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Aripiprazole (OPC-14597)

Alias: OPC-14597; OPC 14597; OPC14597
Cat No.:V0991 Purity: ≥98%
Aripiprazole (formerly OPC-14597; OPC 14597; OPC14597; trade name Abilify) is an approved atypical antipsychotic drug that acts as a high-affinity partial agonist of 5-HT receptor.
Aripiprazole (OPC-14597)
Aripiprazole (OPC-14597) Chemical Structure CAS No.: 129722-12-9
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Aripiprazole (OPC-14597):

  • Aripiprazole D8
  • Aripiprazole (1,1,2,2,3,3,4,4-d8) (Aripiprazole (1,1,2,2,3,3,4,4-d8))
  • Aripiprazole monohydrate (OPC14597)
  • Aripiprazole cavoxil
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Aripiprazole (formerly OPC-14597; OPC 14597; OPC14597; trade name Abilify) is an approved atypical antipsychotic drug that acts as a high-affinity partial agonist of 5-HT receptor. It is a powerful partial agonist at dopamine D2 and 5-HT1A receptors and an antagonist at 5-HT2A receptors, stabilizing the dopamine-serotonin system. Furthermore, aripiprazole has been reported to bind with the antagonist [3H]spiperone and the agonist [125I]7-OH-PIPAT at 0.70±0.22nM and 0.34±0.02nM, respectively.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT1A Receptor ( Ki = 4.2 nM ); 5-HT2A Receptor; 5-HT2B Receptor; 5-HT2C Receptor; D2 Receptor; D3 Receptor; D4 Receptor
ln Vitro

In vitro activity: Aripiprazole exhibits strong binding affinity towards both G protein-coupled and uncoupled receptor states. Aripiprazole strongly stimulates the inhibition of cAMP accumulation mediated by D2 receptors. [1] The dopamine receptors h5-HT(2B), hD(2L) and hD(3) are the ones for which aripiprazole has the highest affinity. However, it also has significant affinity (5-30 nM) for several other 5-HT receptors, including alpha(1A)-adrenergic, hH(1)-histamine, and 5-HT(1A), 5-HT(7). Other G protein-coupled receptors such as the 5-HT(1D), 5-HT(2C), alpha(1B)-, alpha(2A)-, alpha(2B)-, alpha(2C)-, beta(1)-, and beta(2)-adrenergic, and H(3)-histamine receptors are less sensitive to apipirazole (30-200 nM). Aripiprazole functions as a partial agonist at 5-HT(2A), 5-HT(2C), D(3), and D(4) receptors in addition to being an inverse agonist at 5-HT(2B) receptors. [2]

ln Vivo
Aripiprazole reduces the levels of extracellular 5-HIAA in the striatum and medial prefrontal cortex of drug-naive rats, but not in rats that have been continuously treated with ripiprazole. [3] Rat hippocampal dopamine release is markedly increased by apiprimeze (0.1 mg/kg and 0.3 mg/kg). The release of dopamine in the medial prefrontal cortex is slightly but significantly increased by apipicazole (0.3 mg/kg), but not in the nucleus accumbens. Dopamine release in the nucleus accumbens is markedly reduced by apipicazole at doses of 3.0 mg/kg and 10 mg/kg, but not in the medical prefrontal cortex. In the medial prefrontal cortex, apipicazole (0.3 mg/kg) momentarily increases the release of dopamine induced by haloperidol (0.1 mg/kg), while inhibiting the release of dopamine in the nucleus accumbens.[4]
Enzyme Assay
Radioligand Binding Assays [2]
A large number of transiently and stably transfected cloned human cDNAs, obtained via the resources of the National Institute of Mental Health Psychoactive Drug Screening Program (NIMH-PDSP), were used for radioligand binding and functional assays as previously detailed (Rothman et al, 2000; Tsai et al, 2000). Conditions for radioligand binding assays, along with KD values for standard compounds, are listed in Table 1. In initial screening assays, Aripiprazole was tested at a concentration of 10 μM in quadruplicate at a large number of GPCRs, ion channels, and transporters. For molecular targets at which >50% inhibition was measured, Ki determinations were obtained using at least six concentrations of Aripiprazole; Ki values were calculated in quadruplicate using GraphPad Prism. [125I]DOI competition assays were performed as previously described (Choudhary et al, 1992) with the following changes: 12 dilutions of aAripiprazole spanning a range of 0.01–3000 nM were incubated with [125I]DOI (0.3 nM) in total volumes of 0.25 ml at 25°C for 1 h with 5–20 μg of membrane protein in binding buffer (50 mM Tris buffer, pH 7.4, 0.5 mM EDTA, 10 mM MgCl2). Membranes were harvested with a Brandel cell harvester by three ice-cold washes onto polyethyleneimine-pretreated (0.3%) Whatman GF/C filters. Radioactivity bound to filters was quantified by liquid scintillation counting.
Aripiprazole is the first next-generation atypical antipsychotic with a mechanism of action that differs from currently marketed typical and atypical antipsychotics. Aripiprazole displays properties of an agonist and antagonist in animal models of dopaminergic hypoactivity and hyperactivity, respectively. This study examined the interactions of aripiprazole with a single population of human D2 receptors to clarify further its pharmacologic properties. In membranes prepared from Chinese hamster ovary cells that express recombinant D2L receptors, aripiprazole bound with high affinity to both the G protein-coupled and uncoupled states of receptors. Aripiprazole potently activated D2 receptor-mediated inhibition of cAMP accumulation. Partial receptor inactivation using the alkylating agent N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) significantly reduced the maximum effect of aripiprazole on inhibition of cAMP accumulation. This effect was seen with concentrations of EEDQ that did not alter the maximal inhibitory effect of dopamine. Consistent with the expected effects of a partial agonist, increasing concentrations of aripiprazole blocked the action of dopamine with maximal blockade equal to the agonist effect of aripiprazole alone. The efficacy of aripiprazole relative to that of dopamine varied from 25% in cells that lacked spare receptors for dopamine to 90% in cells with receptor reserve. These results, together with previous studies demonstrating partial agonist activity at serotonin 5-hydroxytryptamine (5-HT)1A receptors and antagonist activity at 5-HT2A receptors, support the identification of aripiprazole as a dopamine-serotonin system stabilizer. The receptor activity profile may underlie the unique activity of aripiprazole in animals and its antipsychotic activity in humans. [2]
Cell Assay
Effects of Aripiprazole on cAMP Production [2]
Inhibition of forskolin-stimulated cAMP production[2]
Inhibition of forskolin-stimulated 3′,5′-cyclic adenosine monophosphate (cAMP) production in stable D4 and 5-HT1A receptor expressing cell lines was measured as previously reported (Lawler et al, 1999; Zhang et al, 1994). In brief, cells were grown in 24-well plates and growth media were replaced with fresh F12 medium containing 100 μM IBMX and 100 μM forskolin (all on ice) just prior to experimentation. Serial dilutions (10-fold) of Aripiprazole ranging from 0.1 to 10.000 nM were added to the cells, which were then incubated 20 min at 37°C and 5% CO2. The reaction was terminated by aspiration and the addition of 0.5 ml of ice-cold 3% trichloroacetic acid. Plates were chilled for 1 h at 4°C and spun at 1000 g for 15 min. cAMP was quantified using a competitive binding assay adapted with minor modifications (Nordstedt and Fredholm, 1990). For measurement of cAMP content, trichloroacetic acid extracts (40 μl) were added to reaction tubes containing cAMP assay buffer (100 mM Tris-HCl, pH 7.4, 100 mM NaCl, 5 mM EDTA). [3H]cAMP (1 nM final concentration) was added to each tube, followed by cAMP-binding proteins (approximately 100 μg of crude extract from bovine adrenal cortex in 500 μl of cAMP buffer). The reaction tubes were incubated on ice for 2 h, then harvested with a Brandel cell harvester onto Whatman GF/C filters soaked in water. Filters were allowed to dry, and bound radioactivity was quantified by liquid scintillation counting. The concentration of cAMP in each sample was estimated from a standard curve ranging from 0.1 to 100 pmol of cAMP/assay.
