Description
8-M-PDOT is a melatonin receptor 2 (MT
2) agonist (K
i = 1.12 nM). It is 5.2-fold selective for MT
2 over MT
1 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.
|
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
