Antipsychotic medications are the primary pharmacologic treatment for schizophrenia and were initially discovered fortuitously in the early 1950s. Chlorpromazine was the prototype of this class of medications, retroactively noted as first-generation antipsychotics, which are primarily characterized by their high-affinity antagonism at the dopamine D₂ receptor. The rediscovery of clozapine in 1989 heralded the initial era of second-generation antipsychotics, which extended through 2002. In general, second-generation antipsychotics have lower D₂ affinity, along with high serotonin 5-HT_2A antagonist affinity. Subsequently, several new second-generation drugs were introduced: asenapine and iloperidone in 2009, lurasidone hydrochloride in 2010, and cariprazine and brexpiprazole in 2015.

抗精神病药是精神分裂症的主要药物治疗，最初是在1950年代初偶然发现的。氯丙嗪是这类药物的原型，可追溯地称为第一代抗精神病药，其主要特征是对多巴胺D ₂受体具有高亲和力。1989年氯氮平的重新发现预示了第二代抗精神病药的最初时代，该时代一直延续到2002年。总的来说，第二代抗精神病药的D ₂亲和力较低，而血清素5-HT _2A较高拮抗剂亲和力。随后，又推出了几种第二代新药：2009年的阿塞那平和伊潘立酮，2010年的盐酸拉拉西酮，2015年的卡立哌嗪和布雷普拉唑。