Piromelatine

Piromelatine (Neu-P11) 是褪黑素受体 MT1/MT2 的激动剂，是 5-HT1A 和 5-HT1D 的激动剂，也是 5-HT2B 的拮抗剂。Piromelatine (Neu-P11) 有用于促进睡眠、缓解疼痛、抗神经退行性和抗抑郁等研究的潜能。Piromelatine (Neu-P11) 还具有抑制疼痛相关靶点 P2X3、TRPV1和 Nav1.7 通道的活性。 Piromelatine (Neu-P11) is a melatonin MT 1 /MT 2 receptor agonist, serotonin 5-HT 1A / 5-HT 1D agonist, and serotonin 5-HT 2B 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 In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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% and 43.0%, 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, F 1,24 =15.7, p IC50& Target:MT 1 MT 2 5-HT 1A Receptor 5-HT 1D Receptor 5-HT 2B Receptor

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