Stimulation of cAMP production[2]
Studies of the effects of serotonin and Aripiprazole at 5-HT6 and 5-HT7 receptors were carried out in stable transfectants using methods previously described (Max et al, 1995; Monsma et al, 1993; Shen et al, 1993).
Animal Protocol
Three to five days after cannulation, a dialysis probe was implanted into the medial prefrontal cortex, hippocampus or nucleus accumbens under slight anesthesia with isoflurane. Rats were then housed individually overnight in a dialysis cage. After the overnight perfusion at 0.4 μl/min of the probe, the flow was increased to 1.5 μl/min. One hour later, the dialysate samples were collected every 30 min. The perfusion medium was Dulbecco's phosphate-buffered saline solution including Ca2+ (138 mM NaCl, 8.1 mM Na2HPO4, 2.7 mM KCl, 1.5 mM KH2PO4, 0.5 mM MgCl, 1.2 mM CaCl2, pH 7.4). After stable baseline values in the dialysates were obtained, each rat received two injections, vehicle/Aripiprazole, WAY100635/aripiprazole or Aripiprazole/haloperidol. The locations of the dialysis probes were verified at the end of each experiment by brain dissection. [4]
Aripiprazole was dissolved in 45% 2-hydroxypropyl-β-cyclodextrin (HBC) [4]
0.1 mg/kg and 0.3 mg/kg
Rats
ADME/Pharmacokinetics
Absorption, Distribution and Excretion
Tablet: Aripiprazole is well absorbed after administration of the tablet, with peak plasma concentrations occurring within 3 hours to 5 hours; the absolute oral bioavailability of the tablet formulation is 87%. ABILIFY can be administered with or without food. Administration of a 15 mg ABILIFY tablet with a standard high-fat meal did not significantly affect the Cmax or AUC of aripiprazole or its active metabolite, dehydro-aripiprazole, but delayed Tmax by 3 hours for aripiprazole and 12 hours for dehydro-aripiprazole. Oral Solution: Aripiprazole is well absorbed when administered orally as the solution. At equivalent doses, the plasma concentrations of aripiprazole from the solution were higher than that from the tablet formulation. In a relative bioavailability study comparing the pharmacokinetics of 30 mg aripiprazole as the oral solution to 30 mg aripiprazole tablets in healthy subjects, the solution-to-tablet ratios of geometric mean Cmax and AUC values were 122% and 114%, respectively. The single-dose pharmacokinetics of aripiprazole were linear and dose-proportional between the doses of 5 mg to 30 mg. Extended-release injectable suspension, bimonthly injection: Aripiprazole absorption into the systemic circulation is prolonged following gluteal intramuscular injection due to the low solubility of aripiprazole particles. The release profile of aripiprazole from ABILIFY ASIMTUFII results in sustained plasma concentrations over 2 months following gluteal injection(s). Following multiple doses, the median peak:trough ratio for aripiprazole following an ABILIFY ASIMTUFII dose is 1.3, resulting in a flat plasma concentration profile with Tmax ranging between 1 to 49 days following multiple gluteal administrations of 960 mg.
Following a single oral dose of [14C]-labeled aripiprazole, approximately 25% and 55% of the administered radioactivity was recovered in the urine and feces, respectively. Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.
The steady-state volume of distribution of aripiprazole following intravenous administration is high (404 L or 4.9 L/kg), indicating extensive extravascular distribution.
The clearance of aripiprazole was estimated to be 0.8mL/min/kg. Other studies have also reported a clearance rate of 3297±1042mL/hr.
Oral availability 87%. Aripiprazole is well absorbed and can be administered with or without food. Administration with a high fat meal did not affect the Cmax or AUC, but delayed Tmax by 3 hours for aripiprazole, and 12 hours for dehydro-aripiprazole.
Time to peak concentration: Peak plasma concentrations: within 3 to 5 hours.
The steady-state volume of distribution of aripiprazole following intravenous administration is high (404 L or 4.9 L/kg), indicating extensive extravascular distribution. At therapeutic concentrations, aripiprazole and its major metabolite are greater than 99% bound to serum proteins, primarily to albumin.
There was dose-dependent D2-receptor occupancy indicating brain penetration of aripiprazole in healthy human volunteers administered 0.5 to 30 mg per day.
For more Absorption, Distribution and Excretion (Complete) data for ARIPIPRAZOLE (8 total), please visit the HSDB record page.
Metabolism / Metabolites
Aripiprazole is metabolized primarily by three biotransformation pathways: dehydrogenation, hydroxylation, and N-dealkylation. Based on in vitro studies, CYP3A4 and CYP2D6 enzymes are responsible for the dehydrogenation and hydroxylation of aripiprazole, and N-dealkylation is catalyzed by CYP3A4. Aripiprazole is the predominant drug moiety in systemic circulation. At steady-state, dehydro-aripiprazole, the active metabolite, represents about 40% of aripiprazole AUC in plasma.
Aripiprazole is extensively metabolized in the liver principally via dehydrogenation, hydroxylations, and N-dealkylation by the cytochrome P-450 (CYP) 2D6 and 3A4 isoenzymes. The major active metabolite of aripiprazole, dehydro-aripiprazole, exhibits affinity for D2 receptors similar to that of the parent compound and represents approximately 40% of the aripiprazole area under the concentration-time curve (AUC) in plasma. Steady-state plasma concentrations of both aripiprazole and dehydro-aripiprazole are achieved within 14 days.
