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Anna Herman, Mostafa El Mansari, Nika Adham, Béla Kiss, Bence Farkas, Pierre Blier
Cariprazine, an orally active and potent dopamine D3 -preferring D3 /D2 receptor partial agonist, is approved to treat adults with schizophrenia (in the United States and Europe) and manic or mixed episodes associated with bipolar I disorder (in the United States). Cariprazine also displays partial agonism at serotonin [5-hydroxytryptamine (5-HT)] 5-HT1A receptors and antagonism at 5-HT2A and 5-HT2B receptors in vitro. The study objective was to determine whether cariprazine leads to functional alterations of monoamine systems in vivo via electrophysiological recordings from anesthetized rats...
December 2018: Molecular Pharmacology
Karly P Garnock-Jones
Cariprazine (Vraylar™) is a dopamine D3 -preferring D2 /D3 receptor partial agonist indicated for the treatment of patients with schizophrenia. This narrative review summarizes pharmacological, efficacy and tolerability data relevant to the use of cariprazine in patients with this disorder. In 6-week, phase IIb and III trials in patients with schizophrenia, cariprazine was significantly more efficacious than placebo in improving schizophrenia symptoms, including improvements in Positive and Negative Syndrome Scale (PANSS) total scores...
June 2017: CNS Drugs
(no author information available yet)
No abstract text is available yet for this article.
April 25, 2016: Medical Letter on Drugs and Therapeutics
P De Deurwaerdère
Cariprazine (RGH-188, MP-214, Vraylar[TM]) is a new dopamine receptor ligand developed for the treatment of several neuropsychiatric diseases including schizophrenia and bipolar disorders. Cariprazine displays higher affinity at dopamine D3 receptors and a similar affinity at D2 and 5-HT2B receptors. At variance with some atypical antipsychotics, its affinity at 5-HT1A, 5-HT2A and histamine H1 receptors is modest compared with its three main targets. Cariprazine could correspond to a biased agonist at dopamine receptors, displaying either antagonist or partial agonist properties depending on the signaling pathways linked to D2/D3 receptors...
February 2016: Drugs of Today
Paul L McCormack
Cariprazine (Vraylar) is an oral atypical antipsychotic originated by Gedeon Richter. It is a potent dopamine D3 and D2 receptor partial agonist, which preferentially binds to the D3 receptor. Cariprazine also has partial agonist activity at serotonin 5-HT1A receptors. In September 2015, cariprazine received its first global approval in the USA for the treatment of schizophrenia and for the acute treatment of manic or mixed episodes associated with bipolar I disorder. It is also in development in a variety of countries for the treatment of schizophrenia with predominant negative symptoms (phase III), as adjunctive therapy for major depressive disorder (phase II/III) and for the treatment of bipolar depression (phase II)...
November 2015: Drugs
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