4-P-PDOT

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT 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).

Neuroscience-Neuromodulation

[1].Dubocovich ML. Melatonin receptors: are there multiple subtypes? Trends Pharmacol Sci. 1995 Feb; 16(2):50-6. | [2].hin EJ, et al. Melatonin attenuates memory impairment induced by Klotho gene deficiency via interactive signaling between MT2 receptor, ERK, and Nrf2-related antioxidant potential. Int J Neuropsychopharmacol. 2014 Dec 30; 18(6). pii: pyu105. | [3].Christopher Browning, et al. Pharmacological characterization of human recombinant melatonin mt1 and MT2 receptors. British Journal of Pharmacology (2000) 129, 877-886. | [4].Dubocovich ML, et al. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar; 355(3):365-75. | [5].Roberto Pariente, et al. Participation of MT3 melatonin receptors in the synergistic effect of melatonin on cytotoxic and apoptotic actions evoked by chemotherapeutics. Cancer Chemother Pharmacol. 2017 Nov; 80(5):985-998.

Neurological Disease

Melatonin Receptor