title: Antipsychotic agents screened as human carbonic anhydrase I and II inhibitors.
abstract: The antipsychotic drugs currently used to treat schizophrenia can be divided into two distinct classes, typical and atypical antipsychotics. Many drug molecules are enzyme inhibitors that bind reversibly or irreversibly to their target through intermolecular interactions. That's why enzyme inhibition studies are an important issue for drug design and biochemical applications. In this study, in vitro inhibition effect of some antipsychotic drugs on the purified carbonic anhydrase (CA) I and II isoenzymes were investigated by using CO2 as a substrate. CA I and II were purified from human erythrocytes by a simple one step procedure using Sepharose 4B-L-tyrosine-sulfonamide affinity column. The results showed that all the drugs inhibited the cytosolic carbonic anhydrases enzyme activity in a concentration-dependent fashion. Among the studied drugs, aripiprazole and pramipexole were found to be the most active one for hCA I (IC50: 3.64 and 5.37 μM) and hCA II (IC50: 4.16 and 4.81 μM) activity, respectively.
authors.affiliation: Department of Chemistry, Faculty of Science and Art, Aksaray University , 68100, Aksaray , Turkey and.
authors.forename: Mahmut
authors.initials: M
authors.lastname: Erzengin
authors.forename: Cigdem
authors.initials: C
authors.lastname: Bilen
authors.forename: Adem
authors.initials: A
authors.lastname: Ergun
authors.forename: Nahit
authors.initials: N
authors.lastname: Gencer
mesh_terms: D014150:Antipsychotic Agents / Q000737:chemistry / Q000494:pharmacology*; D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors*; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors*; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D003600:Cytosol / Q000201:enzymology; D004353:Drug Evaluation, Preclinical; D004912:Erythrocytes / Q000166:cytology; D006801:Humans
chemical_list: D014150:Antipsychotic Agents; D002257:Carbonic Anhydrase Inhibitors; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II