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神经信号通路 帕金森与阿尔茨海默症
/ 多巴胺受体 / Rotundine

罗通定 /Rotundine {[allProObj[0].p_purity_real_show]}

货号：A842066 同义名： (-)-Tetrahydropalmatine;L-Tetrahydropalmatine

Rotundine is antagonist for domapmine D1 receptor(Ki = 124 nM) and has a lower binding activity of domapmine D2 receptor and domapmine D3 receptor. It can also inhibit 5-HT1A (Ki = 340 nM).

Rotundine 化学结构 CAS号：483-14-7
Rotundine 化学结构
CAS号：483-14-7
Rotundine 3D分子结构
CAS号：483-14-7
Rotundine 化学结构 CAS号：483-14-7
Rotundine 3D分子结构 CAS号：483-14-7
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Rotundine 纯度/质量文件 产品仅供科研

货号：A842066 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。

Rotundine 生物活性

靶点

  • D3 receptor

    D3 receptor, IC50:3.25 μM

  • D1 receptor

    D1 receptor, IC50:166 nM

  • D2 receptor

    D2 receptor, IC50:1.47 μM
描述 Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM. Rotundine (l-THP) possesses a blocking effect on dopamine D1 and D2 receptors and can inhibit physical dependence in morphine dependent mice and significantly reduce the development of the conditional place preference induced by morphine in mice[3]. Rotundine (6.25, 12.5 mg/kg) does not affect the magnitude of sensitization, but there is a marked difference between oxycodone+oxycodone group and Rotundine (18.75 mg/kg)+oxycodone+oxycodone group, indicating that Rotundine (18.75 mg/kg) greatly inhibits the development of oxycodone sensitization[4]. The various types of NOS (nitric oxide synthase) play different roles in the lung damages after brain I/R (ischemia/reperfusion) injury at different stages in rats. Rotundine injection can ameliorate the damages by modulating the activities of different types of NOS[5]. Compared with the control group, rotundine(> or = 17.1 mg/kg) inhibited gastric acid and decreased secretion of gastric juice(P < 0.01), but had no influence on pepsin activity[6].

Rotundine 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
NCT01631383 Cocaine Use Phase 1 Completed - United States, Maryland ... 展开 >> Maryland Psychiatric Research Center Catonsville, Maryland, United States, 21228 收起 <<
NCT02118610 Schizophrenia Not Applicable Recruiting December 2019 United States, Maryland ... 展开 >> Maryland Psyciatric Research Center Recruiting Catonsville, Maryland, United States, 21228 Contact: Ann Kearns, BS    410-402-6854    akearns@mprc.umaryland.edu 收起 <<
NCT02139761 Cocaine Use Phase 2 Withdrawn(Study funding has no... 展开 >>t been established) 收起 << June 2016 United States, Maryland ... 展开 >> Maryland Psychiatric Research Center Catonsville, Maryland, United States, 21228 收起 <<

Rotundine 参考文献

[1]Wang JB, Mantsch JR. l-tetrahydropalamatine: a potential new medication for the treatment of cocaine addiction. Future Med Chem. 2012 Feb;4(2):177-86.

[2]Liu YL, Liang JH, et al. Effects of l-tetrahydropalmatine on locomotor sensitization to oxycodone in mice. Acta Pharmacol Sin. 2005 May;26(5):533-8.

[3]Wang JB, Mantsch JR. l-tetrahydropalamatine: a potential new medication for the treatment of cocaine addiction. Future Med Chem. 2012;4(2):177‐186

[4]Liu YL, Liang JH, Yan LD, Su RB, Wu CF, Gong ZH. Effects of l-tetrahydropalmatine on locomotor sensitization to oxycodone in mice. Acta Pharmacol Sin. 2005;26(5):533‐538

[5]Zeng AY, Tu EY, Han ZY, Yang GT. Zhongguo Wei Zhong Bing Ji Jiu Yi Xue. 2007;19(6):361‐364

[6]Zhou M, Li X, Geng L, Qu C, Peng S. Zhongguo Zhong Yao Za Zhi. 1998;23(5):

Rotundine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.07mL

2.81mL

1.41mL

28.14mL

5.63mL

2.81mL

Rotundine 技术信息

CAS号483-14-7
分子式C21H25NO4
分子量 355.428
别名 (-)-Tetrahydropalmatine;L-Tetrahydropalmatine;(S)-Tetrahydropalmatine;(–)-Tetrahydropalmatine;(–)-Corydalis B;L-THP
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 105 mg/mL(295.42 mM)，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
动物实验配方

Tags: Rotundine | (-)-Tetrahydropalmatine;L-Tetrahydropalmatine;(S)-Tetrahydropalmatine;(–)-Tetrahydropalmatine;(–)-Corydalis B;L-THP | Dopamine Receptor | AmBeed-信号通路专用抑制剂 | Rotundine 纯度/质量文件 | Rotundine 亚型比较 | Rotundine 生物活性 | Rotundine 临床数据 | Rotundine 参考文献 | Rotundine 实验方案 | Rotundine 技术信息

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