ABILIFY activity is presumably primarily due to the parent drug, aripiprazole, and to a lesser extent, to its major metabolite, dehydro-aripiprazole, which has been shown to have affinities for D2 receptors similar to the parent drug and represents 40% of the parent drug exposure in plasma.
Aripiprazole has known human metabolites that include dehydro-aripiprazole, 4-[(2-oxo-3,4-dihydro-1H-quinolin-7-yl)oxy]butanal, 4-Hydroxyaripiprazole, and 2,3-dichlorophenylpiperazine.
Aripiprazole is metabolized primarily by three biotransformation pathways: dehydrogenation, hydroxylation,and N-dealkylation.Based on in vitro studies,CYP3A4 and CYP2D6 enzymes are responsible for dehydrogenation and hydroxylation of aripiprazole, and N-dealkylation is catalyzed by CYP3A4.Aripiprazole is the predominant drug moiety in the systemic circulation. At steady-state, dehydro-aripiprazole, the active metabolite, represents about 40% of aripiprazole AUC in plasma (RxList, A308).
Route of Elimination: Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.
Half Life: 75-146 hours
Biological Half-Life
The mean elimination half-lives are about 75 hours and 94 hours for aripiprazole and dehydro-aripiprazole, respectively. For populations that are poor CYP2D6 metabolizers, the half-life of aripiprazole is 146 hours and these patients should be treated with half the normal dose. Other studies have reported a half-life of 61.03±19.59 hours for aripiprazole and 279±299 hours for the active metabolite.
The mean elimination half-lives are about 75 hours and 94 hours for aripiprazole and dehydro-aripiprazole, respectively.
Toxicity/Toxicokinetics
Toxicity Summary
IDENTIFICATION AND USE: Aripiprazole is used IM for the acute management of agitation associated with schizophrenia or bipolar disorder, mixed or manic, in adults for whom treatment with aripiprazole is appropriate and who require an IM antipsychotic agent for rapid control of behaviors that interfere with diagnosis and care (e.g., threatening behaviors, escalating or urgently distressing behavior, self-exhausting behavior). Aripiprazole is used orally for the acute treatment of irritability associated with autistic disorder. Aripiprazole is used orally as an adjunct to antidepressants for the acute treatment of major depressive disorder in adults. Aripiprazole is used orally as monotherapy or as an adjunct to either lithium or valproate for the acute treatment of manic or mixed episodes associated with bipolar I disorder with or without psychotic features in adults and pediatric patients 10-17 years of age. The drug also is used orally as monotherapy or as adjunctive therapy with lithium or valproate for the maintenance treatment of bipolar I disorder in adults and pediatric patients 10-17 years of age. Aripiprazole is used orally for the acute and maintenance treatment of schizophrenia in adults and adolescents 13-17 years of age. HUMAN EXPOSURE AND TOXICITY: A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with administration of antipsychotic drugs, including aripiprazole. Two possible cases of NMS occurred during aripiprazole treatment in the premarketing worldwide clinical database. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mental status, and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia). Additional signs may include elevated creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. ANIMAL STUDIES: In female mice, the incidences of pituitary gland adenomas and mammary gland adenocarcinomas and adenoacanthomas were increased at dietary dose of 3 to 30 mg/kg/day. Female rats were treated with oral doses of 2, 6, and 20 mg/kg/day of aripiprazole from 2 weeks prior to mating through day 7 of gestation. Estrus cycle irregularities and increased corpora lutea were seen at all doses, but no impairment of fertility was seen. Increased pre-implantation loss was seen at 6 and 20 mg/kg, and decreased fetal weight was seen at 20 mg/kg. Pregnant rabbits were treated with oral doses of 10, 30, and 100 mg/kg/day of aripiprazole during the period of organogenesis. Decreased maternal food consumption and increased abortions were seen at 100 mg/kg. Treatment caused increased fetal mortality (100 mg/kg), decreased fetal weight (30 and 100 mg/kg), increased incidence of a skeletal abnormality (fused sternebrae at 30 and 100 mg/kg) and minor skeletal variations (100 mg/kg). Aripiprazole and a metabolite (2,3-DCPP) were clastogenic in the in vitro chromosomal aberration assay in CHL cells with and without metabolic activation. The metabolite, 2,3-DCPP, produced increase in numerical aberrations in the in vitro assay in CHL cells in the absence of metabolic activation. A positive response was obtained in the in vivo micronucleus assay in mice, however,the response was shown to be due to a mechanism not considered relevant to humans.
Aripiprazole's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia. Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1A and 5- HT2A receptors, moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors and moderate affinity for the serotonin reuptake pump. Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors. Aripiprazole functions as a partial agonist at the dopamine D2 and the serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A receptor.
Interactions
Substrates of Hepatic Microsomal Enzymes: Substrates of CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4; pharmacokinetic interaction unlikely.
Hypotensive Agents: Potential pharmacologic interaction (additive hypotensive effects)
Famotidine: Coadministration of aripiprazole (given in a single dose of 15 mg) with a 40-mg single dose of the H2 antagonist famotidine, a potent gastric acid blocker, decreased the solubility of aripiprazole and, hence, its rate of absorption, reducing by 37% and 21% the Cmax of aripiprazole and dehydro-aripiprazole, respectively, and by 13% and 15%, respectively, the extent of absorption (AUC). No dosage adjustment of aripiprazole is required when administered concomitantly with famotidine.
Valproate: When valproate (500-1500 mg/day) and aripiprazole (30 mg/day) were coadministered at steady state, the C max and AUC of aripiprazole were decreased by 25%. No dosage adjustment of aripiprazole is required when administered concomitantly with valproate.
For more Interactions (Complete) data for ARIPIPRAZOLE (12 total), please visit the HSDB record page.
References

[1]. J Pharmacol Exp Ther. 2002 Jul;302(1):381-9.

[2]. Neuropsychopharmacology. 2003 Aug;28(8):1400-11.

[3]. Biochem Biophys Res Commun. 1999 Dec 20;266(2):560-3.

[4]. Eur J Pharmacol. 2004 Jun 16;493(1-3):75-83.

Additional Infomation
Therapeutic Uses
Antipsychotic Agents
Aripiprazole is used IM for the acute management of agitation associated with schizophrenia or bipolar disorder, mixed or manic, in adults for whom treatment with aripiprazole is appropriate and who require an IM antipsychotic agent for rapid control of behaviors that interfere with diagnosis and care (e.g., threatening behaviors, escalating or urgently distressing behavior, self-exhausting behavior).
Aripiprazole is used orally for the acute treatment of irritability associated with autistic disorder.
Aripiprazole is used orally as an adjunct to antidepressants for the acute treatment of major depressive disorder in adults.
