Abstract
The stereoselectivities and mechanisms of the inhibition of rat cortical acetylcholinesterase by the enantiomers of huperzine A were determined. (-)-Huperzine A was the more potent enantiomer with a Ki value of 8 nM. (+)-Huperzine A inhibited the enzyme 38-fold less potently with a Ki value of 300 nM. Racemic huperzine A was about two-fold less potent than the more active isomer, (-)-huperzine A. The mechanism of inhibition of acetylcholinesterase for all three drugs was of the mixed linear competitive type.
Original language | English (US) |
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Pages (from-to) | 303-305 |
Number of pages | 3 |
Journal | European Journal of Pharmacology |
Volume | 203 |
Issue number | 2 |
DOIs | |
State | Published - Oct 15 1991 |
Keywords
- (Natural products)
- Acetylcholine
- Alzheimer's disease
- Cerebral cortex
- Cholinomimetics
- Stereochemistry
ASJC Scopus subject areas
- Pharmacology