| CAS |
No.50-55-5 |
| 中文名称 |
利血平(10mM in DMSO,无菌） |
| 英文名称 |
Reserpine(10mM in DMSO，Sterile） |
| 分子式 |
C33H40N2O9 |
| 分子量 |
608.68 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
VMAT2 |
| 通路 |
Membrane Transporter&Ion Channel |
| 背景说明 |
Reserpine 是囊泡单胺转运蛋白 2 (VMAT2) 的抑制剂。 |
| 生物活性 |
Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).[1] |
| In Vitro |
Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2). Reserpine displays a significant effect on the density of dopamine D1 receptors (F2，12=8.81， p[1]. IC50 values of 43.9 and 54.9 μM are obtained after 1 day of treatment with Reserpine in JB6 P+ and HepG2-C8 cells， respectively. Reserpine induces luciferase activity in a dose-dependent manner at concentrations ranging from 5 to 50 μM， and no significant induction is observed at concentrations lower than 5 μM. Results demonstrate that Reserpine (2.5 to 10 μM) also increases the protein expression of Nrf2， HO-1， and NQO1. Reserpine at concentrations of 2.5 to 10 μM decreases the mRNA expression of DNMT1， DNMT3a， and DNMT3b in a concentration-dependent manner in JB6 P+ cells after 7 days of treatment. Reserpine at 10 μM generates a significant difference for DNMT3a expression (p[2]. |
| 细胞实验 |
JB6 P+ cells are seeded in 96-well plates containing Minimum essential media (MEM) at a density of 1×104 cells/mL (100 μL/well) for 1， 3， and 5 days， and HepG2-C8 cells are seeded in plates containing DMEM. After incubation for 24 h， the cells are treated with either DMSO or various concentrations of Reserpine. For JB6 P+ cells， the medium is changed every 2 days for the 3-day and 5-day treatments. Cell viability is assessed using a MTS assay kit according to the manufacturer’s instructions. The absorbance of the formazan product is read at 490 nm， and the cell viability is calculated and compared with the DMSO control group[2]. |
| 动物实验 |
Albino rats of either sex weighing between 100 to 150 g are used in the study. They are acclimatized to the laboratory conditions for at least 10 days prior to the experiment and provided with standard diet and water ad libitum with 12 h light and dark cycle. Animals are divided into different groups of six each and are housed individually in metabolic cages. Group 1: Control animals treated with DMSO intraperitoneally at a dose of 0.1 mL/100 g body weight. Group 2: Animals administered intraperitoneally with Reserpine at a dose of 5 mg/kg body weight. The 24 h urine samples from the point of drug administration are collected for each animal[3]. |
| 激酶实验 |
After incubation for 24 h， JB6 P+ cells (1×105 cells/10-cm dish) are treated with various concentrations of Reserpine. Whole cell lysates are prepared from the treated cells using radioimmunoprecipitation assay buffer supplemented with a protease inhibitor cocktail， and a BCA kit is used to determine protein concentrations[2]. |
| 数据来源文献 |
[1]. Antkiewicz-Michaluk L， et al. Withdrawal from repeated administration of a low dose of reserpine induced opposing adaptive changes in the noradrenaline and serotonin system function: a behavioral and neurochemical ex vivo and in vivo studies in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2015 Mar 3;57:146-54.
[2]. Hong B， et al. Reserpine Inhibit the JB6 P+ Cell Transformation Through Epigenetic Reactivation of Nrf2-Mediated Anti-oxidative Stress Pathway. AAPS J. 2016 May;18(3):659-69.
[3]. Sreemantula S， et al. Reserpine methonitrate， a novel quaternary analogue of reserpine augments urinary excretion of VMA and 5-HIAA without affecting HVA in rats. BMC Pharmacol. 2004 Nov 16;4:30. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号