[CAS NO. 36304-84-4] Dimemorfan phosphate
PRODUCTS SPECIFICATIONS [36304-84-4]
DESCRIPTION [36304-84-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 353.39 |
| Molecular Formula | C18H28NO4P |
| SMILES | O=P(O)(O)O.CN1[C@](CC2=CC=C(C)C=C32)([H])[C@](CCCC4)([H])[C@]34CC1 |
1 Publications Citing Use of MCE
Summary
Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
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 IC 50 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, and 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, as well as the transcriptional activity of NF-κB [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 [1] . 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 as well as the production of oxidative stress (EB staining) in these tissues induced by LPS is markedly inhibited by the treatment with dimemorfan [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 10 mg/mL ( 28.30 mM ; ultrasonic and warming and heat to 60°C)
DMSO : 1 mg/mL ( 2.83 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8297 mL | 14.1487 mL | 28.2973 mL |
| 5 mM | 0.5659 mL | 2.8297 mL | 5.6595 mL |
| 10 mM | 0.2830 mL | 1.4149 mL | 2.8297 mL |
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1.
Add each solvent one by one: PBS
Solubility: 16.67 mg/mL (47.17 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
References
- [1] Shin EJ, et al. Dimemorfan prevents seizures induced by the L-type calcium channel activator BAY k-8644 in mice. Behav Brain Res. 2004 May 5;151(1-2):267-76.
- [2] Wang YH, et al. Anti-inflammatory effects of dimemorfan on inflammatory cells and LPS-induced endotoxin shock in mice. Br J Pharmacol. 2008 Jul;154(6):1327-38.
Synonyms