Piromelatine

Research use only, not for human use.

A novel melatonin melatonin receptor MT1/MT2 and serotonin 5-HT1A/5-HT1D receptor agonist.

A novel melatonin melatonin receptor MT1/MT2 and serotonin 5-HT1A/5-HT1D receptor agonist; inhibits weight gain and improves insulin sensitivity in high-fat/high-sucrose-fed rats; facilitates memory performance and improves cognitive impairment in a rat model of Alzheimer' disease.Alzheimer Disease Phase 2 Clinical.

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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% 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, 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.

Neu-P11

GPCR/G Protein

Melatonin Receptor

Melatonin Receptor

Neurological Disease

Alzheimer Disease

946846-83-9

312.32

C17H16N2O4

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (800.46 mM)

O=C(C1=CC(C=CO1)=O)NCCC2=CNC3=C2C=C(OC)C=C3

N-[2-(5-Methoxy-1H-indol-3-yl)ethyl]-4-oxo-4H-pyran-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years