8-M-PDOT

8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity[1][2].

Signaling Pathways >> Neuronal Signaling >> Melatonin Receptor

Signaling Pathways >> GPCR/G Protein >> Melatonin Receptor

Research Areas >> Neurological Disease

pKi: 8.23 (Melatonin MT2 receptor) and 8.95 (Melatonin MT1 receptor)[2]

8-M-PDOT (10 µg/µL; administrated into the dorsal striatum by bilateral cannulas; for 30 minutes; male Wistar rats) treatment shows anxiolytic-like effect[2]. Animal Model: Male Wistar rats (280-320 g) with Rotenone[2] Dosage: 10 µg/µL Administration: Administrated into the dorsal striatum by bilateral cannulas; for 30 minutes Result: Increased percentage of time spent in the open arms and in the number of open arms entries.

[1]. Browning C, et al. Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors. Br J Pharmacol. 2000 Mar;129(5):877-86.

[2]. Noseda AC, et al. REM sleep deprivation promotes a dopaminergic influence in the striatal MT2 anxiolytic-like effects. Sleep Sci. 2016 Jan-Mar;9(1):47-54.