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Rivastigmine tartrate

CAS No. : 129101-54-8

MCE 站：Rivastigmine tartrate

产品活性：Rivastigmine tartrate (ENA 713; SDZ-ENA 713) 是一种具有口服活性的，有效的胆碱酯酶 (ChE) 抑制剂，可抑制丁酰胆碱酯酶 (BChE) 和乙酰胆碱酯酶 (AChE)，IC₅₀ 分别为 0.037 μM 和 4.15 μM。Rivastigmine tartrate 可透过血脑屏障 (BBB)。Rivastigmine tartrate 是一种拟副交感神经剂或胆碱能剂，用于研究轻度至中度阿尔茨海默氏型痴呆和帕金森氏病引起的痴呆。

研究领域：Neuronal Signaling

作用靶点：AChE

In Vitro: Rivastigmine tartrate (ENA 713; 1 ?M; 24 hours) reduces LPS (2.5 ?g/ml)-induced TNF-α and IL-6 by 50% and 46% combined with carbachol (10 ?M), respectively and does not cause any significant reduction in pro-inflammatory cytokines .
Rivastigmine tartrate (1 ?M), carbachol (10 ?M), or a combination of both drugs, does not have a cytotoxic effect on activated cells.

In Vivo: Rivastigmine tartrate (ENA 713; 0.5-2.5 mg/kg; IP; 60 min before the tests) significantly and dose-dependently improved the behavioral impairments caused by Aluminum (HY-B1521).
Rivastigmine (0.5, 1 mg/kg/day; s.c; for 8 days) reduces by about 50% and 60% respectively, the concentration of IL-6 but not those of TNF-α and IL-1β in BALB/c OlaHsd male mice aged 8-9 weeks weighing 200–250 g with acute colitis.
Rivastigmine (1 mg/kg), but not (0.5 mg/kg), partially antagonized colon shrinkage and completely prevented bleeding. Treatment with rivastigmine (0.5 mg/kg) causes little change in these pathological manifestations, but rivastigmine (1 mg/kg) causes a partial restoration of the structure of the crypts and a reduction in sub-mucosal edema and cell infiltration. Rivastigmine (1 mg/kg) causes a 4.7% reduction in body weight at the end of the experiment.

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