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。
产品描述
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 Ca 2+ 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].
体外活性
Mitragynine (1 μM) blocks T- and L-type Ca 2+ channel currents in N1E-115 neuroblastoma cells [2]. Mitragynine (10 nM-1 μM) reduces KCl-induced Ca 2+ influx in neuroblastoma cells [2].
体内活性
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) C max (μg/mL) 2.3±1.2 0.70±0.21 T max (hr) 1.2±1.1 4.5±3.6 t 1/2 (h) 2.9±2.1 6.6±1.3 Abs t 1/2 (h) 1.72±0.90 AUC 0-∞ (μg/mL·h) 9.2±6.5 8.2±3.0 CL (L/h·kg) 0.29±0.27 7.0±3.0 V d (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%.
Cas No.
4098-40-2
分子式
C23H30N2O4
分子量
398.503
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
