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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Membrane Transporter & Ion Channel > ReserpineCAS：50-55-5
Molecular Formula：C33H40N2O9
Molecular Weight：608.68
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 50-55-5 |
| Name | Reserpine |
| Molecular Formula | C33H40N2O9 |
| Molecular Weight | 608.68 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 200-047-9 |
| MDL | MFCD00005091 |
| SMILES | O=C([C@H]([C@@H](OC)[C@H](OC(C1=CC(OC)=C(OC)C(OC)=C1)=O)C[C@]2([H])CN3CC4)[C@@]2([H])C[C@]3([H])C5=C4C(C=CC(OC)=C6)=C6N5)OC |
| InChIKey | QEVHRUUCFGRFIF-MDEJGZGSSA-N |
| InChI | InChI=1S/C33H40N2O9/c1-38-19-7-8-20-21-9-10-35-16-18-13-27(44-32(36)17-11-25(39-2)30(41-4)26(12-17)40-3)31(42-5)28(33(37)43-6)22(18)15-24(35)29(21)34-23(20)14-19/h7-8,11-12,14,18,22,24,27-28,31,34H,9-10,13,15-16H2,1-6H3/t18-,22+,24-,27-,28+,31+/m1/s1 |
| PubChem CID | 5770 |
| Target Point | VMAT2 |
| Passage | Membrane Transporter&Ion Channel |
| Background | Reserpine is an inhibitor of vesicular monoamine transporter 2 (VMAT2). |
| Biological Activity | Reserpine 是囊泡单胺转运蛋白 2 (VMAT2) 的抑制剂。[1-3] |
| In Vitro | 利血平是囊泡单胺转运蛋白2(VMAT2)的抑制剂。利血平对大鼠纹状体中多巴胺D1受体密度(F2，12 = 8.81，p <0.01)有显著影响。在急性和慢性利血平给药期间多巴胺D1和D2受体的亲和力(Kd)没有变化[1]。在利血平分别在JB6 P +和HepG2-C8细胞中处理1天后，获得43.9和54.9μM的IC 50值。利血平在浓度范围为5至50μM时以剂量依赖性方式诱导荧光素酶活性，并且在低于5μM的浓度下未观察到显著诱导。结果表明，利血平(2.5至10μM)也增加了Nrf2，HO-1和NQO1的蛋白质表达。浓度为2.5至10μM的利血平在处理7天后以浓度依赖性方式降低DNMT1，DNMT3a和DNMT3b的mRNA表达。 10μM的利血平对DNMT3a表达产生显著差异(p <0.05)[2]。 |
| In Vivo | 以0.2 mg / kg腹腔注射的剂量从慢性(14天)但不是急性利血平给药中退出(48小时)，使得不动时间显著减少(F2，18 = 3.68，p <0.05)，但增加了攀爬时间(F2，18 = 4.48，p <0.02)，并且在大鼠强迫游泳试验(FST)中不改变游泳时间(F2，18 = 1.78; NS)[1]。与对照动物相比，剂量为5mg / kg体重的利血平使香草扁桃酸(VMA)的尿排泄特征显著增加。发现用利血平治疗的动物排出的5-羟基吲哚乙酸(5-HIAA)的量多于对照组。利血平观察到剂量依赖性低血压。与对照组相比，剂量为0.5，1，5，10和15μg/ kg的利血平可使血压显著降低(p <0.01)[3]。 |
| Cell Experiment | 将JB6 P +细胞接种于含有最小必需培养基(MEM)的96孔板中，密度为1×10 4细胞/ mL(100μL/孔)，持续1，3和5天，并将HepG2-C8细胞接种于含有DMEM的平板。温育24小时后，用DMSO或各种浓度的利血平处理细胞。对于JB6 P +细胞，培养基每2天更换一次，进行3天和5天的治疗。根据制造商的说明使用MTS测定试剂盒评估细胞活力。在490nm处读取甲product产物的吸光度，并计算细胞活力并与DMSO对照组比较[2]。 |
| Animal Experiment | 在该研究中使用重量在100至150g之间的任一性别的Albino大鼠。它们在实验前至少10天适应实验室条件，并随意提供标准饮食和水，12小时光照和黑暗循环。将动物分成不同的组，每组6只，并分别饲养在代谢笼中。第1组：以0.1mL/100g体重的剂量腹膜内用DMSO处理的对照动物。第2组：以5mg/kg体重的剂量腹膜内给予利血平的动物。从每个动物收集药物施用点的24小时尿样[3]。 |
| Kinase Experiment | 孵育24小时后，用各种浓度的利血平处理JB6P +细胞(1×105细胞/ 10-cm培养皿)。使用补充有蛋白酶抑制剂混合物的放射免疫沉淀测定缓冲液从处理的细胞制备全细胞裂解物，并使用BCA试剂盒测定蛋白质浓度[2]。 |
| Data Literature Source | [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. |
| Unit | Bottle |
| Specification | 20mg 10mM*1mL in DMSO 100mg |
Reserpine 是囊泡单胺转运蛋白 2 (VMAT2) 的抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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