盐酸药根碱

中文名称:

盐酸药根碱

中文同义词:

药根碱盐酸盐;盐酸药根碱;盐酸药根碱, 来源于十大功劳;盐酸药根碱(标准品);盐酸药根碱(药根碱盐酸盐);酸盐药根碱

英文名称:

JATRORRHIZINE HCL(RG)

英文同义词:

JATRORRHIZINE HCL(RG);Jatorrhizine, chloride;Jatrochizine chloride;Nsc150445;Neprotine chloride;Jatrorrhizine，Neprotine chloride，Yatrorhizine chloride;Yatrorhizine chloride;Jatrorrhizine hydrochloride, 98%, from Mahonia fortunei (Lindl.) Fedde

CAS号:

6681-15-8

分子式:

C20H20NO4.ClH

分子量:

374.842

EINECS号:

相关类别:

标准品;中药对照品;植物提取物;对照品;无机碱;中药标准品;植提标准品;分析试剂标准品;分析试剂-对照品

Mol文件:

6681-15-8.mol

熔点 

208-210 °C(Solv: methanol (67-56-1))

储存条件 

Inert atmosphere,Room Temperature

生物活性

Jatrorrhizine chloride 是从黄连中分离得到的生物碱，具有神经保护、抗菌、抗疟原虫和抗氧化活性。Jatrorrhizine chloride 是有效的，具有口服活性的乙酰胆碱酯酶 (AChE) (IC50=872 nM) 的抑制剂，是对 BuChE 的选择性为 115 倍。Jatrorrhizine chloride 通过抑制 uptake-2 transporter 的活性减少血清素 (5-HT) 和去甲肾上腺素 (NE) 的摄取。

靶点

Target Value AChE () 872 nM

Target

Value

AChE ()

872 nM

体外研究

Jatrorrhizine has antiplasmodial and antiamoebic activity, it against Plasmodium falciparum and E. histolytica with IC 50 values of 3.15 and 82.7 µM, respectively.The hOCT2 (organic cation transporter 2), hOCT3, and PMAT (plasma membrane monoamine transporter) are capable of transporting monoamine neurotransmitters in the brain. Jatrorrhizine has the inhibitory potency of jatrorrhizine on 5-HT and NE uptake in hOCT2-, hOCT3-, and PMAT-transfected cells. Jatrorrhizine strongly inhibits PMAT-mediated MPP + uptake with an IC 50 value of 1.05 μM and reduces 5-HT and NE uptake mediated by hOCT2, hOCT3, and hPMAT with IC 50 values of 0.1-1 μM (for OCT2 and OCT3) and 1-10 μM (for PMAT).Clearance of neurotransmitters released into the synaptic cleft is defined by two distinct processes. Uptake-1, the common target of current applied antidepressants, is comprised of the serotonin transporter (SERT), the “SERT”, had a high affinity but low capacity to take up [3H]5-HT. Uptake-2 transporters are an important supplementary regulation system in monoamine clearancethought to be the “NET”, has low affinity but high capacity to take up [ 3 H]5-HT into brain slices. Jatrorrhizine significantly inhibited 5-HT and NE uptake in synaptosomes at 25 μM and 50 μM.

体内研究

Jatrorrhizine chloride (intraperitoneal injection; 5, 10, 20 mg/kg) can significantly reduce the duration of immobility when compared with vehicle control group in tail suspension test (TST). Animal Model: Male ICR albino mice Dosage: 5, 10, 20 mg/kg Administration: Intraperitoneal injection; 5, 10, 20 mg/kg Result: Reduced immobility period in tail suspension test.

Animal Model:

Male ICR albino mice

Dosage:

5, 10, 20 mg/kg

Administration:

Intraperitoneal injection; 5, 10, 20 mg/kg

Result:

Reduced immobility period in tail suspension test.

海关编码 

29399990