Bioactivity | 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]. | ||||||||||||
Target | pKi: 8.23 (Melatonin MT2 receptor) and 8.95 (Melatonin MT1 receptor) | ||||||||||||
In Vivo | 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: | ||||||||||||
Name | 8-M-PDOT | ||||||||||||
CAS | 134865-70-6 | ||||||||||||
Formula | C14H19NO2 | ||||||||||||
Molar Mass | 233.31 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |