Cariprazine
Based on 7 publication(s) in Google Scholar
Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
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- 純度: 99.67%
- CAS 番号: 839712-12-8
- 分子式: C21H32Cl2N4O
- 分子量:427.41
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Cariprazine
More- Nature. 2024 Feb;626(7998):411-418. [Abstract]
- Nat Neurosci. 2022 Jan;25(1):39-49. [Abstract]
- Genes Dis. 2025 Jun 18;13(2):101718. [Abstract]
- ACS Chem Neurosci. 2020 Jan 15;11(2):173-183. [Abstract]
- J Pharm Biomed Anal. 2023 Nov 30:236:115740. [Abstract]
- Fundam Clin Pharmacol. 2022 Dec;36(6):976-984. [Abstract]
- Curr Zool. 2025 Jun 27.
Dopamine Receptor アイソフォーム固有の製品をすべて表示
More5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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5-HT1A Receptor |
D2 Receptor 0.49 nM (Ki) |
D3 Receptor 0.085 nM (Ki) |
5-HT1A Receptor 2.6 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
20.72 μM
Compound: Cariprazine
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Inhibition of recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential after 2 mins by patch clamp assay
Inhibition of recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential after 2 mins by patch clamp assay
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[PMID: 27487565] |
| HEK293 | EC50 |
110 nM
Compound: 2b, cariprazine, RGH-188
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Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
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[PMID: 24831693] |
| HEK293 | EC50 |
5.8 nM
Compound: 2b, cariprazine, RGH-188
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Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
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[PMID: 24831693] |
| HEK293 | IC50 |
1.7 nM
Compound: 2b, cariprazine, RGH-188
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Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
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[PMID: 24831693] |
Cariprazine stimulates inositol phosphate (IP) formation with a high potency (pEC50 8.5) with relatively low efficacy (Emax 30%)[2]. Cariprazine, a novel candidate antipsychotic, demonstrated approximately 10-fold higher affinity for human D3 versus human D2L and human D2S receptors (pKi 10.07, 9.16, and 9.31, respectively). Cariprazine displays high affinity at human serotonin (5-HT) type 2B receptors (pKi 9.24) with pure antagonism. Cariprazine has lower affinity at human and rat hippocampal 5-HT1A receptors (pKi 8.59 and 8.34, respectively) and demonstrates low intrinsic efficacy. Cariprazine displays low affinity at human 5-HT2A receptors (pKi 7.73). Moderate or low affinity for histamine H1 and 5-HT2C receptors (pKi 7.63 and 6.87, respectively) suggest Cariprazine's reduced propensity for adverse events related to these receptors[2]. Cariprazine is over sixfold more potent (EC50=1.4 nM) than Aripiprazole (EC50=9.2 nM) in inhibiting isoproterenol-induced cAMP production in HEK-293 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 839712-12-8
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性状 Solid
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分子量 427.41
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分子式 C21H32Cl2N4O
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Color White to light brown
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SMILES
O=C(N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1)N(C)C
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別名
RGH-188
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nature
2024 Feb;626(7998):411-418. PMID: 38297130 -
Nat Neurosci
Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. [Abstract]2022 Jan;25(1):39-49. PMID: 34887590 -
Genes Dis
circFKBP8(5S,6)-encoded protein promotes stress susceptibility in mice by down-regulating dopamine D3 receptor expression and its downstream AMPK/mTOR/ULK1 autophagy signaling. [Abstract]2025 Jun 18;13(2):101718. PMID: 41459113 -
ACS Chem Neurosci
Discovery of Procognitive Antipsychotics by Combining Muscarinic M1 Receptor Structure-Activity Relationship with Systems Response Profiles in Zebrafish Larvae. [Abstract]2020 Jan 15;11(2):173-183. PMID: 31850734 -
J Pharm Biomed Anal
Volumetric absorptive microsampling for the therapeutic drug monitoring of psychiatric patients treated with cariprazine. [Abstract]2023 Nov 30:236:115740. PMID: 37776628 -
Fundam Clin Pharmacol
Receptor density influences the recruitment bias of aripiprazole and brexpiprazole at the dopamine D2L receptor. [Abstract]2022 Dec;36(6):976-984. PMID: 35767599 -
溶剤 & 溶解度