For more Therapeutic Uses (Complete) data for ARIPIPRAZOLE (6 total), please visit the HSDB record page.
Drug Warnings
/BOXED WARNING/ WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of seventeen placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. ABILIFY (aripiprazole) is not approved for the treatment of patients with dementia-related psychosis. /Included in label/
/BOXED WARNING/ WARNING: INCREASED SUICIDALTHOUGHTS AND BEHAVIORS. Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of adjunctive ABILIFY or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. ABILIFY is not approved for use in pediatric patients with depression. /Included in label/
Contraindications: Known hypersensitivity reaction to aripiprazole or any ingredient in the formulation; such reactions have ranged from pruritus/urticaria to anaphylaxis.
Safety and effectiveness in pediatric patients with bipolar mania were established in a 4-week, placebo-controlled clinical trial in 197 pediatric patients aged 10 to 17 years. The incidence of discontinuation due to adverse reactions between aripiprazole-treated and placebo-treated pediatric patients (10 to 17 years) was 7% and 2%, respectively. Commonly observed adverse reactions associated with the use of aripiprazole in pediatric patients with bipolar mania (incidence of 5% or greater and aripiprazole incidence at least twice that for placebo) somnolence, extrapyramidal disorder, fatigue, nausea, akathisia, blurred vision, salivary hypersecretion, and dizziness. Although maintenance efficacy in pediatric patients has not been systematically evaluated, maintenance efficacy can be extrapolated from adult data along with comparisons of aripiprazole pharmacokinetic parameters in adult and pediatric patients.
For more Drug Warnings (Complete) data for ARIPIPRAZOLE (27 total), please visit the HSDB record page.
Pharmacodynamics
Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1a and 5-HT2a receptors (Ki values of 0.34 nM, 0.8 nM, 1.7 nM, and 3.4 nM, respectively), moderate affinity for dopamine D4, serotonin 5-HT2c and 5-HT7, alpha1-adrenergic and histamine H1 receptors (Ki values of 44 nM, 15 nM, 39 nM, 57 nM, and 61 nM, respectively), and moderate affinity for the serotonin reuptake site (Ki=98 nM). Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors (IC50>1000 nM).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H27CL2N3O2
Molecular Weight
448.39
Exact Mass
447.148
Elemental Analysis
C, 61.61; H, 6.07; Cl, 15.81; N, 9.37; O, 7.14
CAS #
129722-12-9
Related CAS #
Aripiprazole-d8; 1089115-06-9; Aripiprazole (1,1,2,2,3,3,4,4-d8); 1089115-04-7; Aripiprazole monohydrate; 851220-85-4; 1259305-26-4 (cavoxil)
PubChem CID
60795
Appearance
White to off-white solid powder
Density
1.3±0.1 g/cm3
Boiling Point
646.2±55.0 °C at 760 mmHg
Melting Point
139°C
Flash Point
344.6±31.5 °C
Vapour Pressure
0.0±1.9 mmHg at 25°C
Index of Refraction
1.593
LogP
5.59
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
7
Heavy Atom Count
30
Complexity
559
Defined Atom Stereocenter Count
0
SMILES
O=C1NC2=C(C=CC(OCCCCN3CCN(C4=CC=CC(Cl)=C4Cl)CC3)=C2)CC1
InChi Key
CEUORZQYGODEFX-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H27Cl2N3O2/c24-19-4-3-5-21(23(19)25)28-13-11-27(12-14-28)10-1-2-15-30-18-8-6-17-7-9-22(29)26-20(17)16-18/h3-6,8,16H,1-2,7,9-15H2,(H,26,29)
Chemical Name
7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one
Synonyms
OPC-14597; OPC 14597; OPC14597
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 10~90 mg/mL (22.3~200.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 3: 2.5 mg/mL (5.58 mM) in 10% DMF 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.


Solubility in Formulation 4: 2.5 mg/mL (5.58 mM) in 10% DMF 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2302 mL 11.1510 mL 22.3020 mL
5 mM 0.4460 mL 2.2302 mL 4.4604 mL
10 mM 0.2230 mL 1.1151 mL 2.2302 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
A Study to Assess the Safety and Efficacy of ASP4345 as Add-on Treatment for Cognitive Impairment in Subjects With Schizophrenia on Stable Doses of Antipsychotic Medication
CTID: NCT03557931
Phase: Phase 2    Status: Completed
Date: 2024-11-12
A Double-Blind, Randomized Comparative Study of Carliprazine and Aripiprazole in Patients with Acute Schizophrenia
CTID: NCT06589817
Phase: Phase 3    Status: Not yet recruiting
Date: 2024-09-19
Aripiprazole for Bipolar Disorder and Alcohol Use Disorder
CTID: NCT02918370
Phase: Phase 3    Status: Completed
Date: 2024-09-19
A Long-term, Extended Treatment Study of Aripiprazole in Pediatric Patients With Autistic Disorder
CTID: NCT01617460
Phase: Phase 3    Status: Completed
Date: 2024-08-06
Aripiprazole in Body Focused Repetitive Behaviors
CTID: NCT05545891
Phase: Phase 2    Status: Not yet recruiting
Date: 2024-08-01
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Maintenance Electroconvulsive Therapy (ECT) Versus Aripiprazole in Clozapine-resistant Schizophrenia
CTID: NCT06501339
Phase: Phase 4    Status: Not yet recruiting
Date: 2024-07-16


Long-term Antipsychotic Pediatric Safety Trial
CTID: NCT03522168
Phase:    Status: Completed
Date: 2024-07-10
Atypical Antipsychotic-induced Mitochondrial Dysfunction in Patients With Schizophrenia
CTID: NCT06236451
Phase: Phase 4    Status: Recruiting
Date: 2024-04-09
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies
CTID: NCT02893371
Phase:    Status: Terminated
Date: 2024-03-12
Efficacy of Biofeedback in the Treatment of Tic Disorder
CTID: NCT05361993
Phase: Phase 4    Status: Suspended
Date: 2024-03-08
Study on the Optimal Diagnosis and Treatment Strategy of Major Depressive Disorder Based on Anhedonia
