Brexpiprazole5-HT2A, α1B-, and α2C-adrenergic receptors antagonist CAS# 913611-97-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 913611-97-9 | SDF | Download SDF |
PubChem ID | 11978813 | Appearance | Powder |
Formula | C25H27N3O2S | M.Wt | 433.57 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | OPC-34712 | ||
Solubility | DMSO : ≥ 48 mg/mL (110.71 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | 7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one | ||
SMILES | C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=CC(=O)N3)C4=C5C=CSC5=CC=C4 | ||
Standard InChIKey | ZKIAIYBUSXZPLP-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12 nM) and dopamine D2L (Ki=0.3 nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47 nM).In Vitro:Brexpiprazole, a novel serotonin-dopamine activity modulator: A role for serotonin 5-HT1A and 5-HT2A receptors. Brexpiprazole also shows potent antagonist activity at human nor adrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM). Brexpiprazole significantly potentiates nerve growth factor (NGF)-induced neurite outgrowth in PC12 cells, in a concentration dependent manner. Brexpiprazole (1 μM) increases the number of cells with neurites in PC12 cells. Treatment with Brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM) in conjunction with NGF (2.5 ng/mL) increases the number of cells with neurites, in a concentration-dependent manner[1].In Vivo:Brexpiprazole (0.01, 0.03, 0.1 mg/kg, p.o.) significantly ameliorates dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior. In addition, Brexpiprazole alone has no effect on social recognition in untreated controlmice. By contrast, neither Risperidone(0.03 mg/kg, p.o.) nor Olanzapine (0.03 mg/kg, p.o.) alters Dizocilpine induced social recognition deficits. Finally,the effect of Brexpiprazole on Dizocilpine-induced social recognition deficits is antagonized by WAY-100,635. These results suggest that Brexpiprazole can improve Dizocilpine-induced social recognition deficits via 5-HT1A receptor activation in mice[2]. References: |
Brexpiprazole Dilution Calculator
Brexpiprazole Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.3064 mL | 11.5322 mL | 23.0643 mL | 46.1287 mL | 57.6608 mL |
5 mM | 0.4613 mL | 2.3064 mL | 4.6129 mL | 9.2257 mL | 11.5322 mL |
10 mM | 0.2306 mL | 1.1532 mL | 2.3064 mL | 4.6129 mL | 5.7661 mL |
50 mM | 0.0461 mL | 0.2306 mL | 0.4613 mL | 0.9226 mL | 1.1532 mL |
100 mM | 0.0231 mL | 0.1153 mL | 0.2306 mL | 0.4613 mL | 0.5766 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Brexpiprazole is a potent antagonist effects on 5-HT2A, α1B-, and α2C-adrenergic receptors and a partial agonist at serotonin 1A (5-HT1A) and D2 receptors. [1]
5-HT1A receptor is a G protein-coupled receptor that can mediates inhibitory neurotransmission by binding the endogenous neurotransmitter serotonin5-HT. And D2 receptor is a G protein-coupled receptor inhibits adenylyl cyclase activity.
In cloned receptor systems, brexpiprazole displayed partial agonist at h5-HT1A and hD2 receptors, and potent antagonism of h5-HT2A receptors and hα1B/2C-adrenoceptors. [2] When tested in PC12 cells, brexpiprazole increased the number of cells with neurites in a concentration-dependent manner through 5-HT1A receptors and 5-HT2A receptors.[3]
In the dizocilpine-induced social recognition deficits mice model, brexpiprazole (0.01, 0.03, 0.1mg/kg,p.o.) significantly ameliorated the recognition deficits, and had no effect on social recognition in untreated control mice. Brexpiprazole may confer a beneficial effect on social cognition deficits in patients with psychiatric disorders. [1]
References:
[1]. Noriko Yoshimi, Takashi Futamura, Kenji Hashimoto. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. European Neuropsychopharmacology, http://dx.doi.org/10.1016/j.euroneuro.2014.12.014
[2]. Maeda K, Sugino H, Akazawa H et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. journal of pharmacology and experimental therapeutics, 2014 Sep;350(3):589-604.
