2. Neuronal Signaling Membrane Transporter/Ion Channel GPCR/G Protein
  3. Serotonin Transporter Potassium Channel Arrestin Opioid Receptor
  4. Noribogaine hydrochloride

Noribogaine hydrochloride 是一种口服有效、能透过血脑屏障的 SERT 抑制剂 (IC50=50-300 nM) 和 hERG 通道阻滞剂。Noribogaine hydrochloride 能增强血清素能传递，激活 κ-阿片受体 (OPRK) G 蛋白信号通路并抑制 β-arrestin 招募。同时，Noribogaine hydrochloride 阻断 μ-阿片受体 (OPRM) 信号通路以及与心脏复极化相关的离子通道。Noribogaine hydrochloride 可诱导神经突生成、上调 GDNF mRNA 表达、调节阿片类药物耐受性。Noribogaine hydrochloride 可降低实验动物主动寻求酒精的行为，已被广泛应用于抑郁症、成瘾症、酒精成瘾以及心脏毒性等相关领域的研究。

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Noribogaine hydrochloride

Noribogaine hydrochloride Chemical Structure

CAS No. : 110514-35-7

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规格 价格 是否有货 数量
500 μg ￥2739
In-stock
1 mg ￥4382
In-stock
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Noribogaine hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity[1][2][3][4].
IC50 & Target

κ Opioid Receptor/KOR

 

μ Opioid Receptor/MOR

 

体外研究
(In Vitro)

Noribogaine hydrochloride 是一种 OPRK 的部分激动剂，刺激 [35S]GTPγS 结合的最大效应值 Emax=72%，EC50 为 8.75 µM。Noribogaine hydrochloride 与人 OPRK 的结合亲和力 (Ki=720 nM) 高于与人 OPRM 的结合亲和力 (Ki=1520 nM)[1]。

Noribogaine hydrochloride (5-50 μM; 1-6 h) 可强效诱导人神经母细胞瘤细胞系 SH-SY5Y 中 GDNF 的表达呈剂量依赖性升高[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Noribogaine hydrochloride 相关抗体:

RT-PCR[2]

Cell Line: SH-SY5Y human neuroblastoma cells
Concentration: 5-50 μM
Incubation Time: 1 h; 3 h; 6 h
Result: Induced a dose-dependent increase in GDNF expression similar to ibogaine, with a statistically significant effect for the 3-hour incubation.
Increased GDNF expression at 1 hour and 6 hours of incubation.
体内研究
(In Vivo)

Noribogaine hydrochloride (10-40 mg/kg; i.p.) 在 10 和 20 mg/kg 剂量下可恢复吗啡耐受小鼠的吗啡抗伤害感受活性，在 40 mg/kg 剂量下可增强吗啡诱导的镇痛作用，并可预防吗啡镇痛耐受的形成[1]。
Noribogaine hydrochloride 可在大鼠体内对多种成瘾剂的自身给药行为产生持久的抑制作用[1]。
Noribogaine hydrochloride (40 mg/kg；i.p.；单次) 在大鼠单次腹腔注射 40 mg/kg Ibogaine 后可达到较高的脑内浓度 (-20 μM)，且具有优异的血脑屏障通透性，并可诱导中枢介导的催乳素释放[1]。
Noribogaine hydrochloride (1-100 μM；i.p.；持续 2 分钟；操作性自给药实验开始前 3 小时) 可显著、呈剂量依赖性且持久地降低有高自愿饮酒史大鼠的操作性乙醇自给药行为[2]。
Noribogaine (20-40 mg/kg；i.p.；单次给药) hydrochloride 在大鼠腹腔注射单次 40 mg/kg 给药后 0.5 小时可诱导剂量依赖性的类抗抑郁作用，而给药后 3 小时或 20 mg/kg 剂量组未观察到显著作用[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (adult male, 290-320 g for behavioral studies; 8-12 week old male, 280-300 g for pharmacokinetic studies)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; single dose
Result: Induced a significant decrease in immobility time and the 20 mg/kg dose at 0.5 hours post-40 mg/kg administration.
Showed no significant changes in swimming or climbing behavior at 0.5 hours post-administration.
Did not significantly alter locomotor activity in the open field test at 40 mg/kg dose.
Exhibited no significant effect on immobility time, swimming time, or climbing time at 3 hours post-administration.
Reached brain concentrations of 144 μM at 0.5 hours post-40 mg/kg dose and 31 μM at 3 hours post-40 mg/kg dose.
Animal Model: Long-Evans rats with Alcohol use disorder (male, 280-300 g)[2]
Dosage: 0.8 μl of 1 μM (3 ng/μl); 0.8 μl of 10 μM (30 ng/μl); 0.8 μl of 100 μM (300 ng/μl)
Administration: Intra-VTA infusion; over 2 minutes; 3 hours prior to operant self-administration sessions
Result: Significantly reduced operant responding for ethanol.
Significantly reduced ethanol intake.
Produced a long-lasting decrease in ethanol deliveries that persisted for more than 48 hours post-infusion at 10 μM dose.
Produced a long-lasting decrease in ethanol intake that persisted for more than 48 hours post-infusion at 10 μM dose.
Exhibited similar long-lasting effects on ethanol deliveries and intake at 100 μM dose.
分子量

332.87

Formula

C19H25ClN2O
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料

纯度: 99.9%

COA (269 KB) MS (185 KB)

产品使用指南 (1538 KB)
参考文献

Noribogaine hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Noribogaine110514-35-7Serotonin TransporterPotassium ChannelArrestinOpioid Receptor5-HTTSERTSLC6A4KcsAOPRMhERG channelhiPSC-CMsOPRKCaco-2 cellshuman liver microsomesCHO-K1 cellsratsSH-SY5Y human neuroblastoma cellsInhibitorinhibitorinhibit

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