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 |
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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].
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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 |
| 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%. |
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| 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. |
