产品说明书

Rotundine

Print
Chemical Structure| 483-14-7 同义名 : (-)-Tetrahydropalmatine;L-Tetrahydropalmatine;(S)-Tetrahydropalmatine;(–)-Tetrahydropalmatine;(–)-Corydalis B;L-THP
CAS号 : 483-14-7
货号 : A842066
分子式 : C21H25NO4
纯度 : 98%
分子量 : 355.428
MDL号 : MFCD03265591
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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NCT02139761 Cocaine Use Phase 2 Withdrawn(Study funding has no...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 <<
实验方案
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
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):