Schizophrenia is a devastating psychiatric illness that affects 1-2% of the world population and continues as a challenge to neuroscience. In this work, we describe an account about the historical evolution of the dopaminergic hypothesis of schizophrenia discussing, from the medicinal chemistry point of view all different classes of antipsychotic drugs, emphasizing the rational design, structure activity relationships (SAR) and physico-chemical properties related with its molecular mechanism of action.

The concepts of stereochemistry and chirality are introduced, and the ability to distinguish among the different receptors caused by one stereoselective action against chiral drugs is presented. The importance of the behaviour of chiral drugs is emphasized.