Latest research on Aripiprazole

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.

Aripiprazole indications

Side effects of Aripiprazole included significant increase in mean body weight, body mass index, and waist circumference. [source, 2016]
The most common adverse effects attributed to Aripiprazole were nausea/vomiting (5.5%), drowsiness (3.9%), headache (3.5%), and dizziness (3.5%). [source, 2016]
To investigate the effects of cariprazine on D3R/D2R-related signaling, we compared its activity with that of Haloperidol (a typical antipsychotic) and Aripiprazole (a Dopamine D2 partial agonist atypical antipsychotic) in two in vitro assays: a G protein-mediated cAMP inhibition assay and an assay to measure the interaction between the D2R and β-arrestin 2. [source, 2015]
To compare the effects of cariprazine with that of other atypical and typical antipsychotics, we assayed the effects of cariprazine, Aripiprazole, and Haloperidol in cell culture on G protein-mediated cAMP production and β-arrestin 2 recruitment. [source, 2015]
Cariprazine was over sixfold more potent (EC50 = 1.4 nmol/L) than Aripiprazole (EC50 = 9.2 nmol/L) in inhibiting isoproterenol-induced cAMP production in HEK-293 cells; however, both compounds displayed similar maximum effect (∼75% of efficacy, in comparison with the full D2R agonist quinpirole) (Fig.1A; Table1). [source, 2015]
When tested for their ability to antagonize the effect of quinpirole in this assay, all three agents inhibited the ability of quinpirole to promote interactions between D2R and β-arrestin 2; cariprazine (KB = 1.6 nmol/L) was as potent as the classical D2R antagonist Haloperidol (KB = 1.3 nmol/L) and more potent than Aripiprazole (KB = 8.7 nmol/L) (Table1). [source, 2015]
Study inclusion criteria: All the randomized controlled clinical trials that investigated the effect of Aripiprazole on irritability in pervasive developmental disorders were included. [source, 2015]
These studies had not examined the effect of Aripiprazole on irritability in autism. [source, 2015]
One study reported anti-manic effect of Aripiprazole in patients with autism spectrum disorder and bipolar disorder66. [source, 2015]
Another reported lack of any significant effect of Aripiprazole on electrocardiographic data in paediatric patients9. [source, 2015]