Product Introduction
Bioactivity


英文名: Dimemorfan phosphate

描述: Dimemorfan phosphate (3,17-dimethylmorphinan) 是 sigma 1 受体激动剂，用作强效镇咳药。

体外活性: 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 10 mM
DMSO : Insoluble


关键字: Dimemorfan Phosphate | inhibit | Inhibitor | Sigma Receptor | Dimemorfan phosphate | Dimemorfan

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相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Approved Drug Library | NO PAINS Compound Library | Bioactive Compound Library