Rivastigmine tartrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种乙酰胆碱酯酶抑制剂，可抑制丁酰胆碱酯酶和乙酰胆碱酯酶。

An acetylcholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase; a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.Alzheimer's Disease Approved(In Vitro):Rivastigmine tartrate (ENA 713; 1 μM; 24 hours) reduces LPS (2.5 μg/ml)-induced TNF-α and IL-6 by 50% and 46% combined with carbachol (10 μM), respectively and does not cause any significant reduction in pro-inflammatory cytokines .Rivastigmine tartrate (1 μM), carbachol (10 μM), 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.

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

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. Animal Model:Male Wistar albino rats weighing 190–240 g (90 days old)Dosage:0.5, 1, 1.5 and 2.5 mg/kg Administration:IP; single dose Result:Significantly and dose-dependently improved the behavioral impairments caused by Aluminum (100 mg/kg/day; i.p.; for 60 days)

ENA-713 | SDZ ENA-713

Metabolic Enzyme/Protease

AChE

AChR

Neurological Disease

Alzheimer Disease

129101-54-8

400.4235

C18H28N2O8

>98% (HPLC)

10 mM in DMSO

CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O

Carbamic acid, N-ethyl-N-methyl-, 3-[(1S)-1-(dimethylamino)ethyl]phenyl ester, (2R,3R)-2,3-dihydroxybutanedioate (1:1)

(-20℃)

With Ice Pack

≥ 2 years