[3]. Tamaki Ishima, Takashi Futamura, Yuta Ohgi et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin–dopamine activity modulator: A role for serotonin 5-HT1A and 5-HT2A receptors. European Neuropsychopharmacology, http://dx.doi.org/10.1016/j.euroneuro.2015.01.014
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Brexpiprazole.[Pubmed:28228056]
Ann Pharmacother. 2017 Apr;51(4):315-322.
OBJECTIVE: To review the pharmacology and clinical data for Brexpiprazole in schizophrenia and major depressive disorder (MDD). DATA SOURCES: An English-language literature search using PubMed and MEDLINE was performed using the term Brexpiprazole. All articles containing human clinical trial data published up to September 2016 were evaluated for inclusion as well as information from the manufacturer's product labeling. STUDY SELECTION/DATA EXTRACTION: Phase 3 trials for Brexpiprazole were evaluated. Key in vitro and animal data were incorporated into the pharmacology and pharmacokinetic sections where appropriate. DATA SYNTHESIS: Four phase 3 trials have evaluated the use of Brexpiprazole as a primary therapy for schizophrenia or as an antidepressant adjunct for MDD. For its schizophrenia indication, Brexpiprazole was studied in 2 placebo-controlled trials of approximately 1300 patients, with 4 mg of Brexpiprazole consistently showing superiority over placebo. For MDD, Brexpiprazole was compared with placebo as an adjunct to antidepressants in approximately 1000 patients who had failed trials of 1 to 3 prior antidepressants. The 2-mg and 3-mg dosages of Brexpiprazole showed consistent superiority over placebo in the MDD trials. Common treatment emergent adverse effects included akathisia and weight gain. CONCLUSIONS: Brexpiprazole showed efficacy for the treatment of schizophrenia in the range of 2 to 4 mg/d and as an adjunct to antidepressant therapy in MDD when dosed at 2 to 3 mg/d. Advantages of this drug include once-daily dosing, good tolerability, and lack of effect on sexual function. Disadvantages include the lack of long-term safety data and potentially high cost.
Clinical role of brexpiprazole in depression and schizophrenia.[Pubmed:28331332]
Ther Clin Risk Manag. 2017 Mar 10;13:299-306.
Brexpiprazole, a serotonin-dopamine activity modulator, is the second D2 partial agonist to come to market and has been approved for the treatment of schizophrenia and as an adjunctive treatment in major depressive disorder. With less intrinsic activity than aripiprazole at the D2 receptor and higher potency at 5-HT2A, 5-HT1A, and alpha1B receptors, the pharmacological properties of Brexpiprazole suggest a more tolerable side effect profile with regard to akathisia, extrapyramidal dysfunction, and sedation. While no head-to-head data are currently available, double-blind placebo-controlled studies show favorable results, with the number needed to treat (NNT) vs placebo of 6-15 for response in acute schizophrenia treatment and 4 for maintenance. NNT is 12 for response and 17-31 for remission vs placebo in major depression. In schizophrenia trials, treatment-emergent adverse effects (TEAEs) and discontinuation rates due to TEAEs were lower in treatment groups vs placebo (7.1%-9.2% vs 14.7%, respectively). Meanwhile, discontinuation rates due to TEAEs in depression studies were higher in treatment groups vs placebo (1.3%-3.5% vs 0-1.4%, respectively) and appeared dose dependent. Rates of akathisia are lower compared to those with aripiprazole and cariprazine, weight gain is more prominent than with aripiprazole, cariprazine, or ziprasidone, and sedation is less than with aripiprazole but more than with cariprazine. Brexpiprazole target dosing is 2-4 mg in schizophrenia and 2 mg in depression augmentation. Dose adjustments should be considered in hepatic or renal dysfunction and/or in poor cytochrome P450 2D6 metabolizers. While Brexpiprazole represents an exciting second entry for D2 partial agonists with positive studies thus far, direct head-to-head comparisons will shed more light on the efficacy and side effect profile of Brexpiprazole.