THE INVESTIGATION OF THE INTERACTION OF SEVERAL ANTIPSYCHOTIC DRUGS WITH HUMAN CHOLINESTERASE ENZYMES

Abstract

Phenothiazines and butyrophenones are one of the important antipsychotic group of drugs. They have been utilized for many years for treatment of schizophrenia and other psychotic disorders. They are the main constituents of the first generation, also referred as typical, antipsychotic drugs. They are known for their potential to antagonize dopamine D2 receptors. With respect to their structures, they are able to cross the blood brain barrier and interact with various types of receptors. In order to investigate their potential to interact with cholinesterase enzymes, within this research, we have designed a series of experiments. Although, earlier studies have shown that some of those compounds have the potential to inhibit cholinesterase enzyme, for the first time, we have evaluated their potential to inhibit human isoforms of acetylcholinesterase and butyrylcholinesterase. The results strongly pointed out that phenothiazines are selective and potent inhibitors of the human butyrylcholinesterase enzyme.