中文名稱:阿立哌唑 | 英文名稱:Aripiprazol |
CAS:129722-12-9 | 有效期: 一年 |
Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
IC50 Value: 4.2 nM(Ki)
Target: 5-HT Receptor
Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.
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[2]. Burris KD, Molski TF, Xu C et al. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther. 2002 Jul;302(1):381-9.
[3]. Swainston Harrison T, Perry CM. Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36.
[4]. Nagasaka Y, Oda K, Iwatsubo T, Kawamura A, Usui T. Nagasaka Y, Oda K, Iwatsubo T, Kawamura A, Usui T. Effects of aripiprazole and its active metabolite dehydroaripiprazole on the activities of drug efflux transporters expressed both in the intestine and at the blood-brain barrier. Biopharm Drug Dispos. 2012 Jul 27. doi: 10.1002/bdd.1801.
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