产品
编 号：F351515
分子式：C23H30N2O4
分子量：398.5
分子式：C23H30N2O4
分子量：398.5
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 4098-40-2
产品详情
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.
体内研究：
Mitragynine (300 nM-10 μM) inhibits the twitch response to electrical stimulation in guinea-pig vas deferens in a concentration-dependent manner.Mitragynine (3-10 μM) inhibits nicotine-induced (1 mM) contraction of guinea-pig vas deferens in a concentration-dependent manner.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.Pharmacokinetic Parameters of Mitragynine in male Sprague-Dawley rats.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)
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%.
体外研究：
Mitragynine (1 μM) blocks T- and L-type Ca2+ channel currents in N1E-115 neuroblastoma cells.Mitragynine (10 nM-1 μM) reduces KCl-induced Ca2+ influx in neuroblastoma cells.
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.
体内研究：
Mitragynine (300 nM-10 μM) inhibits the twitch response to electrical stimulation in guinea-pig vas deferens in a concentration-dependent manner.Mitragynine (3-10 μM) inhibits nicotine-induced (1 mM) contraction of guinea-pig vas deferens in a concentration-dependent manner.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.Pharmacokinetic Parameters of Mitragynine in male Sprague-Dawley rats.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)
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%.
体外研究：
Mitragynine (1 μM) blocks T- and L-type Ca2+ channel currents in N1E-115 neuroblastoma cells.Mitragynine (10 nM-1 μM) reduces KCl-induced Ca2+ influx in neuroblastoma cells.
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