DMSO : 2 mg/mL (4.68 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.34 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
These assays are done in 50 mM Tris (pH 7.4), 100 mM NaCl, 7 mM MgCl2, 1 mM EDTA, and 1 mM DTT. Assay tubes (final volume 250 μL) contain 50 μM (striatum and hippocampus) or 1 μM (D2 and D3 cell membrane) GDP, the ligand to be examined, and membrane suspension (250 μg tissue/tube for the striatum and hippocampus and 20 μg protein/tube for hD2 and hD3 membranes). Samples are preincubated for 10 min at 30°C. After the addition of 50 pM [35S]GTPγS, membranes are incubated for an additional 60 min at 30°C. Nonspecific binding is determined in the presence of 10 μM GTPγS; basal binding is determined in the presence of buffer only. The assay is terminated by rapid filtration through UniFilter GF/B using a harvester, and the membranes washed four times with 1 mL of ice-cold buffer. After drying (40°C for 1 h), 40 μL of Microscint is added to the filters, and the bound radioactivity is determined by a TopCount NXT counter[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells are seeded on a 24-well tissue culture plate in 500 μL of medium. Fifty microliters of medium containing 0.55 μCi myo-[3H]inositol is added (final concentration 1 μCi/mL) and incubated for 18-20 h. Cells are then washed three times with buffer containing 140 mM NaCl, 5 mM KCl, 2 mM CaCl2, 5 mM HEPES, 5 mM Na-HEPES, 20 mM glucose, and 10 mM LiCl (pH 7.4). Cells are then incubated for an additional 60 min (37°C) in medium with test compounds alone (agonist test) or alongside 1000 nM (±)-Quinpirole (antagonist test). Medium is then aspirated off, cells are lysed by adding 400 μL of 0.1 M HCl/2 mM CaCl2, and supernatants are frozen at −72°C. After thawing and centrifugation at 1000g for 10 min, 200 μL of each supernatant is loaded on 250 μL of AG1-X8 (formate form) anion exchange column. Effluent is discarded, and columns are washed twice in 1.5 mL of distilled water. IPs are eluted with 2.5 mL of 1 M ammonium formate/0.1 M formic acid directly into scintillation vials, 10 mL of Optiphase HiSafe 3 is added, and the radioactivity is determined in a TriCarb 4900 scintillation counter[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Experiments are performed on wild-type C57Bl/6J mice. In tests of cognitive functions, it is essential to employ concentrations of drugs that have no effects on emotional behavior and that do not impair locomotor activity. Whether Cariprazine (administered at a dose range of 0.005 to 0.15 mg/kg) is first tested affected the behavior of mice in the EPM, a test of anxiety-related behavior that is also critically dependent upon normal locomotor activity. Animals are exposed to an EPM apparatus designed for mice (leg height: 45 cm, arm length: 35 cm, lane width: 5 cm, wall height: 15 cm). Testing (under 100 lux lighting) is performed between 1 and 4 PM. Mice are placed in the center of the maze and their time spent in open arms and the number of closed and open arm entries during a 5 min test period is recorded. Measures of the time spent in open arms and the number of open arm entries served as a measure of anxiety-like behavior. The number of closed arm entries served as a measure of locomotor activity.
Rats[4]
Adult male Sprague-Dawley rats (150-300 g) are used. Cariprazine is dissolved in 0.9% saline and administered at 0.06, 0.25, 0.5, and 1.0 mg/kg via intraperitoneal (i.p.) injection 1 h before i.c.v. injection of ouabain and daily thereafter for 7 days. Open field activity is assessed immediately following the i.c.v. injection and again after 7 days (the activity is noted 10-14 h after the last i.p. injection of Cariprazine).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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参考文献
[1]. Seneca N, et al. Occupancy of dopamine D2 and D3 and serotonin 5-HT1A receptors by the novel antipsychotic drug candidate, cariprazine (RGH-188), in monkey brain measured using positron emission tomography. Psychopharmacology (Berl). 2011 Dec;218(3):579-8 [Content Brief]
[2]. Kiss B, et al. Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile. J Pharmacol Exp Ther. 2010 Apr;333(1):328-40. [Content Brief]
[3]. Zimnisky R, et al. Cariprazine, a dopamine D(3)-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse. Psychopharmacology (Berl). 2013 Mar;226(1):91-100 [Content Brief]
[4]. Gao Y, et al. Cariprazine exerts antimanic properties and interferes with dopamine D2 receptor β-arrestin interactions. Pharmacol Res Perspect. 2015 Feb;3(1):e00073. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3397 mL | 11.6984 mL | 23.3967 mL | 58.4918 mL |
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