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Dimemorfan phosphate

Catalog No. T5027   CAS 36304-84-4
Synonyms: 3,17-dimethylmorphinan

Dimemorfan phosphate (3,17-dimethylmorphinan) is a sigma 1 receptor agonist. Dimemorfan phosphate is used as a potent antitussive.

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Dimemorfan phosphate Chemical Structure
Dimemorfan phosphate, CAS 36304-84-4
Pack Size Availability Price/USD Quantity
50 mg In stock $ 39.00
100 mg In stock $ 59.00
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Purity: 99.67%
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Biological Description
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Storage & Solubility Information
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

Storage

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

Solubility Information

H2O: 10 mM

DMSO: Insoluble

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Immunology/Inflammation Compound Library Anti-Cancer Compound Library GPCR Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Bioactive Compound Library Drug Repurposing Compound Library ReFRAME Related Library

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Keywords

Dimemorfan phosphate 36304-84-4 GPCR/G Protein Sigma receptor Dimemorfan Phosphate inhibit Inhibitor 3,17-dimethylmorphinan Sigma Receptor Dimemorfan inhibitor

 

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