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aripiprazole (Abilify Maintena / Lu AF41155 / aripiprazole ERIS)

✓ Approved

Otsuka Holdings Co., Ltd. · DRD2 · 小分子

什么是 aripiprazole？

aripiprazole 是一种小分子，由Otsuka Holdings Co., Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intramuscular (IM) Injection。

药物档案

商品名Abilify Maintena, Lu AF41155, aripiprazole ERIS
公司Otsuka Holdings Co., Ltd.
药物类别小分子
分子靶点DRD2, HTR1A, HTR2A
给药途径Injectable (Others), Intramuscular (IM) Injection
状态Approved
来源： ClinicalTrials.gov, Otsuka Holdings Co., Ltd.

作用机制

分子靶点

aripiprazole 作用于 3 个分子靶点：

DRD2dopamine receptor D2 (D2DR, D2R)
HTR1A5-hydroxytryptamine receptor 1A (PFMCD, 5-HT1A)
HTR2A5-hydroxytryptamine receptor 2A (5-HT2A, HTR2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

aripiprazole 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersSchizophrenia✓ Approved
Psychiatric disordersBipolar disorder✓ Approved

相关研究文献

PubMedCase reports in psychiatry2026-10-26

When You Hear Hoofbeats, It May Still Be the Medication: A Case of Aripiprazole-Induced Hypersexuality Masquerading as Psychiatric Decompensation.

Cudjoe Nana N, Jenkins Terrance C TC, Stallworth Brittany B, Mwai Cansery Kathomi CK et al.

Aripiprazole has a known association with impulse-control disorders (ICDs), yet these adverse effects are frequently underrecognized and misattributed to psychiatric decompensation, particularly in women. We report a case of a 27-year-old African American woman with schizoaffective disorder who developed marked, new-onset hypersexual behavior temporally associated with aripiprazole. Aripiprazole accounts for a majority of ICDs reported among this class of antipsychotics, likely due to its D2/D3 partial agonism. This case highlights the critical need for clinicians to maintain a high index of suspicion for medication-induced ICDs when patients develop new impulsive or compulsive behaviors.

PMID 42928885
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PubMedChemMedChem2026-10-26

Synthesis of Nitrogen-Containing Heterocyclic Scaffolds and Applications in Scaffold Hopping: Development of an Aripiprazole Analog.

Alegbejo Price Temitayo Omowumi TO, Winant Pieterjan P, Júnior Paulo Eliandro da Silva PEDS, Melo Shaiani Maria Gil de SMG et al.

Heteroaromatic ring systems play a crucial role in drug development because they modulate physicochemical properties and expand the range of molecular interactions compared to non-heterocyclic aromatic rings. They are also widely represented among approved drugs. Among heteroatoms, nitrogen is the most prevalent in the diverse scaffold space of heterocyclic drugs, including those generated by fragment-based drug discovery approach. In this work, we show the synthesis of a set of novel or underexplored nitrogen heterocyclic fragments, obtained in three to five steps in moderate yields. In total, 12 fused [6,6] saturated/unsaturated bicycles were synthesized, which fulfill the general rule of fragment-like compounds. These heterocycles increased the fragment space of the CRAFT library and showed potential application in scaffold-hopping strategies for drug design. As a proof of concept, 2,6-naphthyridin-3-ol 2 was used to replace the 7-hydroxy-3,4-dihydroquinolin-2(1H)-one core of aripiprazole 41, generating 3-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-2,6-naphthyridine 40, that effectively blocked cocaine-induced hyperactivity in rodents at 20 mg/kg without inducing catalepsy, displaying a pharmacological profile similar to aripiprazole and demonstrating promising antipsychotic potential.

PMID 42928417
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PubMedBiotech (Basel (Switzerland))2026-10-26

Pharmaceutical Residues in Human Urine from Patients Under Antiretroviral Regimens and Self-Reported Healthy Individuals Before and After Three Months' Storage: Implication for Agricultural Reuse in Pretoria, South Africa.

Lizbelt Mugivhisa Liziwe ML, Faith Baloyi Khanyi BK, Oladeji Oluwaseun Mary OM, Olatunji Olatunde Stephen OS et al.

Background/Objectives: Pharmaceutical residues in human urine have raised serious concerns about the safe reuse of urine in agriculture. The current study investigates and compares the concentrations of pharmaceuticals in urine samples collected from male patients undergoing active antiretroviral regimens and self-reported "healthy individuals" at a government hospital in Pretoria, South Africa, and determines how the residues changed during three months of ambient storage, which is the usual recommendation before use in agriculture. Methods: The urine samples were collected in a plastic bottle to prevent fecal contamination, and 15 targeted compounds were analyzed using solid-phase extraction and liquid chromatography-mass spectrometry. The linearity ranged from 0.9910 to 0.9999, 75.5% to 99.1% for recovery, and intra-day and inter-day precision were below 6%. The urine from each group was collected into one pooled sample and then analyzed both pre- and post-storage. Results: Thirteen pharmaceuticals were detected in urine from patients on regular medication before storage; in "healthy individuals", detections rose from eight to twelve after storage. Concentrations in the composite samples after storage were higher for some of the compounds but lower for others, including caffeine, nevirapine, prednisolone and 17α-ethinylestradiol. Metformin was highest overall at 1186.25 µg/L and remained at 806.68 µg/L after storage. The highest concentration for all the pharmaceuticals was reported for metformin, with a value of 1186.25 µg/L, occurring in the group of patients on a regular regimen. There could be a possibility that the rise can be attributed to the hydrolysis of conjugated metabolites during storage; however, no analysis of conjugates was carried out. Conclusions: This study shows the need for appropriate treatment of human urine prior to its reuse as fertilizer and echoes the importance of further research into human exposure pathways and effective pharmaceutical removal strategies.

