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Updated: Jul 2, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Competitive inhibition of sodium-dependent high affinity choline uptake by harmala alkaloids
Abstract:
The actions of five harmala alkaloids on the sodium dependent high affinity choline uptake activity in rat striatal synaptosomes was investigated. All five compounds were found to be competitive inhibitors of the uptake system. Harmalol (Ki approximately 3.4 microM) and 2-methylharmine (Ki approximately 5.7 microM) were found to be relatively potent inhibitors in a series with an ascending order of inhibitory potency of harmaline less than 2-methylharmaline less than harmine less than 2-methylharmine less than harmalol.
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