3D Quantitative Structure-Activity Relationship (COMFA) Study of Heterocyclic Arylpiperazine Derivatives with 5-HT_1A Activity

Abstract

Pharmacological treatment of schizophrenia has been traditionally dominated by dopamine D₂ receptor antagonists, known to cause severe extrapyramidal side effects, which can be attributed to the blockade of D₂ receptors in the striatum. Current antipsychotic research focuses on compounds with multireceptorial activity (different dopamine receptor subtypes, serotonine and adrenerg and muscarinic receptors has been sudied). Recent observations indicate, that control of both dopaminergic and serotoninergic systems is important for adequate antipsychotic therapy. It has been reported, that 5-HT_1A receptor agonists reverse antipsychotic induced catalepsy.