D-Tetrahydropalmatine
(Synonyms: 右旋四氢巴马汀) 目录号 : GC38228
A tetrahydroberberine alkaloid
Cas No.:3520-14-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
D-Tetrahydropalmatine is a tetrahydroberberine alkaloid that has been found in Corydalis.1 In vivo, D-Tetrahydropalmatine (32 mg/kg) reverses apomorphine-induced inhibition of dopaminergic firing in the substantia nigra pars compacta (SNC) in paralyzed rats.2
1.Liao, J., Liang, W.-Z., and Tu, G.-S.Isolation and identification of eleven tertiary alkaloids in Corydalis decumbensJ. Chin. Pharma. Sci.4(2)57-61(1995) 2.Sun, B.C., Huang, K.X., and Jin, G.Z.Comparison of effects of tetrahydropalmatine enantiomers on firing activity of dopamine neurons in substantia nigra pars compactaZhongguo Yao Li Xue Bao13(4)292-297(1992)
| Cas No. | 3520-14-7 | SDF | |
| 别名 | 右旋四氢巴马汀 | ||
| Canonical SMILES | COC1=CC=C2C(CN3CCC4=CC(OC)=C(OC)C=C4[C@@]3([H])C2)=C1OC | ||
| 分子式 | C21H25NO4 | 分子量 | 355.43 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at 2-8°C,protect from light |
| 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。 |
||
| 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 | |||
 |
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Organic cation transporter 1 mediates the uptake of monocrotaline and plays an important role in its hepatotoxicity
Toxicology 2013 Sep 15;311(3):225-30.PMID:23831208DOI:10.1016/j.tox.2013.06.009.
Monocrotaline (MCT) is a kind of toxic retronecine-type pyrrolizidine alkaloids (PAs) from plants of Crotalaria, which can be bio-activated by cytochrome P450 (CYP) enzymes in liver and then induce hepatotoxicity. Since CYPs are localized in the endoplasmic reticulum, the influx of MCT to the liver is the key step for its hepatotoxicity. The objective of the present study was to investigate the role of organic cation transporter 1 (OCT1), a transporter mainly expressed in liver, in the uptake of MCT and in hepatotoxicity induced by MCT. The results revealed that MCT markedly inhibited the uptake of 1-methyl-4-phenylpyridinium (MPP(+)), an OCT1 substrate, in Madin-Darby canine kidney (MDCK) cells stably expressing human OCT1 (MDCK-hOCT1) with the IC50 of 5.52±0.56μM. The uptake of MCT was significantly higher in MDCK-hOCT1 cells than in MDCK-mock cells, and MCT uptake in MDCK-hOCT1 cells followed Michaelis-Menten kinetics with the Km and Vmax values of 25.0±6.7μM and 266±64pmol/mg protein/min, respectively. Moreover, the OCT1 inhibitors, such as quinidine, D-Tetrahydropalmatine (d-THP), obviously inhibited the uptake of MCT in MDCK-hOCT1 cells and isolated rat primary hepatocytes, and attenuated the viability reduction and LDH release of the primary cultured rat hepatocytes caused by MCT. In conclusion, OCT1 mediates the hepatic uptake of MCT and may play an important role in MCT induced-hepatotoxicity.
Effects of tetrahydroprotoberberines on dopamine receptor subtypes in brain
Zhongguo Yao Li Xue Bao 1989 Mar;10(2):104-10.PMID:2530755doi
The effects of 12 tetrahydroprotoberberines (THPBs) on D1 and D2 receptors labelled with [3H]DA, [3H]Sch-23390 and [3H]spiperone were evaluated. Their effects on the activity of adenylate cyclase stimulated with DA 40 mumols/L were also assessed. All of the l-THPBs tested behaved as DA receptor antagonists with preferential affinity toward the D1 receptors. Among them, l-stepholidine (l-SPD), a THPB analog with 2 hydroxy groups at the C2 and C10 positions, was the most potent. Its affinity toward D1 receptors was 4-7 times higher than that toward D2 receptors. The results suggest that the hydroxy groups in l-THPBs are very important factors in determining the affinity to DA receptors. Moreover, D-Tetrahydropalmatine (d-THP), a dextro-THPB analog, displayed no affinity for the D2 receptor subtype, while its optical isomer, l-THP, was a DA receptor antagonist. This indicates that the levo-optical configuration is necessary for the affinity of THPBs to DA receptors. In addition, l-SPD was 18 times more potent than haloperidol with respect to binding to D1 receptors, but 14 times weaker for D2 receptors. Thus, it is expected that the clinical effects of l-SPD can be distinguished from that of haloperidol.