| Identification | Back Directory | [Name]
8-M-PDOT | [CAS]
134865-70-6 | [Synonyms]
AH 002
8-M-PDOT
8-METHOXY-2-PROPIONAMIDOTETRALIN | [Molecular Formula]
C14H19NO2 | [MDL Number]
MFCD00901636 | [MOL File]
134865-70-6.mol | [Molecular Weight]
233.31 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Description]
8-M-PDOT is a melatonin receptor 2 (MT2) agonist (Ki = 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 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
|