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celecoxib + tramadol HCl (MR308 / Velyntra / Seglentis)

✓ Approved

Kowa · OPRM1 · 小分子

什么是 celecoxib + tramadol HCl?

celecoxib + tramadol HCl 是一种小分子,由Kowa研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

商品名MR308, Velyntra, Seglentis
公司Kowa
药物类别小分子
分子靶点OPRM1, PTGS2, SLC6A2, SLC6A4
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

celecoxib + tramadol HCl 作用于 4 个分子靶点:

OPRM1opioid receptor mu 1 (MOP, M-OR-1)
PTGS2prostaglandin-endoperoxide synthase 2 (PHS-2, PGG/HS)
SLC6A2solute carrier family 6 member 2 (NAT1, NET)
SLC6A4solute carrier family 6 member 4 (SERT1, 5-HTTLPR)
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

celecoxib + tramadol HCl 针对 2 个适应症,涉及 2 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved
Injury, poisoning and procedural complicationsProcedural painPhase III

相关研究文献

PubMedAntibiotics (Basel, Switzerland)2026-07-27

Suppression of Quorum Sensing and Virulence Factors by Meloxicam and Celecoxib in Methicillin-Resistant Staphylococcus aureus Clinical Isolates.

Ali Reham R, El-Domany Ramadan A RA, Shaaban Mona I MI

Background:Staphylococcus aureus is a major cause of life-threatening infections, and increasing antimicrobial resistance necessitates alternative therapeutic strategies. This study evaluated the antiquorum sensing and antivirulence activities of selected nonsteroidal anti-inflammatory drugs (NSAIDs) against S. aureus clinical isolates by targeting the accessory gene regulator (agr). Methods: Antimicrobial susceptibility and virulence factor production were evaluated in 56 S. aureus clinical isolates. The MICs of six NSAIDs (Diclofenac, ketoprofen, ketorolac, meloxicam, indomethacin and celecoxib) were determined by broth microdilution, and the effects of sub-MICs (½ and ¼ MIC) on virulence factors were assessed. The expression of agrA, hlb, and hld was analyzed by qRT-PCR, and molecular docking was performed to evaluate interactions with AgrA receptor. Results: Among the isolates, high resistance rates were accompanied with cefoxitin, ceftazidime, and cefepime. Hemolysin, protease, and lipase production were detected in 42.86%, 89.28%, and 94.64% of isolates, respectively. Meloxicam and celecoxib at sub-MIC levels significantly reduced hemolysin, protease, and lipase activities. Additionally, both drugs markedly downregulated agrA expression by 88.9-95.3% and significantly reduced hlb and hld expression by 90.5-99.9% without affecting bacterial growth. Molecular docking demonstrated favorable binding interactions with AgrA. Conclusions: Meloxicam and celecoxib could be promising adjunctive therapies against S. aureus through suppression of the Agr-regulated virulence traits.

PMID 42505670
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PubMedMetabolites2026-07-27

Cheonggukjang-Derived Bacillus Strains Exhibit Protective Effects Against HCl/Ethanol-Induced Gastric Injury Associated with Reduced Inflammatory Responses.

Lee Yun-Seong YS, Kim Sooah S

Hydrochloric acid (HCl)/ethanol-induced gastric mucosal injury is closely associated with oxidative stress and inflammatory responses. Probiotics are promising therapeutic agents for gastrointestinal disorders. Therefore, this study evaluated the preventive effects of Cheonggukjang-derived Bacillus strains on HCl/ethanol-induced gastric mucosal injury in a rat model (n = 5 per group), with emphasis on inflammatory mechanisms. Eight-week-old male Sprague-Dawley rats were orally administered Bacillus amyloliquefaciens C393 1.0 × 109 CFU (B393), Bacillus subtilis C439 1.0 × 109 CFU (B439), or B. subtilis C512 1.0 × 109 CFU (C512). Gastric injury was induced by oral administration of HCl/ethanol (150 mM HCl in 60% ethanol). HCl/ethanol exposure significantly increased symptom scores, gastric mucosal lesion area, and histopathological damage. Pretreatment with B393 and B439 significantly attenuated these alterations. Moreover, HCl/ethanol administration increased gastric secretion volume and decreased gastric pH, both of which were significantly normalized by B393 and B439. Serum levels of pro-inflammatory cytokines, including tumor necrosis factor-α and interleukin-6, were significantly elevated following HCl/ethanol exposure but were markedly reduced by B393 and B439. Immunohistochemical analysis demonstrated that nuclear factor-kappa B activation in gastric tissues was significantly suppressed in these groups. These findings indicate that Cheonggukjang-derived Bacillus strains exert strain-specific gastroprotective effects possibly by suppressing NF-κB-mediated inflammatory signaling.

PMID 42506433
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PubMedNanomaterials (Basel, Switzerland)2026-07-27

Synthesis of Analcime and ZSM-5 Zeolite by Diatomite Without Organic Structure-Directing Agent and Adsorption Properties of Their Acid-Modified Samples on Toluene.

Pan Fanghui F, Wang Jianxiang J, Iqbal Javed J, Yu Fei F et al.

