Rivastigmine

Synonyms: SDZ-ENA 713, Exelon

Rivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).

Rivastigmine Chemical Structure

Rivastigmine Chemical Structure

CAS No. 123441-03-2

Purity & Quality Control

Rivastigmine Related Products

Signaling Pathway

Biological Activity

Description Rivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).
Targets
cholinesterase [1]
In Vivo
In vivo Preclinical biochemical studies indicates that rivastigmine has central nervous system selectivity over peripheral inhibition. It ameliorates memory impairment in rats with forebrain lesions. The drug is rapidly absorbed orally, with a bioavailability of 0.355 and low protein binding (40%). Its elimination halflife is less than 2 hours, and it is converted to an inactive metabolite at the site of action, bypassing hepatic metabolic pathways. Its disposition essentially is unaltered in patients with renal or hepatic impairment. It also has dosedependent effects on AChE inhibition[1].
Animal Research Animal Models Male Wistar albino rats
Dosages 0.5, 1, 1.5 and 2.5 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05768126 Recruiting
Depressive Disorder
UMC Utrecht|ZonMw: The Netherlands Organisation for Health Research and Development|St. Antonius Hospital|Tergooi Hospital
September 29 2021 Phase 4
NCT01585272 Completed
Alzheimer''s Dementia
Novartis Pharmaceuticals|Novartis
August 2012 Phase 4
NCT01073319 Completed
Methamphetamine Dependence|Substance Abuse|Methamphetamine Abuse
Baylor College of Medicine|National Institute on Drug Abuse (NIDA)
July 2009 Phase 1
NCT01312363 Completed
Alzheimer''s Disease
Seoul National University Hospital|Seoul National University Bundang Hospital|Seoul St. Mary''s Hospital|Korea University|Bobath Memorial Hospital|Chung-Ang University Hosptial Chung-Ang University College of Medicine|Hanyang University|Kwandong University Myongji Hospital|Inha University Hospital|SungAe General Hospital|Ewha Womans University|Inje University|Hanyang University Seoul Hospital|Kyunghee University Medical Center|Hallym University Medical Center|Pusan National University Hospital|Konyang University Hospital|Wonkwang University Sanbon Medical Center|Yong-in Hyoja Geriatric Hospital|Jeju National University|Dong-A University Hospital
June 2009 --
NCT00624663 Completed
Rivastigmine Toxicity
Tel-Aviv Sourasky Medical Center|Medical Corps Israel Defense Force
January 2009 Not Applicable

Chemical Information & Solubility

Molecular Weight 250.34 Formula

C14H22N2O2

CAS No. 123441-03-2 SDF Download Rivastigmine SDF
Density 1.038 g/mL
Smiles CCN(C)C(=O)OC1=CC=CC(=C1)C(C)N(C)C
Storage (From the date of receipt) 2 years -80°C liquid

In vitro
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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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