产品
编 号：F534475
分子式：C17H16N2O4
分子量：312.32
分子式：C17H16N2O4
分子量：312.32
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 946846-83-9
产品详情
生物活性：
Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
体内研究：
Piromelatine (20 mg/kg, ip, daily) treatment prevents insulin resistance induced by sleep restriction. Piromelatine (5-50 mg/kg, ip, daily) decreases plasma glucose significantly.Piromelatine (100 mg/kg) decreases thermal hyperalgesia and mechanical allodynia in PSL (partial sciatic nerve ligation) mice.Animal Model:Twenty four male Sprague-Dawley rats (3 months old, weighing 250-300 g).
Dosage:20 mg/kg.
Administration:IP, daily at 8:00 p.m.
Result:Resulted in significantly decreased plasma glucose levels (6.670.35 mmol/L, 6.770.34 mmol/L vs. 8.27 0.38 mmol/L), and the plasma glucose levels of the two groups were even neared to that of the normal control group (6.07±0.35 mmol/L). Resulted in a decrease in triglycerides and total cholesterol levels (51.8% and43.0%, respectively) and an elevation in HDL-C level (increase of 32.4%).
Animal Model:Five groups of 12-wk-old rats (10/group).
Dosage:5-50 mg/kg.
Administration:Intraperitoneal injection in 18:00 every day.
Result:Plasma glucose was decreased significantly by 27.3%, 34.5% and 61.5%, respectively.
Animal Model:Male C57BL/6 J mice, weighing 22-26 g (10 weeks old; PSL mice).
Dosage:25, 50, or 100 mg/kg.
Administration:IP 1 h before assessment of thermal hyperalgesia and mechanical allodynia.
Result:Remarkably prolonged thermal latency (surgery×treatment interaction, F1,24=15.7, p<0.001; surgery×treatment×hours interaction, F5,120=3.0, p<0.05) and increased mechanical threshold (surgery×treatment interaction, F1,24=18.4, p<0.001; surgery× treatment×hours interaction, F5,120=2.6, p<0.05) for 4 h after administration of piromelatine to PSL mice.
Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
体内研究：
Piromelatine (20 mg/kg, ip, daily) treatment prevents insulin resistance induced by sleep restriction. Piromelatine (5-50 mg/kg, ip, daily) decreases plasma glucose significantly.Piromelatine (100 mg/kg) decreases thermal hyperalgesia and mechanical allodynia in PSL (partial sciatic nerve ligation) mice.Animal Model:Twenty four male Sprague-Dawley rats (3 months old, weighing 250-300 g).
Dosage:20 mg/kg.
Administration:IP, daily at 8:00 p.m.
Result:Resulted in significantly decreased plasma glucose levels (6.670.35 mmol/L, 6.770.34 mmol/L vs. 8.27 0.38 mmol/L), and the plasma glucose levels of the two groups were even neared to that of the normal control group (6.07±0.35 mmol/L). Resulted in a decrease in triglycerides and total cholesterol levels (51.8% and43.0%, respectively) and an elevation in HDL-C level (increase of 32.4%).
Animal Model:Five groups of 12-wk-old rats (10/group).
Dosage:5-50 mg/kg.
Administration:Intraperitoneal injection in 18:00 every day.
Result:Plasma glucose was decreased significantly by 27.3%, 34.5% and 61.5%, respectively.
Animal Model:Male C57BL/6 J mice, weighing 22-26 g (10 weeks old; PSL mice).
Dosage:25, 50, or 100 mg/kg.
Administration:IP 1 h before assessment of thermal hyperalgesia and mechanical allodynia.
Result:Remarkably prolonged thermal latency (surgery×treatment interaction, F1,24=15.7, p<0.001; surgery×treatment×hours interaction, F5,120=3.0, p<0.05) and increased mechanical threshold (surgery×treatment interaction, F1,24=18.4, p<0.001; surgery× treatment×hours interaction, F5,120=2.6, p<0.05) for 4 h after administration of piromelatine to PSL mice.
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