8-M-PDOT

Product Name8-M-PDOT
CAS134865-70-6
MFC14H19NO2
MW233.31
EINECS
MOL File134865-70-6.mol

Chemical Properties

Boiling point	447.8±45.0 °C(Predicted)
Density	1.09±0.1 g/cm3(Predicted)
storage temp.	Store at RT
solubility	Soluble to 50 mM in ethanol and to 100 mM in DMSO
form	Powder
pka	15.87±0.20(Predicted)
color	White to off-white

Usage And Synthesis

Description

8-M-PDOT is a melatonin receptor 2 (MT₂) agonist (K_i = 1.12 nM). It is 5.2-fold selective for MT₂ over MT₁ receptors in a radioligand binding assay. Striatal microinfusion of 8-M-PDOT (10 μg/μl) increases the percentage of time spent in the open arms of the elevated plus maze, indicating anxiolytic-like activity, in a rat model of rotenone-induced Parkinson''s disease.

Uses

AH 002 is a selective melatonin receptor agonist.

Biological Activity

Melatonin receptor agonist, 20-fold selective for the MT 2 (vs MT 1 ) subtype. At human recombinant MT 1 and MT 2 receptors, displays pK i values of 8.23 and 8.95 respectively.

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:	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.

IC 50

MT2

References

[1] CHRISTOPHER BROWNING. Pharmacological characterization of human recombinant melatonin mt1 and MT2 receptors[J]. British Journal of Pharmacology, 2009, 129 5: 877-886. DOI: 10.1038/sj.bjp.0703130
[2] ANA CAROLINA D. NOSEDA. REM sleep deprivation promotes a dopaminergic influence in the striatal MT2 anxiolytic-like effects[J]. Sleep Science, 2016, 9 1: Pages 47-54. DOI: 10.1016/j.slsci.2015.10.002

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