8-M-PDOT
8-M-PDOT Basic information
- Product Name:
- 8-M-PDOT
- Synonyms:
-
- 8-METHOXY-2-PROPIONAMIDOTETRALIN
- 8-M-PDOT
- AH 002
- 8 M PDOT,8MPDOT
- Propanamide, N-(1,2,3,4-tetrahydro-8-methoxy-2-naphthalenyl)-
- 8-M-PDOT, 10 mM in DMSO
- CAS:
- 134865-70-6
- MF:
- C14H19NO2
- MW:
- 233.31
- Mol File:
- 134865-70-6.mol
8-M-PDOT 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
8-M-PDOT Usage And Synthesis
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
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