|3-(trans-4-(2-(4-(2,3-二氯苯基)哌嗪-1-基)乙基)环己基)-1,1-二甲基脲|CsnPharm

CAS No.: 839712-12-8

Cariprazine/卡利拉嗪 Catalog No. CSN16030

Synonyms: RGH-188;MP-214;卡利拉嗪

Cariprazine exhibits high selectivity and affinity to dopamine D3 receptor (Ki=0.09 nM) and lower binding activity to dopamine D2 receptor and 5-HT(1A) with Ki of 0.5 nM and 2.6 nM repectively. It has been used as antipsychotics in the treatment of schizophrenia and bipolar disorder.

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靶点选择性

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技术信息

生物活性

靶点 Dopamine Receptor D3

Ki:0.09nM Dopamine Receptor D2

Ki:0.5nM 5-HT Receptor 1A

Ki:2.6nM
描述Cariprazine is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D(3) and D(2) receptors and moderate affinity to serotonin 5-HT(1A) receptors. Cariprazine occupied D(2)/D(3) receptors in a dose-dependent and saturable manner, with the lowest dose occupying ~5% of receptors and the highest dose showing more than 90% occupancy^[3]. Cariprazine demonstrated approximately 10-fold higher affinity for human D(3) versus human D(2L) and human D(2S) receptors (pKi 10.07, 9.16, and 9.31, respectively). Cariprazine 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). Moderate or low affinity for histamine H(1) and 5-HT(2C) receptors (pK(i) 7.63 and 6.87, respectively) suggest cariprazine's reduced propensity for adverse events is related to these receptors^[4]. Cariprazine pretreatment significantly attenuated the emergence of these cognitive deficits in PCP-treated (phencyclidine) wild-type mice, but not in PCP-treated D(3)-receptor knockout mice^[5]. Cariprazine was generally well tolerated in clinical trials, with most adverse events being of mild to moderate severity, and metabolic changes observed were considered generally not clinically significant. Cariprazine is a useful addition to the treatment options for schizophrenia, and may be of particular use in patients with predominantly negative symptoms^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00862992	Schizophrenia	Phase 2	Completed	-	Japan ... more >> Hoyu Hospital Kure-City, Hiroshima-ken, Japan Collapse <<
NCT00854100	Major Depressive Disorder	Phase 2	Completed	-	-
NCT00404573	Schizophrenia	Phase 2	Completed	-	United States, Missouri ... more >> For information regarding investigative sites, contact Forest Professional Affairs St Louis, Missouri, United States, 63045 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3397 mL
- 11.6983 mL
- 23.3967 mL
- 5 mM
- 0.4679 mL
- 2.3397 mL
- 4.6793 mL
- 10 mM
- 0.2340 mL
- 1.1698 mL
- 2.3397 mL

技术信息

CAS号	839712-12-8	储存条件	粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C21H32Cl2N4O	运输	蓝冰
分子量	427.41	别名	RGH-188;MP-214;卡利拉嗪

