Rivastigmine (tartrate)

Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyryl ChE (BChE) and acetyl ChE (AChE, IC50s = 0.037 and 4.15 µM, respectively). It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-beta (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 µM.. In a rat model of Alzheimer's disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1beta, and beta-secretase 1 (BACE1) mRNA expression in the cerebral cortex. It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer's disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress. Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer's disease and Parkinson's disease.Formal Name: N-ethyl-N-methyl-carbamic acid, 3-[(1S)-1-(dimethylamino)ethyl]phenyl ester, 2R,3R-dihydroxybutanedioate. CAS Number: 129101-54-8. Synonyms: Exelon, SDZ-ENA 713. Molecular Formula: C14H22N2O2 . C4H6O6. Formula Weight: 400.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 16 mg/ml, Ethanol: 16 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: CCN(C)C(OC1=CC([C@H](C)N(C)C)=CC=C1)=O.OC(C(O)=O)C(O)C(O)=O. InChi Code: InChI=1S/C14H22N2O2.C4H6O6/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4,5-1(3(7)8)2(6)4(9)10/h7-11H,6H2,1-5H3,1-2,5-6H,(H,7,8)(H,9,10)/t11-,/m0./s1. InChi Key: GWHQHAUAXRMMOT-MERQFXBCSA-N.