CTID: NCT05389046
Phase: N/A    Status: Recruiting
Date: 2024-01-17
VA Aripiprazole vs Esketamine for Treatment Resistant Depression
CTID: NCT05554627
Phase: Phase 4    Status: Withdrawn
Date: 2024-01-05
Trial to Evaluate the Short-term Safety & Efficacy of Brexpiprazole Monotherapy in the Treatment of Adolescents With Schizophrenia
CTID: NCT03198078
Phase: Phase 3    Status: Completed
Date: 2023-12-20
A Trial of Multiple-doses of Aripiprazole in Adults With Schizophrenia or Bipolar 1 Disorder
CTID: NCT04030143
Phase: Phase 1/Phase 2    Status: Completed
Date: 2023-11-18
Fluoxetine vs Aripiprazole Comparative Trial (FACT)
CTID: NCT02357849
Phase: Phase 4    Status: Terminated
Date: 2023-11-15
Multidisciplinary Design to Optimize Schizophrenia Treatment Based on Multi-omics Data and Systems Biology Analysis
CTID: NCT06060886
Phase: Phase 4    Status: Not yet recruiting
Date: 2023-09-29
Sequenced Treatment Alternatives to Relieve Adolescent Depression (STAR-AD)
CTID: NCT05814640
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2023-08-14
Add-on Aripiprazole on Cardiometabolic Profile in Treatment Resistant Schizophrenia: RCT
CTID: NCT05766540
Phase: Phase 4    Status: Not yet recruiting
Date: 2023-07-20
Real-life Assessment of Abilify Maintena + Rexult in Schizophrenia
CTID: NCT05169268
Phase:    Status: Recruiting
Date: 2023-07-05
Substance Misuse To Psychosis for Stimulants
CTID: NCT03485417
Phase: Phase 2/Phase 3    Status: Recruiting
Date: 2023-07-05
Bioequivalence Study of Aripiprazole From Apipe 10 mg Orally Disintegrating Tablets (Man. by: P&C Labs (Pellets & CR Products), Egypt) Versus Abilify 10 mg Orodispersible Tablets (Otsuka Pharmaceutical Netherlands B.V., Netherlands)
CTID: NCT05804721
Phase: Phase 1    Status: Completed
Date: 2023-04-07
Impact of Aripiprazole on Postoperative Analgesia in Laparoscopic Hysterectomy
CTID: NCT05103410
Phase: Phase 4    Status: Completed
Date: 2023-02-06
A Safety Study Comparing LY2140023 to Atypical Antipsychotic Standard Treatment in Schizophrenic Patients
CTID: NCT00845026
Phase: Phase 2    Status: Completed
Date: 2022-11-08
Acceptance and Commitment Therapy in SSRI-Resistant Obsessive Compulsive Disorder
CTID: NCT02955654
Phase: N/A    Status: Withdrawn
Date: 2022-09-14
A Study of Safety and Tolerability in Subjects With Schizophrenia
CTID: NCT01354353
Phase: Phase 1    Status: Completed
Date: 2022-09-14
Bioequivalence Study of Aripiprazole in Healthy Adult Subjects Under Fasting Condition
CTID: NCT05532254
Phase: Phase 1    Status: Completed
Date: 2022-09-08
A Comparison Study of LY2140023 and Aripiprazole in Schizophrenia Patients
CTID: NCT01328093
Phase: Phase 3    Status: Terminated
Date: 2022-09-07
Aripiprazole Augmentation Therapy in Treatment-resistant Depression
CTID: NCT00276978
Phase: Phase 3    Status: Withdrawn
Date: 2022-08-10
Comparative Effectiveness Research Trial for Antidepressant Incomplete and Non-responders With TRD
CTID: NCT02977299
Phase: Phase 4    Status: Completed
Date: 2022-04-27
The Impact of Aripiprazole Long-acting on Myelin and Cognition in the Onset of Schizophrenia
CTID: NCT05322031
Phase: Phase 4    Status: Unknown status
Date: 2022-04-22
ABLE: Abilify in Bipolar Disorder for Long-term Effectiveness
CTID: NCT00484471
Phase: Phase 4    Status: Completed
Date: 2022-03-31
CAE Plus LAI in Individuals With Bipolar Disorder at Risk for Treatment Non-adherence (BD-CAEL)
CTID: NCT03408873
Phase: Phase 4    Status: Completed
Date: 2022-02-17
An Observational Drug Utilization Study of Asenapine in the United Kingdom (P08308)
CTID: NCT01498770
Phase:    Status: Completed
Date: 2022-02-04
Efficacy of Aripiprazole Versus Placebo in the Reduction of Aggressive and Aberrant Behavior in Autistic Children
CTID: NCT00468130
Phase: N/A    Status: Completed
Date: 2022-01-14
To Assess the Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Participants With Major Depressive Disorder (MDD)
CTID: NCT01123707
Phase: Phase 3    Status: Terminated
Date: 2021-12-22
Study to Evaluate the Efficacy, Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Participants With Major Depressive Disorder (MDD)
CTID: NCT01111565
Phase: Phase 3    Status: Terminated
Date: 2021-12-21
MAintain the Efficacy and Safety in Treatment of Schizophrenia After Switching to Long-acTing Injectable aRipiprazole From Oral Atypical Antipsychotics
CTID: NCT03376763
Phase: Phase 4    Status: Completed
Date: 2021-12-17
A Study to Compare Disease Progression and Modification Following Treatment With Paliperidone Palmitate Long-Acting Injection or Oral Antipsychotics in Participant's With Recent-onset Schizophrenia or Schizophreniform
CTID: NCT02431702
Phase: Phase 3    Status: Completed
Date: 2021-12-03
Safety and Efficacy of Brexpiprazole in the Treatment of Schizophrenia
CTID: NCT03874494
Phase: Phase 3    Status: Completed
Date: 2021-11-12
Study to Evaluate the Efficacy, Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Participants With Major Depressive Disorder (MDD)
CTID: NCT01111552
Phase: Phase 3    Status: Terminated
Date: 2021-10-26
Study to Evaluate the Efficacy, Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Participants With Major Depressive Disorder (MDD)
CTID: NCT01111539
Phase: Phase 3    Status: Terminated
Date: 2021-10-20
Efficacy & Safety Study of Once-weekly Oral Aripiprazole in Children and Adolescents With Tourette's Disorder
CTID: NCT01418339
Phase: Phase 3    Status: Completed
Date: 2021-10-07
Safety and Tolerability Study of Once-weekly Oral Aripiprazole in Children and Adolescents With Tourette's Disorder
CTID: NCT01416441
Phase: Phase 3    Status: Completed
Date: 2021-10-07
