Tolserine (2-methylphenserine) is an inhibitor of acetylcholinesterase. It has been described as of potential interest for the treatment of myasthenia gravis (MG) and Alzheimer's disease.
Chemistry Tolserine is a substituted derivative of phenserine. Additionally, certain analogs of tolserine possess less selectivity between different cholinesterase enzymes.
Biological activity As an inhibitor of the AChE enzyme, tolserine slows the breakdown of acetylcholine, a neurotransmitter. Tests have described tolserine as having an average IC50 value of 8.13 nM and an estimated Ki of 4.69 nM, which represents a more potent inhibition than its parent compound phenserine.
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