expert Rev Neurother. 2011;11(7):925‐935

[4]Mierau J, Schneider FJ, Ensinger HA, Chio CL, Lajiness ME, Huff RM. Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. Eur J Pharmacol. 1995;290(1):29‐36

[5]Andrabi SS, Ali M, Tabassum H, Parveen S, Parvez S. Pramipexole prevents ischemic cell death via mitochondrial pathways in ischemic stroke. Dis Model Mech. 2019;12(8):dmm033860.

[6]Raj R, Wairkar S, Sridhar V, Gaud R. Pramipexole dihydrochloride loaded chitosan nanoparticles for nose to brain delivery: Development, characterization and in vivo anti-Parkinson activity. Int J Biol Macromol. 2018;109:27‐35

[7]El-Mallakh RS, Penagaluri P, Kantamneni A, Gao Y, Roberts RJ. Long-term use of pramipexole in bipolar depression: a naturalistic retrospective chart review. Psychiatr Q. 2010;81(3):207‐213

Pramipexole 2HCl/盐酸普拉克索 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.18mL

7.04mL

3.52mL

Pramipexole 2HCl/盐酸普拉克索 技术信息

CAS号104632-25-9
分子式C10H19Cl2N3S
分子量 284.25
SMILES Code NC1=NC2=C(C[C@@H](NCCC)CC2)S1.[H]Cl.[H]Cl
MDL No. MFCD00876894
别名 (S)-Pramipexole (hydrochloride); SND919; (–)-Pramipexole
运输蓝冰
InChI Key QMNWXHSYPXQFSK-KLXURFKVSA-N
Pubchem ID 119569
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C
溶解方案 配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案一

Tags: Pramipexole dihydrochloride | (S)-Pramipexole (hydrochloride);SND919;(–)-Pramipexole | Dopamine Receptor | AmBeed-信号通路专用抑制剂 | Pramipexole 2HCl/盐酸普拉克索 纯度/质量文件 | Pramipexole 2HCl/盐酸普拉克索 亚型比较 | Pramipexole 2HCl/盐酸普拉克索 生物活性 | Pramipexole 2HCl/盐酸普拉克索 临床数据 | Pramipexole 2HCl/盐酸普拉克索 参考文献 | Pramipexole 2HCl/盐酸普拉克索 实验方案 | Pramipexole 2HCl/盐酸普拉克索 技术信息

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