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Mitragynine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mitragynine图片
CAS NO:4098-40-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
(-)-Mitragynine
产品介绍
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。
生物活性

Mitragynine ((-)-Mitragynine) is a psychoactive compound. Mitragynine has a high affinity toμ-opioid receptors, acts at supraspinal μ- and δ-opioid receptors for its antinociceptive effects. Mitragynine can inhibitCa2+channelcurrents 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].

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±1.20.70±0.21
Tmax(hr)1.2±1.14.5±3.6
t1/2(h)2.9±2.16.6±1.3
Abs t1/2(h)1.72±0.90
AUC0-∞(μg/mL·h)9.2±6.58.2±3.0
CL (L/h·kg)0.29±0.277.0±3.0
Vd(L/kg)0.79±0.4264±23
F (%)3.03±1.47

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

4098-40-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.