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00862992	Schizophrenia	Phase 2	Completed	-	Japan ... more >> Hoyu Hospital Kure-City, Hiroshima-ken, Japan Collapse <<
NCT00854100	Major Depressive Disorder	Phase 2	Completed	-	-
NCT00404573	Schizophrenia	Phase 2	Completed	-	United States, Missouri ... more >> For information regarding investigative sites, contact Forest Professional Affairs St Louis, Missouri, United States, 63045 Collapse <<
NCT00694707	Schizophrenia	Phase 2	Completed	-	-
NCT00852202	Bipolar Depression	Phase 2	Completed	-	-
NCT00852202	-	-	Completed	-	-
NCT01376076	Schizophrenia	Phase 1	Completed	-	United States, California ... more >> Forest Investigative Site 001 Glendale, California, United States, 91206 Forest Investigative Site 004 Long Beach, California, United States, 90806 United States, New Jersey Forest Investigative Site 002 Willingboro, New Jersey, United States, 08046 United States, Texas Forest Investigative Site 003 Houston, Texas, United States, 77008 Collapse <<
NCT00488618	-	-	Completed	-	-
NCT00839852	Schizophrenia	Phase 2	Completed	-	-
NCT01396447	Depression, Bipolar	Phase 2	Completed	-	-
NCT02165098	Pharmacokinetic Profile	Phase 1	Completed	-	United Kingdom ... more >> Hammersmith Medicines Research London, United Kingdom, NW10 7EW Collapse <<
NCT01058668	Mania Bipolar... more >> I Disorder Collapse <<	Phase 3	Completed	-	-
NCT01396447	-	-	Completed	-	-
NCT01059539	Bipolar I Disorder	Phase 3	Completed	-	-
NCT00488618	Bipolar Disorder	Phase 2	Completed	-	United States, Missouri ... more >> For information regarding investigative sites, contact Forest Professional Affairs St. Louis, Missouri, United States, 63045 Collapse <<
NCT01058668	-	-	Completed	-	-
NCT01058096	Bipolar Disorder ... more >> Mania Collapse <<	Phase 3	Completed	-	United States, California ... more >> Forest Investigative Site 004 Long Beach, California, United States, 90813 Forest Investigative Site 005 Riverside, California, United States, 92506 Forest Investigative Site 007 San Diego, California, United States, 92123 United States, Illinois Forest Investigative Site 009 Chicago, Illinois, United States, 60640 United States, Louisiana Forest Investigative Site 006 Lake Charles, Louisiana, United States, 70601 United States, Mississippi Forest Investigative Site 001 Flowood, Mississippi, United States, 39232 United States, Missouri Forest Investigative Site 003 Creve Couer, Missouri, United States, 63141 United States, Ohio Forest Investigative Site 008 Cleveland, Ohio, United States, 44109 United States, Oklahoma Forest Investigative Site 010 Oklahoma City, Oklahoma, United States, 73116 United States, Texas Forest Investigative Site 002 Houston, Texas, United States, 77008 India Forest Investigative Site 106 Vijayawada, Andhra Pradesh, India, 520002 Forest Investigative Site 112 Vizag, Andhra Pradesh, India, 530017 Forest Investigator Site 108 Varanasi, Durgakund, India, 221005 Forest Investigative Site 103 Ahmedabad, Gujarat, India, 380013 Forest Investigative Site 120 Ahmedabad, Gujarat, India, 380015 Forest Investigative Site 105 Bangalore, Karnataka, India, 560010 Forest Investigative Site 107 Bangalore, Karnataka, India, 560027 Forest Investigative Site 118 Mangalore, Karnataka, India, 575001 Forest Investigative Site 113 Mangalore, Karnataka, India, 575018 Forest Investigative Site 115 Manipal, Karnataka, India, 576104 Forest Investigative Site 114 Mysore, Karnataka, India, 570004 Forest Investigative Site 101 Aurangabad, Maharashtra, India, 431005 Forest Investigative Site 110 Nasik, Maharashtra, India, 422101 Forest Investigative Site 111 Pune, Maharashtra, India, 411004 Forest Investigative Site 104 Pune, Maharashtra, India, 411030 Forest Investigative Site 121 Chennai, Tamilnadu, India, 600003 Forest Investigative Site 109 Kanpur, Uttar Pradesh, India, 200005 Forest Investigative Site 119 Lucknow, Uttar Pradesh, India, 226006 Collapse <<
NCT01104766	-	-	Completed	-	-
NCT01469377	-	-	Completed	-	-
NCT01715805	Major Depressive Disorder	Phase 3	Completed	-	-
NCT01104766	Schizophrenia	Phase 3	Completed	-	-
NCT03430544	Cocaine Use Disorder	Phase 2	Recruiting	July 31, 2020	United States, Pennsylvania ... more >> University of Pennsylvania Recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Stefanie Darnley, BS 215-746-1820 stefd@pennmedicine.upenn.edu Collapse <<
NCT03573297	Bipolar I Disorder ... more >> Mania Depression Collapse <<	Phase 3	Recruiting	July 17, 2021	-
NCT01104779	Schizophrenia	Phase 3	Completed	-	-
NCT03738215	Major Depressive Disorder	Phase 3	Not yet recruiting	July 9, 2021	United States, California ... more >> Omega Clinical Trials Not yet recruiting La Habra, California, United States, 92614 United States, Florida MD Clinical Not yet recruiting Hallandale Beach, Florida, United States, 33009 United States, Louisiana Dr. Gary J. Booker Not yet recruiting Shreveport, Louisiana, United States, 71104 United States, Oklahoma Sooner Clinical Research Not yet recruiting Oklahoma City, Oklahoma, United States, 73112 United States, Tennessee Clinical Neuroscience Solutions, Inc Not yet recruiting Memphis, Tennessee, United States, 38119 Collapse <<
NCT01058096	-	-	Completed	-	-
NCT01104779	-	-	Completed	-	-
NCT01469377	Major Depressive Disorder	Phase 2	Completed	-	-
NCT01412060	Schizophrenia	Phase 3	Completed	-	-
NCT03593213	Schizophrenia	Phase 3	Recruiting	June 7, 2021	-
NCT03739203	Major Depressive Disorder	Phase 3	Recruiting	July 9, 2021	-
NCT01412060	-	-	Completed	-	-
NCT02670538	Bipolar Disorder ... more >> Depression Collapse <<	Phase 3	Completed	-	-
NCT02670551	Bipolar Disorder ... more >> Depression Collapse <<	Phase 3	Completed	-	-
NCT01838876	Major Depressive Disorder	Phase 3	Completed	-	-
NCT01104792	Schizophrenia	Phase 3	Completed	-	-

靶点	Description	IC50
Dopamine Receptor D3		Ki:0.09nM
Dopamine Receptor D2		Ki:0.5nM
5-HT Receptor 1A		Ki:2.6nM

Cariprazine/卡利拉嗪 Catalog No. CSN16030

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