Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dimemorfan phosphate (3,17-dimethylmorphinan) is a sigma 1 receptor agonist. Dimemorfan phosphate is used as a potent antitussive.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
50 mg | In stock | $ 39.00 | |
100 mg | In stock | $ 59.00 |
Description | Dimemorfan phosphate (3,17-dimethylmorphinan) is a sigma 1 receptor agonist. Dimemorfan phosphate is used as a potent antitussive. |
Targets&IC50 | σ1 receptor:150 nM(Ki) |
In vitro | Dimemorfan (5-20 μM) inhibits both fMLP- and PMA-induced ROS production in a concentration-dependent manner and is relatively more potent in inhibiting fMLP-induced ROS production with an IC50 value of 7.0 μM. Dimemorfan (10-50 μM) does not display significant activity in scavenging free radicals by xanthine/xanthine oxidase system. Dimemorfan significantly suppressed Mac-1 upregulation both in PMA- and fMLP-activated groups. Dimemorfan (10-20 μM) significantly suppresses LPS-induced ROS and NO production, suppresses LPS-induced iNOS protein expression, and both the percentage of the positively stained population and the MCF intensities of MCP-1 and TNF-α in BV2 cytosol. Dimemorfan (20 μM) significantly blocks the degradation of cytosolic Iκ-Bα and nuclear translocation of NF-κB p65 and the transcriptional activity of NF-κB. |
In vivo | Dimemorfan (6.25 or 12.5 mg/kg, s.c.) significantly attenuates the BAY k-8644-induced convulsive behaviors, in a dose-related manner (6.25 mg/kg dimemorfan+BAY k-8644 or 12.5 mg/kg dimemorfan+BAY k-8644 versus Saline+BAY k-8644, P<0.05 and P<0.01, respectively). Dimemorfan significantly attenuates BAY k-8644-induced increases in the c-fos and c-jun protein expression in a dose-dependent manner. Dimemorfan does not significantly affect locomotor activity or produce significant circling behavior in any locomotor pattern in mice. Dimemorfan (1 and 5 mg/kg, i.p.) surpresses the incarease of the plasma levels of TNF-α in mice. The infiltration of neutrophils into lung and liver and the production of oxidative stress (EB staining) in these tissues induced by LPS is obviously inhibited by the treatment with dimemorfan. |
Synonyms | 3,17-dimethylmorphinan |
Molecular Weight | 353.4 |
Formula | C18H25N.H3O4P |
CAS No. | 36304-84-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 10 mM
DMSO: Insoluble
You can also refer to dose conversion for different animals. More
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Dimemorfan phosphate 36304-84-4 GPCR/G Protein Sigma receptor Dimemorfan Phosphate inhibit Inhibitor 3,17-dimethylmorphinan Sigma Receptor Dimemorfan inhibitor