Rotundine
(Synonyms: 罗通定; (-)-Tetrahydropalmatine; L-Tetrahydropalmatine) 目录号 : GC14657
An antinociceptive alkaloid
Cas No.:483-14-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Kunming mice, initially weighing 18 to 22 g are used in this study. Four groups of mice are given Rotundine (l-THP) (6.25, 12.5, and 18.75 mg/kg) or saline, respectively, once per day for 7 consecutive days, followed by a 5 d withdrawal period. On d 13, all animals are challenged with saline. On day 1, 7, and 13, after 40-min treatment with Rotundine or saline, the mice are put into the test boxes and locomotor activity is monitored for 60 min[2]. |
References: [1]. Wang JB, et al. l-tetrahydropalamatine: a potential new medication for the treatment of cocaine addiction. Future Med Chem. 2012 Feb;4(2):177-86. | |
Levo-tetrahydropalmatine (l-THP) is an active herbal constituent of preparations containing plant species of the genera Stephania and Corydalis. In China, it has been approved and used for a number of clinical indications under the drug name Rotundine.
In vitro: In contrast to other THPB derivatives, l-THP is an antagonist at both of D1 and D2 receptors. The Ki values for l-THP at D1 and D2 dopamine receptors are approximately 124 nM (D1) and 388 nM (D2), while the IC50 values are 166 nM and 1.4 μM for D1 and D2, respectively. The relatively high affinity of l-THP at D1 vs. D2 receptors, distinguishes it from other available dopamine receptor antagonist drugs (e.g., haloperidol) [1].
In vivo: It has been found that l-THP produces dose-dependent reductions in locomotor activity and operant responding for non-drug reinforcers in rats [1].
Clinical trials: It has long been recognized l-THP has therapeutic values for treating a number of CNS related conditions. The effectiveness of l-THP as a non-opioid analgesic agent resulted in the approval of purified l-THP for this indication by the Chinese SFDA and has led to extensive investigation of the pharmacological properties of l-THP [1]
Reference:
[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.
| Cas No. | 483-14-7 | SDF | |
| 别名 | 罗通定; (-)-Tetrahydropalmatine; L-Tetrahydropalmatine | ||
| Canonical SMILES | COC1=C(C2=C(CC3C4=CC(=C(C=C4CCN3C2)OC)OC)C=C1)OC | ||
| 分子式 | C21H25NO4 | 分子量 | 355.43 |
| 溶解度 | ≥ 16mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8135 mL | 14.0675 mL | 28.1349 mL |
| 5 mM | 0.5627 mL | 2.8135 mL | 5.627 mL |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8135 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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