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Updated: Jun 23, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
Published on: February 11, 2019
Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition
Jeroen C Verheijen1, Kjesten A Wiig, Shoucheng Du
1Sention Inc., 1 Richmond Square, Providence, RI 02906, USA. verheij@wyeth.com
Abstract:
Conjugation of the phenol derived from rivastigmine with amphetamines gave access to novel carbamate cholinesterase inhibitors. All compounds possessed increased affinity and selectivity for AChE compared to rivastigmine and were orally bioavailable. Compound 4a, incorporating d-amphetamine, caused significant inhibition of cholinesterase in vivo at doses that were well tolerated. Release of amphetamine from 4a was demonstrated following in vitro and in vivo inhibition of cholinesterase. Compound 4a was also effective in alleviating scopolamine induced amnesia in a rat passive avoidance model.
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