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。
| 生物活性 | Piromelatine (Neu-P11) is amelatonin MT1/MT2receptor agonist,serotonin 5-HT1A/5-HT1Dagonist, andserotonin 5-HT2Bantagonist. 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[1][2][3]. |
| IC50& Target | 5-HT1AReceptor | 5-HT1DReceptor | 5-HT2BReceptor | MT1 | MT2 |
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体内研究
(In Vivo) | Piromelatine (20 mg/kg, ip, daily) treatment prevents insulin resistance induced by sleep restriction[1].
Piromelatine (5-50 mg/kg, ip, daily) decreases plasma glucose significantly[2].
Piromelatine (100 mg/kg) decreases thermal hyperalgesia and mechanical allodynia in PSL (partial sciatic nerve ligation) mice[3].
| Animal Model: | Twenty four male Sprague-Dawley rats (3 months old, weighing 250-300 g)[1]. | | 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%).
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| Animal Model: | Five groups of 12-wk-old rats (10/group)[2]. | | 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)[3]. | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(800.46 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2018 mL | 16.0092 mL | 32.0184 mL | | 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | | 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.66 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.66 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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