Wood Martyn, Reavill Charlie
GlaxoSmithKline, Schizophrenia and Bipolar Neurophysiology and Pharmacology, Psychiatry CEDD, Harlow, Essex, UK.
Expert Opin Investig Drugs. 2007 Jun;16(6):771-5. doi: 10.1517/13543784.16.6.771.
Aripiprazole has made a significant contribution to the treatment of schizophrenia and related disorders with an improved safety and tolerability profile, which has been attributed to its unique pharmacological profile. It has been claimed that partial agonism of the dopamine D(2) and 5-HT(1A) receptors and antagonism of the 5-HT(2) receptor contribute to the clinical profile of aripiprazole, a so-called dopamine- and 5-HT stabiliser. However, recent studies have questioned the role of the 5-HT-mediated systems in the mechanism of action of aripiprazole. This report reviews published and unpublished data that suggest that aripiprazole acts as a selective partial agonist at the dopamine D(2) receptor and does not affect 5-HT receptors at therapeutic doses.
阿立哌唑对精神分裂症及相关障碍的治疗做出了重大贡献，其安全性和耐受性有所改善，这归因于其独特的药理学特性。据称，多巴胺D(2)和5-羟色胺(5-HT)(1A)受体的部分激动作用以及5-HT(2)受体的拮抗作用促成了阿立哌唑的临床特性，即所谓的多巴胺和5-HT稳定剂。然而，最近的研究对5-HT介导系统在阿立哌唑作用机制中的作用提出了质疑。本报告回顾了已发表和未发表的数据，这些数据表明阿立哌唑在多巴胺D(2)受体上作为选择性部分激动剂起作用，且在治疗剂量下不影响5-HT受体。