Efficacy & Safety Study of Once-weekly Oral Aripiprazole in Children and Adolescents With Tourette's Disorder (TD)
CTID: NCT01418352
Phase: Phase 3    Status: Completed
Date: 2021-10-07
Aripiprazole as an Adjunct to Atypical Antipsychotics for Weight Reduction and Improvement in Metabolic Profile
CTID: NCT02949752
Phase: Phase 4    Status: Completed
Date: 2021-07-21
Pan European Collaboration on Antipsychotic Naïve Schizophrenia II
CTID: NCT02339844
Phase: Phase 4    Status: Completed
Date: 2021-04-28
Trial to Evaluate the Long-term Efficacy of Oral Aripiprazole in the Treatment of Pediatric Participants With Tourette's Disorder
CTID: NCT03661983
Phase: Phase 4    Status: Terminated
Date: 2021-03-09
A Study Comparing the Efficacy and Safety of Ziprasidone and Aripiprazole for the Treatment fo Schizophrenia or Schizoaffective Disorder in Hospitalized Patients
CTID: NCT00634348
Phase: Phase 4    Status: Completed
Date: 2021-02-21
Clinical Efficacy and Change of Life Quality Through Using the Comprehensive Behavioral Intervention Treatment for Tics
CTID: NCT04765085
Phase: N/A    Status: Withdrawn
Date: 2021-02-21
Pharmacologic Treatment of Acute Episode of Schizophrenia: a Real World Study
CTID: NCT03289026
Phase: Phase 4    Status: Completed
Date: 2021-02-05
Effectiveness of Aripiprazole Long-acting Injection in Recent Onset and Chronic Schizophrenia Patients
CTID: NCT03839251
Phase: Phase 4    Status: Completed
Date: 2021-01-27
Aripiprazole Oral Solution in the Treatment of Children and Adolescents With Autistic Disorder
CTID: NCT03487770
Phase: Phase 3    Status: Completed
Date: 2020-12-29
Aripiprazole IM Depot in the Acute Treatment of Adults With Schizophrenia
CTID: NCT03172871
Phase: Phase 3    Status: Completed
Date: 2020-12-29
Aripiprazole Oral Solution in the Treatment of Children and Adolescents With Tourette's Syndrome
CTID: NCT03487783
Phase: Phase 3    Status: Completed
Date: 2020-12-29
A Trial of Single- and Multiple-doses of Aripiprazole in Adult Subjects With Schizophrenia or Bipolar I Disorder
CTID: NCT03854409
Phase: Phase 1    Status: Completed
Date: 2020-09-02
European Long-acting Antipsychotics in Schizophrenia Trial
CTID: NCT02146547
Phase: Phase 4    Status: Completed
Date: 2020-09-01
Atypical Antipsychotics Influence on the Safety of the Heart and Monitoring Indicators Model Building
CTID: NCT04446234
Phase: Phase 4    Status: Unknown status
Date: 2020-08-26
Examining the Effects of Antipsychotic Medications on Insulin Sensitivity
CTID: NCT00895921
Phase: Phase 4    Status: Completed
Date: 2020-08-11
Best Event Schizophrenia Trial--A Randomized Double-Blind Trial of Aripiprazole and Risperidone in Schizophrenia
CTID: NCT00712270
Phase: Phase 4    Status: Terminated
Date: 2020-07-28
A Trial to Explore Acceptance and Performance of Using a Digital Medicine System With Healthcare Professionals and Adults With Schizophrenia, Schizoaffective Disorder, or First Episode Psychosis on an Oral Atypical Antipsychotic
CTID: NCT03568500
Phase: Phase 4    Status: Completed
Date: 2020-07-16
Treatment of Children With ADHD Who do Not Fully Respond to Stimulants
CTID: NCT00279409
Phase: Phase 2    Status: Terminated
Date: 2020-06-19
Bergen Psychosis Project 2 - The Best Intro Study
CTID: NCT01446328
Phase: Phase 4    Status: Completed
Date: 2020-06-19
DIMES - DIgital MEdicine Study for Adults With Schizophrenia, Bipolar I Disorder, or Major Depression Currently Using Aripiprazole
CTID: NCT03881449
Phase: Phase 4    Status: Unknown status
Date: 2020-06-18
Combination Treatment for Augmenting Language in Children With ASD
CTID: NCT02574741
Phase: Phase 2    Status: Completed
Date: 2020-04-29
Antipsychotic Effects on Brain Function in Schizophrenia
CTID: NCT01913327
Phase: Phase 4    Status: Terminated
Date: 2020-04-20
Aripiprazole, Abilify Maintena Collaborative Clinical Protocol
CTID: NCT02717130
Phase: N/A    Status: Terminated
Date: 2020-04-13
Effectiveness of Second Generation Antipsychotics in First Episode Psychosis Patients: 1-year Follow-up
CTID: NCT02532491
Phase: Phase 4    Status: Unknown status
Date: 2020-02-12
Neurocognitive Effectiveness in Treatment of First-episode Non-affective Psychosis: 3-years Follow-up
CTID: NCT03883204
Phase: Phase 4    Status: Unknown status
Date: 2020-01-14
An Open-Label, Multicenter, Rollover, Long-term Study of Aripiprazole Intramuscular Depot in Participants With Schizophrenia
CTID: NCT01129882
Phase: Phase 3    Status: Completed
Date: 2020-01-06
Side Effect Study of Antipsychotic Medicines to Treat Childhood Bipolar Disorder
CTID: NCT00746252
Phase: N/A    Status: Terminated
Date: 2020-01-06
Double-Blind Placebo Controlled Study of Adjunctive Aripiprazole for Symptomatic Hyperprolactinemia In Premenopausal Women With Schizophrenia
CTID: NCT01338298
Phase: N/A    Status: Completed
Date: 2019-09-27
Effectiveness of Second Generation Antipsychotics in First Episode Psychosis Patients: 3-year Follow-up
CTID: NCT03090503
Phase: Phase 4    Status: Unknown status
Date: 2019-07-10
A Comparison of Medication Augmentation and PST in the Treatment of Depression in Older Adults
CTID: NCT01942187
Phase: Phase 4    Status: Withdrawn
Date: 2019-04-18
Aripiprazole, Abilify Maintena Collaborative Clinical Protocol
CTID: NCT02472652
Phase: Phase 4    Status: Terminated
Date: 2019-04-11
Aripiprazole (Abilify®) as an Adjunctive Treatment for Inadequate Response in Major Depressive Disorder
CTID: NCT01696617
Phase: Phase 4    Status: Completed
Date: 2019-04-09
Evaluating the Effectiveness of Aripiprazole and D-Cycloserine to Treat Symptoms Associated With Autism
CTID: NCT00198107
Phase: Phase 3    Status: Completed
Date: 2019-04-09
Therapeutic Drug Monitoring in Child and Adolescent Psychiatry
