ERB-196

ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Neurological Disease

Research Areas >> Inflammation/Immunology

ERβ[1]

ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist. ERB-196 significantly reduces histopathologic evidence of injury to the gastrointestinal mucosal surface (0.7±0.1 vs. 2.3±0.2 for control; p<0.05). The mucosal mass of 10-cm segments of small bowel mucosa shows better preservation of mucosal mass than control treatment (63±20 [ERB-196] vs. 31±24 [control]), but this difference fails to reach statistical significance (p<0.06). The administration of ERB-196 is highly effective in the prevention of lethality. Consistent with the neutropenic rat model, ERB-196 significantly increases survival when compare with vehicle control[1].

The neutropenic rat model of pseudomonas sepsis are used in this study. For the survival study, ERB-196 (50 mg/kg; n=12) or vehicle control (n=8) is administered daily by orogastric feeding beginning on day 4 after the first dose of cyclophosphamide and continuing for 8 days. Animals are assessed clinically and pathologically by measuring daily body weight, body temperature, presence of bacteremia, circulating endotoxin levels, and pathologic evidence of damage to the gastrointestinal epithelium and liver by light microscopy and electron microscopy. Blood and tissue samples are serially diluted in sterile saline and incubated at 37°C on pseudomonas agar for quantitative assessment of bacterial concentrations[1].

[1]. Cristofaro PA, et al. WAY-202196, a selective estrogen receptor-beta agonist, protects against death in experimental septic shock. Crit Care Med. 2006 Aug;34(8):2188-93.

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