Tolserine
AChE inhibitor derived from Phenserine
From Wikipedia, the free encyclopedia
Tolserine (2-methylphenserine) is an inhibitor of acetylcholinesterase. It has been described as of potential interest for the treatment of myasthenia gravis (MG)[1] and Alzheimer's disease.[2]
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| Names | |
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| IUPAC name
[(3aR,8bS)-3,4,8b-Trimethyl-2,3a-dihydro-1H-pyrrolo[2,3-b]indol-7-yl] N-(2-methylphenyl)carbamate | |
| Other names
2-Methylphenserine | |
| Identifiers | |
3D model (JSmol) |
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| Properties | |
| C21H25N3O2 | |
| Molar mass | 351.450 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Chemistry
Tolserine is a substituted derivative of phenserine.[3] Additionally, certain analogs of tolserine possess less selectivity between different cholinesterase enzymes.[4]
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.[5]