Interaction of antipsychotic drugs with sucrase; kinetics and structural study.

In this study, the interaction between trifluoperazine and haloperidol as antipsychotic drugs on oral drug yeast sucrase was investigated. The results showed that both drugs could reduce sucrase activity and decrease the Vmax of the enzyme by non-competitive inhibition. The IC50 and Ki values of the drugs were determined to be 0.7 and 0.068 mM and 0.45 and 0.063 mM for haloperidol and trifluoperazine, respectively. The results suggested that trifluoperazine binds to the enzyme with higher affinity than haloperidol. Fluorescence measurement was used for conformational investigations of the drugs and sucrase interaction. It was shown that the drugs bind to free enzyme and enzyme-substrate complex which are accompanied with hyperchromicity. This suggests that tryptophan residues of the enzyme transferred to hydrophobic medium after binding of the drugs to the enzyme. The conformational changes due to binding of trifluoperazine to the enzyme were different from that of haloperidol. PMID: 28103775 [PubMed - as supplied by publisher]
Source: Current Clinical Pharmacology - Category: Drugs & Pharmacology Authors: Tags: Curr Clin Pharmacol Source Type: research