2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. Opioid Receptor Calcium Channel
  4. Mitragynine

Mitragynine  (Synonyms: (-)-Mitragynine)

目录号: HY-119645 纯度: 99.75%
COA 产品使用指南

摩尔计算器

Mitragynine ((-)-Mitragynine) 是一种精神类化合物。Mitragynine 对 μ-阿片受体 (μ-opioid receptors) 有较高的亲和力，通过作用于脊椎上的 μ- 和 δ- 阿片受体来发挥镇痛作用。Mitragynine 可抑制神经母细胞瘤细胞 Ca2+ 通道 (calcium channel) 电流，也能抑制豚鼠输精管对电刺激的抽搐反应。具有止痛、止咳、止泻、肾上腺素能和抗疟活性。

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Mitragynine Chemical Structure

Mitragynine Chemical Structure

CAS No. : 4098-40-2

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Mitragynine 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mitragynine ((-)-Mitragynine) is a psychoactive compound. Mitragynine has a high affinity to μ-opioid receptors, acts at supraspinal μ- and δ-opioid receptors for its antinociceptive effects. Mitragynine can inhibit Ca2+ channel currents in neuroblastoma cells and inhibit the twitch response to electrical stimulation in guinea-pig vas deferens. Analgesic, antitussive, antidiarrheal, adrenergic, antimalarial activity[1][2].

IC50 & Target[1]

L-type calcium channel

 

μ Opioid Receptor/MOR

 

δ Opioid Receptor/DOR

 

体外研究
(In Vitro)

Mitragynine (1 μM) blocks T- and L-type Ca2+ channel currents in N1E-115 neuroblastoma cells[2].
Mitragynine (10 nM-1 μM) reduces KCl-induced Ca2+ influx in neuroblastoma cells[2].

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

Mitragynine 相关抗体:
体内研究
(In Vivo)

Mitragynine (300 nM-10 μM) inhibits the twitch response to electrical stimulation in guinea-pig vas deferens in a concentration-dependent manner[2].
Mitragynine (3-10 μM) inhibits nicotine-induced (1 mM) contraction of guinea-pig vas deferens in a concentration-dependent manner[2].
Mitragynine (1.5 mg/kg for IV, 50 mg/kg for PO, single dosage) exhibits a biphasic elimination from plasma, and the oral absorption is slow, prolonged and incomplete[3].
Pharmacokinetic Parameters of Mitragynine in male Sprague-Dawley rats[3].

IV (1.5 mg/kg) PO (50 mg/kg)
Cmax (μg/mL) 2.3±1.2 0.70±0.21
Tmax (hr) 1.2±1.1 4.5±3.6
t1/2 (h) 2.9±2.1 6.6±1.3
Abs t1/2 (h) 1.72±0.90
AUC0-∞ (μg/mL·h) 9.2±6.5 8.2±3.0
CL (L/h·kg) 0.29±0.27 7.0±3.0
Vd (L/kg) 0.79±0.42 64±23
F (%) 3.03±1.47

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

Animal Model: Male Sprague-Dawley rats (12-16 weeks old, 280-315 g)[3]
Dosage: 1.5 mg/kg for IV, 50 mg/kg for PO
Administration: IV or PO, single dosage (Pharmacokinetic analysis)
Result: Exhibited a biphasic elimination from plasma, and the oral absorption was slow, prolonged and incomplete, with a calculated absolute oral bioavailability value of 3.03%.
分子量

398.50

Formula

C23H30N2O4
CAS 号
性状

固体

颜色

Light yellow to yellow

初始来源
运输条件

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

-20°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
参考文献

Mitragynine 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Mitragynine4098-40-2(-)-MitragynineOpioid ReceptorCalcium ChannelCa2+ channelsCa channelsopioidanalgesicantitussiveantidiarrhealadrenergicantimalarialantinociceptiveneuroblastoma cellsguinea-pigvas deferensN1E-115Inhibitorinhibitorinhibit

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