Atypical Antipsychotics: Modelling and QSAR

Abstract

Antipsychotic drugs may be defined as medications that alleviate delusions, hallucinations and some aspects of formal thought disorder that occur in a variety of illnesses, most notably schizophrenia. The mechanism of action of these drugs has focused on their interaction with the central nervous system (CNS) neurotransmitter dopamine (DA). However, recent studies strongly implicate the neurotransmitter serotonin (5HT) as a further target of action. Antipsychotic drugs are further loosely classified into typical or atypical, initially based on animal model tests. A set of ligands ((R)- and (S)-octoclothepin, clozapine, Org5222, seroquel, olanzapine, sertindole, risperidone, ziprasidone, zotepine, remoxipride, loxapine) with high affinity for D2 and 5HT2A and classified as atypical and typical antipsychotics were selected for pharmacophore mapping. Further studies were carried out on sertindole, risperidone, zotepine, ziprasidone and haloperidol once a pharmacophore model has been established. [on SciFinder (R)]