Rivastigmine

SKU: orb1226711

Description

An acetylcholinesterase (AChE) 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 (S-Rivastigmine; 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 (1 μM), carbachol (10 μM), or a combination of both drugs, does not have a cytotoxic effect on activated cells.(In Vivo):Rivastigmine (S-Rivastigmine; 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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 123441-03-2
• MW: 250.3367
• Purity: >98% (HPLC)
• Formula: C₁₄H₂₂N₂O₂
• SMILES: CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C
• Target: AChE
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Rivastigmine (S-Rivastigmine; 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).
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• In Vitro:
  Rivastigmine (S-Rivastigmine; 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 (1 μM), carbachol (10 μM), or a combination of both drugs, does not have a cytotoxic effect on activated cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

S-Rivastigmine

Quick Database Links

Gene Symbol

AChE