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/ 多巴胺受体 / Ropinirole hydrochloride

盐酸罗匹尼罗 /Ropinirole hydrochloride {[allProObj[0].p_purity_real_show]}

货号：A553861 同义名： SKF 101468 hydrochloride;Ropinirole (hydrochloride)

Ropinirole HCl selectively inhibit dopamine D2 receptor with Ki of 29 nM. It is used for the treatment of spontaneous parkinson's disease.

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Ropinirole hydrochloride 化学结构 CAS号：91374-20-8
Ropinirole hydrochloride 化学结构
CAS号：91374-20-8
Ropinirole hydrochloride 3D分子结构
CAS号：91374-20-8
Ropinirole hydrochloride 化学结构 CAS号：91374-20-8
Ropinirole hydrochloride 3D分子结构 CAS号：91374-20-8
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Ropinirole hydrochloride 纯度/质量文件 产品仅供科研

货号：A553861 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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

 		98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 95%
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

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

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		98+%
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 ✔ 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

 		++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		98%
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%
Quetiapine hemifumarate ✔ Adrenergic Receptor 98%
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。

Ropinirole hydrochloride 生物活性

靶点

  • D2 receptor

    D2 receptor, Ki:29 nM
描述 Ropinirole (Hydrochloride), a selective agonist of dopamine D2/D3, is in use for the treatment of parkinsonism[3]. Ropinirole decreased ICSS (intracranial self-stimulation) thresholds and induced anxiolytic- and antidepressive-like effects without affecting motor activity or spatial memory. Ropinirole significantly affects emotionality at doses (1-10 mg/kg, i.p.) that exert no robust effects on locomotion or cognition[4]. Ropinirole transiently increased premature responses, a measure of motor impulsivity, and this change was larger and more long-lasting in the cued task[5]. Ropinirole hydrochloride potentially targets multiple mechanisms of ALS (amyotrophic lateral sclerosis) pathology (i.e., oxidative stress, mitochondrial dysfunction, and abnormal aggregation of TDP-43/FUS protein, which is representative of the ALS phenotype), with promising preclinical study results based on iPSC (induced pluripotent stem cells) research[6].

Ropinirole hydrochloride 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
NCT02339064 Idiopathic Parkinson's Disease Phase 3 Active, not recruiting October 2019 United States, Arizona ... 展开 >> Phoenix, Arizona, United States, 85013 United States, California Loma Linda, California, United States, 92354 Los Angeles, California, United States, 90033 Los Angeles, California, United States, 90095 United States, Colorado Aurora, Colorado, United States, 80045 Englewood, Colorado, United States, 80113 United States, Florida Boca Raton, Florida, United States, 33486 United States, Georgia Atlanta, Georgia, United States, 30329 Augusta, Georgia, United States, 30912 United States, Illinois Chicago, Illinois, United States, 60611 Chicago, Illinois, United States, 60612 United States, Kansas Kansas City, Kansas, United States, 66160 United States, Michigan West Bloomfield, Michigan, United States, 48322 United States, New York Albany, New York, United States, 12208 United States, Ohio Cincinnati, Ohio, United States, 45219 United States, Oregon Portland, Oregon, United States, 97239 United States, Pennsylvania Philadelphia, Pennsylvania, United States, 19107 United States, Washington Kirkland, Washington, United States, 98034 收起 <<
NCT02386423 Restless Leg Syndrome Not Applicable Completed - United States, Pennsylvania ... 展开 >> Baycity Associated in Podiatry Inc Erie, Pennsylvania, United States, 16509 收起 <<
NCT01052831 Impulse Control Disorder ... 展开 >> Parkinson Disease 收起 << Phase 4 Completed - United States, Pennsylvania ... 展开 >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 收起 <<

Ropinirole hydrochloride 参考文献

[1]Iida M, Miyazaki I, et al. Dopamine D2 receptor-mediated antioxidant and neuroprotective effects of ropinirole, a dopamine agonist. Brain Res. 1999 Aug 14;838(1-2):51-9.

[2]Eden RJ, Costall B, et al. Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist. Pharmacol Biochem Behav. 1991 Jan;38(1):147-54.

[3]Gershon AA, Amiaz R, Shem-David H, Grunhaus L. Ropinirole Augmentation for Depression: A Randomized Controlled Trial Pilot Study. J Clin Psychopharmacol. 2019;39(1):78‐81

[4]Mavrikaki M, Schintu N, Nomikos GG, Panagis G, Svenningsson P. Ropinirole regulates emotionality and neuronal activity markers in the limbic forebrain. Int J Neuropsychopharmacol. 2014;17(12):1981‐1993

[5]Tremblay M, Barrus MM, Cocker PJ, Baunez C, Winstanley CA. Increased motor impulsivity in a rat gambling task during chronic ropinirole treatment: potentiation by win-paired audiovisual cues. Psychopharmacology (Berl). 2019;236(6):1901‐1915

[6]Takahashi S, Morimoto S, Okano H. Brain Nerve. 2019;71(9):943‐952

Ropinirole hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.37mL

0.67mL

0.34mL

16.84mL

3.37mL

1.68mL

33.69mL

6.74mL

3.37mL

Ropinirole hydrochloride 技术信息

CAS号91374-20-8
分子式C16H25ClN2O
分子量 296.84
别名 SKF 101468 hydrochloride;Ropinirole (hydrochloride);SKF-101468A;Ropinirole HCl
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 16 mg/mL(53.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(336.88 mM)，配合低频超声助溶
动物实验配方

Tags: Ropinirole hydrochloride | SKF 101468 hydrochloride;Ropinirole (hydrochloride);SKF-101468A;Ropinirole HCl | Dopamine Receptor | AmBeed-信号通路专用抑制剂 | Ropinirole hydrochloride 纯度/质量文件 | Ropinirole hydrochloride 亚型比较 | Ropinirole hydrochloride 生物活性 | Ropinirole hydrochloride 临床数据 | Ropinirole hydrochloride 参考文献 | Ropinirole hydrochloride 实验方案 | Ropinirole hydrochloride 技术信息

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