Dimemorfan phosphate |
| رقم الكتالوجGC30956 |
ديميمورفان فوسفات هو ناهض مستقبلات سيجما 1 ، يستخدم كمضاد للسعال قوي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 36304-84-4
Sample solution is provided at 25 µL, 10mM.
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Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
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, 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].
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].
[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.
Animal experiment: | C57BL/6 mice receive each morphinan (dextromethorphan, dextrorphan or dimemorfan) compound (20 or 40 mg/kg, i.p. per day) or PCP (2.5 or 5 mg/kg, i.p. per day) once a day for 7 days. Ten minutes after the last treatment with each drug, locomotor activity is measured for 30 min using an automated video-tracking system. Eight test boxes (40 cm×40 cm×30 cm high) are operated simultaneously by an IBM computer. Animals are studied individually during locomotion in each test box, where they are adapted for 10 min before starting the experiment. A printout for each session showed the pattern of the ambulatory movements of the test box. The distance traveled in cm by the animals in horizontal locomotor activity is analyzed. Data are collected and analyzed between 09:00 and 17:00 h. |
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. | |
| Cas No. | 36304-84-4 | SDF | |
| Canonical SMILES | O=P(O)(O)O.CN1[C@](CC2=CC=C(C)C=C32)([H])[C@](CCCC4)([H])[C@]34CC1 | ||
| Formula | C18H28NO4P | M.Wt | 353.39 |
| الذوبان | Water : 20 mg/mL (56.59 mM);DMSO : 1 mg/mL (2.83 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 | 0.283 mL | 1.4149 mL | 2.8297 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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