|Targets||5-HT Receptor | Dopamine Receptor|
|Description||Cariprazine is an orally active D2/D3 dopamine receptor antagonist exhibits high selectivity and affinity to dopamine D3(Ki=0.09 nM) and D2 (Ki=0.5 nM) receptors and moderate affinity to serotonin 5-HT(1A) receptors. It is used as an antipsychotic drug candidate for the potential treatment of schizophrenia, bipolar mania and depression. It has also been used as a potential adjunct in treatment-resistant major depressive disorder. It had lower affinity at human and rat hippocampal 5-HT(1A) receptors (pK(i) 8.59 and 8.34, respectively) and demonstrated low intrinsic efficacy.Cariprazine displayed low affinity at human 5-HT(2A) receptors (pK(i) 7.73) in vitro. It could reduce the rewarding effect of cocaine and attenuated relapse to cocaine seeking with half maximal effective dose values of 0.2, 4.2, and 0.17 mg/kg, respectively. It was developed by Gedeon Richter and received FDA approval on September 17, 2015 and is currently owned by Gedeon Richter and Actavis. It is in phase III clinical trials in patients with schizophrenia and in patients with bipolar disorder.|
|B0084-459781||25 mg||$298||In stock|
|Appearance||White to off-white Solid|
|Synonyms||Urea, N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N -diMethyl-;N'-[trans-4-[2-[4-(2,3-Dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea;RGH 188;3-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethylurea;Vraylar|
|Solubility||10 mM in DMSO ; water:1000 mg/ml|
|Application||Cariprazine is used as an antipsychotic drug candidate for the potential treatment of schizophrenia, bipolar mania and depression. It has also been used as a potential adjunct in treatment-resistant major depressive disorder.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Boiling Point||600.1±55.0 °C | Condition: Press: 760 Torr|
|Density||1.24±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
|Current Developer||Cariprazine was developed by Gedeon Richter and received FDA approval on September 17, 2015. It is currently owned by Gedeon Richter and Actavis. It is in phase III clinical trials in patients with schizophrenia and in patients with bipolar disorder.|
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