CTID: NCT01057329
Phase:    Status: Completed
Date: 2019-03-06
Family Intervention in Recent Onset Schizophrenia Treatment (FIRST)
CTID: NCT02600741
Phase:    Status: Completed
Date: 2019-01-23
Identification of Multi-modal Bio-markers for Early Diagnosis and Treatment Prediction in Schizophrenia Individuals
CTID: NCT03790085
PhaseEarly Phase 1    Status: Unknown status
Date: 2018-12-31
Side Effects of Newer Antipsychotics in Older Adults
CTID: NCT00245206
Phase: Phase 4    Status: Completed
Date: 2018-12-17
Safety and Efficacy of Cariprazine in Patients With Schizophrenia
CTID: NCT01104766
Phase: Phase 3    Status: Completed
Date: 2018-10-29
Biomarkers in Autism of Aripiprazole and Risperidone Treatment (BAART)
CTID: NCT01333072
Phase: Phase 4    Status: Completed
Date: 2018-09-26
Open-label Study to Evaluate the Effectiveness of an Intramuscular Formulation of Aripiprazole (OPC-14597) as Maintenance Treatment in Patients With Bipolar I Disorder
CTID: NCT01710709
Phase: Phase 3    Status: Completed
Date: 2018-09-21
Chinese First Episode Schizophrenia's Optimal Dynamic Antipsychotic Treatment Regime
CTID: NCT03510325
Phase: Phase 4    Status: Unknown status
Date: 2018-08-01
Aripiprazole in Children With Autism: A Pilot Study
CTID: NCT00208533
Phase: Phase 2    Status: Completed
Date: 2018-07-30
Preventing Relapse in Schizophrenia: Oral Antipsychotics Compared To Injectables: Evaluating Efficacy
CTID: NCT00330863
Phase: Phase 4    Status: Completed
Date: 2018-07-10
Metabolic Effects of Antipsychotics in Children
CTID: NCT00205699
Phase: Phase 4    Status: Completed
Date: 2018-06-15
Study to Determine the Pharmacokinetics, Safety & Tolerability of Aripiprazole in Adults With Schizophrenia
CTID: NCT03150771
Phase: Phase 1    Status: Completed
Date: 2018-06-12
VA Augmentation and Switching Treatments for Improving Depression Outcomes
CTID: NCT01421342
Phase: Phase 3    Status: Completed
Date: 2018-05-29
Exploratory Trial to Assess the Functionality of an Integrated Call Center for the Digital Medicine System
CTID: NCT02722967
Phase: Phase 2    Status: Completed
Date: 2018-05-23
Canadian Biomarker Integration Network for Depression Study
CTID: NCT01655706
Phase: Phase 3    Status: Completed
Date: 2018-05-11
Dopaminergic Effects of Adjunctive Aripiprazole on the Brain in Treatment-Resistant Depression
CTID: NCT00953745
Phase: N/A    Status: Completed
Date: 2018-04-19
Whole Blood and Plasma Sample Collection for the Development of Antipsychotic Immunoassays From Participants Taking Aripiprazole, Olanzapine, Paliperidone, or Risperidone
CTID: NCT02634463
Phase: Phase 1    Status: Completed
Date: 2018-04-18
Pharmacovigilance in Gerontopsychiatric Patients
CTID: NCT02374567
Phase: Phase 3    Status: Terminated
Date: 2018-02-28
Study of Aripiprazole to Reduce Medical Risks in Bipolar Disorder
CTID: NCT00665444
Phase: N/A    Status: Terminated
Date: 2017-11-22
An Exploratory Study of Naltrexone Plus Aripiprazole for Alcohol Dep
HAMLETT. Handling Antipsychotic Medication: Long-term Evaluation of Targeted Treatment. A pragmatic single blind RCT of continuation versus discontinuation/ dose reduction of antipsychotic medication in patients remitted after a first episode of psychosis
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2019-04-04
A Randomized, Placebo-controlled Trial to Evaluate the Long-term (ie, Maintenance) Efficacy of Oral Aripiprazole in the Treatment of Pediatric Subjects with Tourette’s
CTID: null
Phase: Phase 3, Phase 4    Status: Prematurely Ended
Date: 2019-01-31
A Multicenter, Randomized, Double-blind, Placebo- and Active controlled Trial to Evaluate the Efficacy of Brexpiprazole Monotherapy for the Treatment in Adolescents (13-17 years old) With Schizophrenia
CTID: null
Phase: Phase 3    Status: Ongoing, Prematurely Ended, Completed
Date: 2019-01-11
Metabolic Dysfunctions Associated with Pharmacological Treatment of Schizophrenia
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2018-05-23
A Multicentre, 8-week, Single-arm, Open-label, Pragmatic Trial to Explore Acceptance and Performance of Using a Digital Medicine System with Healthcare Professionals and
CTID: null
Phase: Phase 4    Status: Completed
Date: 2018-03-12
PREemptive Pharmacogenomic testing for Preventing Adverse drug REactions
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2017-06-09
TAILOR - a randomized clinical trial: Tapered discontinuation versus maintenance therapy of antipsychotic medication in patients with newly diagnosed schizophrenia or schizophreniform psychosis in remission of psychotic symptoms
CTID: null
Phase: Phase 4    Status: Prematurely Ended
Date: 2017-03-03
Pharmacovigilance in children and adolescents:
CTID: null
Phase: Phase 3    Status: Completed
Date: 2017-02-28
English: Are Antipsychotics Neurotoxic or Neuroprotective? A Randomised Multicentre Longitudinal Study for Comparison of Two Therapy Strategies for the Treatment of Schizophrenia.
CTID: null
Phase: Phase 4    Status: Prematurely Ended
Date: 2016-08-31
Evaluation of the necessity of a pharmacological treatment with antipsychotics for the prevention of relapse in long-term stabilized schizophrenic patients: a randomized, single-blind, longitudinal trial
CTID: null
Phase: Phase 4    Status: Completed
Date: 2014-11-04
EFFICACY AND SAFETY OF INHALED LOXAPINE COMPARED WITH IM ANTIPSYCHOTIC IN ACUTELY AGITATED PATIENTS WITH SCHIZOPHRENIA OR BIPOLAR DISORDER
CTID: null
Phase: Phase 3    Status: Completed
Date: 2014-10-31
Randomized, flexible-dose, open-label comparison to investigate the effectivenes of second generation antipsychotics in first episode psychosis patients.
