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AAT Bioquest

What are the inhibitors of acetylcholinesterase?

Posted January 16, 2024


Answer

There are various kinds of acetylcholinesterase inhibitors. 

Organophosphates, commonly used as pesticides, act as inhibitors of acetylcholinesterase. Their widespread usage has led to significant exposure and toxicity concerns, making them one of the primary causes of poisoning worldwide. Exposure to organophosphates can occur through accidental contact, agricultural activities, or intentional exposure in cases of self-harm. 

In the symptomatic treatment of Alzheimer's disease, three ChE inhibitors are commonly prescribed: donepezil, tacrine, galantamine, and rivastigmine. Donepezil, tacrine and galantamine are AChE-selective inhibitors, and rivastigmine is a butyrylcholinesterase inhibitor. AChE inhibitors are useful in treating Alzheimer's disease due to their effective ability to penetrate the blood-brain barrier. 

Carbamate acetylcholinesterase inhibitors such as neostigmine or pyridostigmine, which have charged quaternary structures at physiological pH, are unable to pass through the blood-brain barrier.

Additional resources

What are cholinesterase inhibitors?

Enzymes

Acetylcholinesterase Inhibitors (IC50, Ki)

Amplite® Colorimetric Acetylcholinesterase Assay Kit