Efficacy of cariprazine across symptom domains in patients with acute exacerbation of schizophrenia: Pooled analyses from 3 phase II/III studies was written by Marder, Stephen;Fleischhacker, W. Wolfgang;Earley, Willie;Lu, Kaifeng;Zhong, Yan;Nemeth, Gyorgy;Laszlovszky, Istvan;Szalai, Erzsebet;Durgam, Suresh. And the article was included in European Neuropsychopharmacology in 2019.Synthetic Route of C21H32Cl2N4O This article mentions the following:
Schizophrenia affects various symptom domains, including pos. and neg. symptoms, mood, and cognition. Cariprazine, a dopamine D3/D2 receptor partial agonist and serotonin 5-HT1A receptor partial agonist, with preferential binding to D3 receptors, is approved for the treatment of adult patients with schizophrenia and mania associated with bipolar I disorder. Post hoc analyses evaluated mean change from baseline to week 6 in PANSS-derived symptom factors (pos. symptoms, neg. symptoms, disorganized thought, uncontrolled hostility/excitement, anxiety/depression) and PANSS single items for cariprazine vs. placebo. P values were not adjusted for multiple comparisons. At week 6, statistically significant differences vs. placebo were seen for cariprazine on all 5 PANSS factors (P < 0.01 all). Effects sizes ranged from 0.21 (anxiety/depression) to 0.47 (disorganized thought). Dose-response anal. from the fixed-dose studies found significant differences for all cariprazine doses (1.5, 3.0, 4.5, and 6.0 mg/d) vs. placebo in PANSS total score, and in neg. symptom and disorganized thought factor scores (P < 0.001). Differences between cariprazine and placebo were also statistically significant on 26 of 30 PANSS single items (P < 0.05). In these post hoc analyses, cariprazine was effective vs. placebo in improving all 5 PANSS factor domains, suggesting that it may have broad-spectrum efficacy in patients with acute schizophrenia. In the experiment, the researchers used many compounds, for example, 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8Synthetic Route of C21H32Cl2N4O).
3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Synthetic Route of C21H32Cl2N4O
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics