SR-31747
Names
Biological Activity
[Description]:
SR-31747 is a new sigma ligand with immunosuppressive properties.
[Related Catalog]:
[In Vitro]
SR-31747 is capable of inhibiting T-cell proliferation when added as late as 24 h after activation. SR-31747 arrests proliferation in yeast cells in a dose-dependent manner[2].
[In Vivo]
SR 31747 dramatically blocks lipopolysaccharide-induced production of interleukin (IL)-1, IL-6 and tumor necrosis factor-alpha in a dose-dependent manner (ED50 2 mg/kg)[1].
[Animal admin]
IL-1, IL-6 and TNF-a are induced by i.p. injection of LPS into BALBIc mice. SR 31747 or reference substances are administered i.p. at the indicated doses together with LPS (0.5 mg/kg). Control animals are treated with LPS and vehicle. Blood samples are collected from the retro-orbital sinus 1 hr or 4 hr after LPS injection for the determination of TNF-α, IL-1 and IL-6. Plasma is prepared and stored frozen until experiments. The IL-1 plasma level is determined by a competitive radioreceptor assay with the use of the murine NOBEL4 cell line and [125I]-IL-1. The IL-6 assay is conducted with the B9 murine IL-6-dependent cell line. The TNF-a plasma level is evaluated by the cytolytic assay with the dactinomycin-treated LM6 cell line, derived from the murine fibroblastic L929 cell line. Each determination is performed on a pool of three different plasma samples. None of the molecules administered affect these assays even at the highest dose (10-5 M), which thereby rules out the possibility of any direct effect caused by the presence ofdrugs in treated-animal sera. In the various tests, one unit is defined as the amount of cytokines able to induce 50% of the maximal effect.
[References]
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Chemical & Physical Properties
[ Molecular Formula ]:
C23H34ClN
[ Molecular Weight ]:
359.97600
[ Exact Mass ]:
359.23800
[ PSA ]:
3.24000
[ LogP ]:
7.05550