de Paulis Tomas
IDrugs. 2007 Mar;10(3):193-201.
Vilazodone is a combined selective serotonin reuptake inhibitor (SSRI) and a 5-HT(1A) receptor partial agonist that is being developed by Clinical Data Inc for the treatment of depression. In preclinical studies, vilazodone compared favorably to other antidepressants such as paroxetine and fluoxetine. Orally administered vilazodone inhibited ultrasonic vocalization in the rat after electrical foot shock (a model of anxiolytic activity). Yet, in the forced swimming test model of depression in rats, vilazodone administered intraperitoneally was active at 1 mg/kg but not at 3 or 10 mg/kg. During clinical trials, vilazodone completely abolished REM sleep for 8 h and demonstrated antidepressant efficacy that was equal to that of current antidepressant therapeutics. The author concludes that the success of vilazodone as an effective antidepressant agent will depend on whether the drug can produce a more rapid antidepressant effect than other SSRI agents, or if specific genetic markers of patients can be associated with clinical efficacy.
维拉唑酮是一种兼具选择性5-羟色胺再摄取抑制剂（SSRI）和5-HT(1A)受体部分激动剂特性的药物，正由临床数据公司研发用于治疗抑郁症。在临床前研究中，维拉唑酮与其他抗抑郁药如帕罗西汀和氟西汀相比具有优势。口服维拉唑酮可抑制大鼠在电击足部后发出的超声波鸣叫（一种抗焦虑活性模型）。然而，在大鼠抑郁症的强迫游泳试验模型中，腹腔注射维拉唑酮在1mg/kg时有活性，但在3mg/kg或10mg/kg时无活性。在临床试验期间，维拉唑酮使快速眼动睡眠完全消失达8小时，并显示出与当前抗抑郁治疗药物相当的抗抑郁疗效。作者得出结论，维拉唑酮作为一种有效抗抑郁药的成功与否将取决于该药物是否能比其他SSRI药物产生更快的抗抑郁效果，或者患者的特定基因标记是否能与临床疗效相关联。
