多巴胺受体部分激动剂阿立哌唑药理作用与临床应用

阿立哌唑是一种多巴胺D2受体部分激动剂,对5-HT1A受体具有部分激动活性和5-HT2A受体阻滞活性.它可以改善精神分裂症阳性症状,而不引起运动障碍和催乳素增高,很少引起锥体外系反应.初步临床研究表明,阿立哌唑对精神分裂症有效,安全、耐受良好.

Pharmacological and clinical researches of aripiprazole, a dopamine partial agonists

Aripiprazole,a new type of atypical antipsychotics, works through a combination of partial agonist activity at dopamine D_2 receptors and serotonin 5HT_(1A) receptors, and antagonist activity at serotonin 5HT_(2A) receptors. The dopamine D_2 partial agonist is expected to reduce the positive symptoms of schizophrenia without producing movement disorders or elevated prolactin levels. Antagonist activity at 5HT_(2a) receptors is thought to be associated with a low liability for EPS and beneficial effects on the negative symptoms of schizophrenia. Preliminary clinical trials have shown that aripiprazole is effective, safe, and well tolerated for the improvement of positive and negative symptoms of schizophrenia.