Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.
説明 | Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats. |
In vivo | Piromelatine (Neu-P11) has been shown to inhibit weight gain and improve insulin sensitivity in high-fat/high-sucrose-fed (HFSD) rats. The objective of this study was to investigate the effects of piromelatine on insulin sensitivity in sleep-restricted rats. Sleep restriction was established by rotating cages intermittently for 20h thereby sleeping time of rats was limited to 4 hours per day. During 8 days of sleep restriction, rats were injected intraperitoneally with piromelatine (20mg/kg), melatonin (5mg/kg), or a vehicle. The results showed that sleep restriction increased plasma glucose, fasting insulin, total cholesterol (TC), triglycerides (TG), and oxidative stress markers while HDL-cholesterol (HDL-C) level and glucose tolerance were decreased. However, under piromelatine or melatonin treatment, the levels of plasma glucose, TG, and TC decreased and HDL-C, glucose tolerance, and antioxidative potency increased when compared with the vehicle-treated group. Piromelatine could regulate metabolic profiles and insulin sensitivity, and attenuate insulin resistance induced by sleep restriction.[3] |
別名 | NEU-P-11, NEU-P 11, NEU-P11 |
分子量 | 312.32 |
分子式 | C17H16N2O4 |
CAS No. | 946846-83-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (320.18 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Piromelatine 946846-83-9 GPCR/G Protein Membrane transporter/Ion channel Neuroscience P2X Receptor MT Receptor 5-HT Receptor Sodium Channel TRP/TRPV Channel NEU-P-11 NEU-P 11 NEU-P11 Inhibitor inhibitor inhibit