PMID 42930069
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PubMedBiosensors2026-10-26

Porous Transducers and Hybrid Recognition for Bulky Nitrosamine Impurities: Toward 3D-MXene-Aptamer Detection of Tricyclic NDSRIs.

Shah Tirath T, Patel Ankur A, Shah Jignesh J, Shah Darshil D

Pharmaceutical quality control faces an emerging problem with Tricyclic nitrosamine drug substance-related impurities (NDSRIs), for example, N-nitroso clozapine. The impurities preserve the compl ete structure of their parent active pharmaceutical ingredients, which consist of bulky lipophilic molecules with restricted conformational flexibility. The retention of bulky lipophilic structures from the parent active pharmaceutical ingredients in these impurities results in their complete overlap with other substances, which causes matrix ion suppression and weak ionization and unstable mass-spectrometric responses. The LC-MS/MS method functions as the official standard but its workflow requires excessive solvent use and produces complicated equipment systems, which prevent its use for routine ultra-trace monitoring. This narrative review analyzes hybrid electrochemical sensing technology to determine if it can solve the current problem by using tricyclic NDSRIs steric complexity as a functional benefit for detection purposes. The research combines data from nitrosamine detection with studies on porous 3D-printed electrodes, MXene electrochemistry, molecularly imprinted polymers, aptamer engineering and the computational systematic evolution of ligands by exponential enrichment (SELEX), molecularly imprinted polymer (MIP) and signal-off aptasensing. This review presents that planar electrodes create an unfavorable structure for bulky tricyclic analytes because they lead to surface obstruction and increased resistance during charge transfer. This review demonstrates that gyroid and TPMS-type porous scaffolds with a Ti3C2Tx MXene coating offer superior internal surface area, enhanced diffusion channels and accelerated electron movement. The dual MIP-aptamer system enables selective recognition by using MIP to perform shape-based target capture and specimen protection and aptamer to recognize specific molecular targets. The design process for aptamers includes E/Z nitrosamine isomer modeling, docking and molecular dynamics, and AI-based sequence selection methods, which form the core approach to targeting N-nitroso clozapine (N-CZN)-like proteins. This research outlines a new technique, which uses steric hindrance to block redox-probe entry, thus generating an electrical signal through current reduction. This review presents a fundamental operational model which supports the development of eco-friendly portable electrochemical devices to detect tricyclic NDSRIs with maximum sensitivity.

PMID 42930082
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PubMedJournal of chemical information and modeling2026-10-26

Bridging the Markush Gap in Optical Chemical Structure Recognition via a CLIP-Derived Visual Backbone and Synthetic Data Generation.

Huang Qixing Q, Chang Haohua H, Mao Liyun L, Shen Zihao Z et al.

The rapidly growing chemical literature contains invaluable information for pharmaceutical research and molecular biology, yet manual extraction on a large scale is increasingly impractical. Optical chemical structure recognition (OCSR), which converts molecular depictions into machine-readable representations, provides a key route toward automated chemical information extraction. However, existing OCSR methods remain limited in recognizing Markush structures, which are widely used in chemical documents, particularly pharmaceutical patents, because of their structural complexity and the scarcity of annotated data. Here, we introduce CLIP-OCSR, an encoder-decoder framework that integrates a domain-adaptively pretrained CLIP-RN50 vision encoder with a transformer decoder for chemical structure recognition, with a focus on Markush representations. To address data scarcity, we developed a synthetic data generation strategy that produces diverse Markush images paired with pseudo-SMILES representations encoding substituent, frequency, and position variations. Benchmarking demonstrates that CLIP-OCSR achieves competitive performance on standard OCSR benchmarks and shows strong capability in recognizing Markush structures involving substituents and frequency variations. For structures with position variations, CLIP-OCSR generates pseudo-SMILES predictions that retain the corresponding positional information, enabling the downstream enumeration of possible positional isomers. Beyond image-only OCSR, we extend CLIP-OCSR toward multimodal Markush structure extraction by integrating graphical recognition with LLM-based textual variable-definition extraction, enabling downstream structure instantiation. Overall, this work advances automated recognition of complex chemical structures and provides a framework for the structured extraction of Markush information from chemical documents.

PMID 42929585
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PubMedArchiv der Pharmazie2026-10-26

Clarifying Problems in the Synthetic Pathway Towards Methylene-Type Levodopa Acylals as Potential Prodrugs.

Keydel Tobias T, Theele Yann Y, Link Andreas A

Here, we report a practical synthetic pathway towards levodopa (l-DOPA) acylals with a special emphasis on problems occurring during preparation, low yields or unmanageable side reactions, and how to circumvent them. The key step can be performed rapidly by microwave irradiation in a green chemistry manner. Final compounds can be achieved after deprotection approaches but exhibit inadequate properties in terms of stability, thwarting the adaptation of the double ester concept discussed here to the important active pharmaceutical ingredient levodopa. However, a future outlook is provided, discussing potential structural and chemical changes for stable levodopa acylals.

PMID 42929392
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