利血平作用機制 - Medchemexpress - MCE中國

1、Product Data SheetReserpineCat. No.: HY-N0480CAS No.: 50-55-5分式: CHNO分量: 608.68作靶點: Monoamine Transporter; Autophagy作通路: Membrane Transporter/Ion Channel; Autophagy儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數據體外實驗 DMSO : 25 mg/mL (41.07 mM; Need ul

2、trasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.6429 mL 8.2145 mL 16.4290 mL5 mM 0.3286 mL 1.6429 mL 3.2858 mL10 mM 0.1643 mL 0.8214 mL 1.6429 mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存時，請在 6 個內使，-20C 儲存時，

3、請在 1 個內使。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現現配，當天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現沉淀、析出現象，可 以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.11 mM); Clear solution此案可獲得 2.5

4、 mg/mL (4.11 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.11 mM); Clear solution此案可獲得 2.5 mg/mL (4.11 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L

5、 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性 Reserpine囊泡單胺轉運蛋 2 (VMAT2) 的抑制劑。IC & Target VMAT21體外研究 Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2). Reserpine displays a significant effect onthe density of dopamine D1 receptors (F2

6、,12=8.81, p0.01) in the rat striatum. The affinity (Kd) for the dopamine D1and D2 receptors during withdrawal from acute and chronic administration of reserpine is not change1. IC50 valuesof 43.9 and 54.9 M are obtained after 1 day of treatment with Reserpine in JB6 P+ and HepG2-C8 cells, respective

7、ly.Reserpine induces luciferase activity in a dose-dependent manner at concentrations ranging from 5 to 50 M, and nosignificant induction is observed at concentrations lower than 5 M. Results demonstrate that Reserpine (2.5 to 10 M) also increases the protein expression of Nrf2, HO-1, and NQO1. Rese

8、rpine at concentrations of 2.5 to 10 Mdecreases 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 M generates a significant difference for DNMT3a expression (p0.05)2.體內研究 Withdrawal (48 h) from chronic (14-d

9、ay) but not acute Reserpine administration in a dose of 0.2 mg/kg i.p. producesa significant reduction of the immobility time (F2,18=3.68, p0.05), but increases the climbing time (F2,18=4.48,p0.02), and does not change the swimming time (F2,18=1.78; NS) in the forced swim test (FST) in rats1. Reserp

10、ine ata dose of 5 mg/kg body weight produces significant increase in the urinary excretion profile of vanillylmandelic acid(VMA) compare to control animals. The amount of 5-hydroxyindoleacetic acid (5-HIAA) excreted in animals treatedwith Reserpine is found to be more than in the control. Dose depen

11、dent hypotension is observed with Reserpine.Reserpine at doses of 0.5, 1, 5, 10 and 15 g/kg produce significant (p0.01) reduction in blood pressure compare tocontrol3.PROTOCOLKinase Assay 2 After incubation for 24 h, JB6 P+ cells (1105 cells/10-cm dish) are treated with various concentrations ofRese

12、rpine. Whole cell lysates are prepared from the treated cells using radioimmunoprecipitation assay buffersupplemented with a protease inhibitor cocktail, and a BCA kit is used to determine protein concentrations2.MCE has not independently confirmed the accuracy of these methods. They are for referen

13、ce only.Cell Assay 2 JB6 P+ cells are seeded in 96-well plates containing Minimum essential media (MEM) at a density of 1104 cells/mL(100 L/well) for 1, 3, and 5 days, and HepG2-C8 cells are seeded in plates containing DMEM. After incubation for 24h, the cells are treated with either DMSO or various

14、 concentrations of Reserpine. For JB6 P+ cells, the medium ischanged every 2 days for the 3-day and 5-day treatments. Cell viability is assessed using a MTS assay kit according tothe manufacturers instructions. The absorbance of the formazan product is read at 490 nm, and the cell viability iscalcul

15、ated and compared with the DMSO control group2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Albino rats of either sex weighing between 100 to 150 g are used in the study. They are acclimatized to theAdministration 3 laboratory conditions for a

16、t least 10 days prior to the experiment and provided with standard diet and water adlibitum with 12 h light and dark cycle. Animals are divided into different groups of six each and are housedindividually in metabolic cages. Group 1: Control animals treated with DMSO intraperitoneally at a dose of 0

17、.1mL/100 g body weight. Group 2: Animals administered intraperitoneally with Reserpine at a dose of 5 mg/kg bodyweight. The 24 h urine samples from the point of drug administration are collected for each animal3.MCE has not independently confirmed the accuracy of these methods. They are for referenc

18、e only.Page 2 of 3 www.MedChemEREFERENCES1. Antkiewicz-Michaluk L, et al. Withdrawal from repeated administration of a low dose of reserpine induced opposing adaptive changes in thenoradrenaline and serotonin system function: a behavioral and neurochemical ex vivo and in vivo studies in the rat. Prog Neuropsychopharmacol BiolPsychiatry. 2015 Mar 3;57:146-54.