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4-P-PDOT is a MT2-receptor-specific antagonist, it is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity). In CHO-MT2 cells, 4-P-PDOT is an agonist, producing a concentration-dependent inhibition of forskolin stimulated cyclic AMP, with a pEC50 value of 8.72 and intrinsic activity of 0.86. In vivo, 4-P-PDOT (0.5-1.0 mg/kg; intravenous injection) treatment on klotho mutant mice significantly reverses antioxidant effects mediated by Melatonin.
Molecular Weight | 279.38 |
Formula | C19H21NO |
CAS Number | 134865-74-0 |
Form | Solid |
Solubility (25°C) | DMSO ≥ 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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8-M-PDOT
8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. |
6-Chloromelatonin
6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. |
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Piromelatine
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. |
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