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2014-08-05
Interventional, open-label, flexible-dose extension study of aripiprazole once-monthly in patients with schizophrenia
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-11-12
Dopaminergic genotype of schizophrenic patients and the benefit of adjunctive aripiprazole to risperidone treatment. The effect on hormonal and metabolic measures
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2013-10-17
A Phase 3, Multicenter, Extension of Study ALK9072-003 to Assess the Long-term Safety and
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-03-28
A 26-week, Multicenter, Open-label, Extension Study of Aripiprazole Intramuscular Depot (OPC-14597, Lu AF41155) in Patients with Schizophrenia
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-03-25
A 28-week, randomised, open-label study evaluating the effectiveness of aripiprazole once-monthly versus paliperidone palmitate in adult patients with
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-03-20
An Open-Label, Multicenter Study Evaluating the Safety and Tolerability of Once-daily Oral Aripiprazole in Children and Adolescents with Tourette’s Disorder
CTID: null
Phase: Phase 3    Status: Ongoing, Prematurely Ended, Completed
Date: 2013-03-12
A Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled Study of the Efficacy and Safety of ALKS 9072 in Subjects with Acute Exacerbation of Schizophrenia
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-02-19
A 52-week, Multicenter, Open-label Study to Evaluate the Effectiveness of an Intramuscular Depot Formulation of Aripiprazole (OPC-14597) as Maintenance Treatment in Patients with Bipolar I Disorder
CTID: null
Phase: Phase 3, Phase 4    Status: Completed
Date: 2013-02-14
A Multicenter, Randomized, Double-blind, Placebo-controlled Study Evaluating the Safety and Efficacy of Fixed-dose Once-daily Oral Aripiprazole in Children and Adolescents with Tourette’s Disorder
CTID: null
Phase: Phase 3    Status: Not Authorised, Prematurely Ended, Completed
Date: 2013-01-30
A 52-week, Multicenter, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Efficacy, Safety, and Tolerability of an Intramuscular Depot Formulation of Aripiprazole (OPC-14597) as Maintenance Treatment in Patients with Bipolar I Disorder
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-01-13
A 12-week, Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled Trial of Aripiprazole Intramuscular Depot (OPC-14597, Lu AF41155) in the Acute Treatment of Adults With Schizophrenia
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-01-11
Randomized multicentric open-label phase III clinical trial to evaluate the efficacy of continual treatment versus discontinuation based in the presence of prodromes in a first episode of non-affective psychosis.
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2012-06-08
Long-Term Open-Label Safety Study of Pomaglumetad Methionil in Patients with Schizophrenia
CTID: null
Phase: Phase 3    Status: Completed, Prematurely Ended
Date: 2012-02-06
A Multicenter, Open-label Study to Assess Hospitalization Rates in Adult Subjects with Schizophrenia Treated Prospectively for 6 Months with Aripiprazole IM Depot Compared with 6-month Retrospective Treatment with Oral Antipsychotics in a Naturalistic Community Setting in Europe, Canada, and Asia.
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2012-01-30
Clinical and neuropsychological factors associated with second generation antipsychotic response in patients diagnosed with first episode of early onset schizophrenia spectrum disorders
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2012-01-02
A Multicenter, Randomized, Double-blind, Placebo-controlled Study Evaluating the Safety and Efficacy of Fixed-Dose Once-weekly Oral Aripiprazole in Children and Adolescents with Tourette’s Disorder
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2011-12-15
An Open-Label, Multicenter Study Evaluating the Safety and Tolerability of Once-weekly Oral Aripiprazole in Children and Adolescents with Tourette’s Disorder
CTID: null
Phase: Phase 3    Status: Completed, Prematurely Ended
Date: 2011-12-15
A Multicenter, Randomized, Double-blind, Placebo-controlled Study Evaluating the Safety and Efficacy of Flexible-Dose Once-weekly Oral Aripiprazole in Children and Adolescents with Tourette's Disorder
CTID: null
Phase: Phase 3    Status: Completed
Date: 2011-11-07
A Long-term, Multicenter, Open-Label Study to Evaluate the Safety and Tolerability of Flexible-Dose Oral Aripiprazole (OPC-14597) as Maintenance Treatment
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2011-06-14
A Multicenter, 52-week, Open-label Study to Assess the Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Patients with Major Depressive Disorder
CTID: null
Phase: Phase 3    Status: Completed, Prematurely Ended
Date: 2011-04-14
The Bergen-Stavanger-Innsbruck-Trondheim Study
CTID: null
Phase: Phase 4    Status: Completed
Date: 2011-04-14
A Phase 3, Multicenter, Double-Blind Comparison of LY2140023 and Aripiprazole in Patients with DSM-IV-TR Schizophrenia Followed by Open-Label Treatment with LY2140023
CTID: null
Phase: Phase 3    Status: Completed, Prematurely Ended
Date: 2011-04-06
Cognitive impairment in bipolar disorder treated with aripiprazole
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-01-04
An Open-Label, Multicenter, Rollover, Long-term Study of Aripiprazole Intramuscular Depot in Patients with Schizophrenia
CTID: null
Phase: Phase 3    Status: Completed
Date: 2010-12-22
A Multicenter, Randomized, Double-blind Study to Evaluate the Efficacy, Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Patients with Major Depressive Disorder.
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2010-12-15
A Multicenter, Randomized, Double-blind Study to Evaluate the Efficacy, Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Patients with Major Depressive Disorder.
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2010-11-02
A Multicenter, Randomized, Double-blind Study to Evaluate the Efficacy, Safety and Tolerability of an Oral Aripiprazole/Escitalopram Combination Therapy in Patients with Major Depressive Disorder.
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2010-10-04
A Long-Term, Open-Label, Multicenter Study of LY2140023 Compared to Atypical Antipsychotic Standard of Care in Patients with DSM-IV-TR Schizophrenia
CTID: null
Phase: Phase 2    Status: Completed
Date: 2010-09-07
A 24-month, Prospective, Randomized, Active-Controlled, Open-Label, Rater Blinded, Multicenter, International Study of the Prevention of Relapse Comparing Long-Acting Injectable Paliperidone Palmitate to Treatment as Usual with Oral Antipsychotics Monotherapy in Adults With Schizophrenia.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2010-03-10
A pilot study of Aripiprazole treatment for antipsychotic induced hyperprolactinaemia in young patients with severe mental illness and learning disabilities.
CTID: null
Phase: Phase 4    Status: Completed
Date: 2010-02-09
The TEA Trial- Tolerance and Effect of Antipsychotics in children and adolescents with psychosis
CTID: null
Phase: Phase 4    Status: Completed
Date: 2010-02-08
Estudio de Fase 2, de 17 Semanas, Multicéntrico, Aleatorizado y Doble Ciego, Sobre la Eficacia de LY2140023 Combinado con Tratamiento Clínico Habitual Comparado con Placebo Combinado con Tratamiento Clínico Habitual, en Pacientes con Esquizofrenia con Síntomas Negativos Prominentes
CTID: null
Phase: Phase 2    Status: Completed
Date: 2010-02-02
Estudio multicéntrico, aleatorizado, doble ciego, controlado, de dosis flexibles y grupos paralelos para evaluar la ef e.querySelector("font strong").innerText = 'View More' } e

Biological Data
  • Aripiprazole is a low potency partial agonist at the 5-HT1A receptor stably expressed in 1ACHO cells. Neuropsychopharmacology . 2003 Aug;28(8):1400-11.
  • Effect of aripiprazole on serotonin 5-HT2A receptors. Neuropsychopharmacology . 2003 Aug;28(8):1400-11.
  • Aripiprazole is an inverse agonist at the 5-HT2B receptor in HEK-293 cells. Neuropsychopharmacology . 2003 Aug;28(8):1400-11.
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