Zeolites are porous aluminosilicate crystalline materials that are widely used for the adsorption of volatile organic compounds (VOCs). The synthesis of zeolites without organic structure-directing agents (OSDAs) is attractive because of its low cost and environmental friendliness. In this study, analcime and the ZSM-5 zeolite were synthesized from natural diatomite under OSDA-free conditions through different crystallization routes. Analcime was prepared by regulating the hydrothermal conditions, while the ZSM-5 zeolite was synthesized by combining hydrothermal condition regulation with seed-induced crystallization. Hydrochloric acid modification was further used to improve the pore structures and adsorption properties of the zeolites. The optimum acid treatment conditions were 1.0 mol·L-1 HCl for analcime and 0.5 mol·L-1 HCl for the ZSM-5 zeolite. After acid modification, the specific surface area and pore volume of analcime increased to 271.7 m2·g-1 and 0.130 cm3·g-1, respectively, and its tolune adsorption capacity increased from 18.3 mg·g-1 to 23.2 mg·g-1, corresponding to a 26.6% improvement. For the ZSM-5 zeolite, the optimal modified sample showed a specific surface area of 307.9 m2·g-1, a pore volume of 0.172 cm3·g-1, and a toluene adsorption capacity of 65.4 mg·g-1, which was 5.5% higher than that of the unmodified sample. Adsorption kinetic analysis indicated that pore diffusion played an important role in toluene adsorption, while acid modification introduced additional acid sites that contributed to chemisorption. Overall, the ZSM-5 zeolite showed a higher adsorption capacity than analcime because of its larger surface area, higher pore volume, and more accessible adsorption sites. This study provides a low-cost and environmentally friendly route for preparing diatomite-derived zeolite adsorbents for VOC removal.

PMID 42506497
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PubMedActa parasitologica2026-07-27

Axenic Cultivation of the First Human-Derived Breviata anathema from a Patient with Fascioliasis in West Bengal, India.

Sardar Sanjib Kumar SK, Ghosal Ajanta A, Saito-Nakano Yumiko Y, Suzuki Jun J et al.

To establish axenic cultivation of a human-derived Breviata anathema (strain T76) isolated from the stool of a patient with fascioliasis and to characterize its biological properties. T76 was maintained in American Type Culture Collection (ATCC) medium 207, supplemented with sulfate-reducing Desulfovibrio desulfuricans and co-cultured with Pseudomonas aeruginosa, at 30 °C. Axenic cultivation was attempted by transferring T76 flagellates to various axenic culture media supplemented with antibiotics for parasitic intestinal protozoan species. The 18 S rRNA gene sequence of T76 exhibited significant homology with the free-living, bacterivorous B. anathema (ATCC 50338), a member of the rare clade Obazoa. Axenic cultivation of B. anathema (T76) was achieved in YIGADHA-S medium, in which gluconic acid and dihydroxyacetone replaced glucose as energy substrates. B. anathema (T76) was isolated from a patient with fascioliasis, exposed through consumption of aquatic plants from ponds, a known habitat of this organism. Axenic cultivation of T76 was established in YIGADHA-S medium, originally developed for Entamoeba dispar, and cyst-like spherical bodies harboring flagellates were observed and exhibited resistance to 0.1 N HCl.

PMID 42507263
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PubMedCureus2026-07-27

Assessment of Drug Utilization Pattern of Antimicrobials Prescribed in the Orthopedic Department of a Tertiary Care Hospital.

Patil Kartiki P KP, Thorat Vandana M VM, Chawla Leesha L LL

Introduction The purpose of prescription patterns is to collect valid data, which would help in formulating appropriate guidelines to ensure the rational use of medicines. Unfortunately, information about the use of medicines in patients visiting orthopedic clinics in tertiary care hospitals in India, especially in Maharashtra, is scanty. Therefore, the present study was undertaken with the primary objective to evaluate the current drug-prescribing trend of antimicrobials in the management of inpatients of the orthopedic department and secondary objectives to assess group-wise distribution of antimicrobials prescribed to inpatients of the orthopedic department and to assess additional drugs prescribed to these patients. Methods This study was a cross-sectional observational study done on 99 patients who were admitted to the wards of the orthopedics department of the hospital. The drug utilization assessment was done by using the WHO core drug prescribing indicators. The assessment of the drugs prescribed according to the essential drug list was done using the National List of Essential Drugs Medicines (NLEM) 2022 of India. Results The study population was predominantly elderly (47.5% ≥60 years) with male predominance (62.6%), and falls (58.6%) as the leading cause, followed by road traffic accidents (35.3%). Antimicrobial use was dominated by broad-spectrum agents, particularly ceftriaxone (43.4%), ciprofloxacin (47.5%), and metronidazole (54.5%), with moderate use of aminoglycosides (35.4%). Fixed-dose combinations were led by Cefuroxime + Sulbactam (25.2%). Supportive therapy was extensive, including ranitidine (62.6%), tramadol (59.6%), antihypertensives, insulin, and nutraceuticals. Combination therapies such as Bromelain + Trypsin + Rutoside (37.4%) were frequently used. Conclusion This study reflects a pattern of polypharmacy characterized by extensive use of broad-spectrum antimicrobials and adjunctive therapies, emphasizing the need for rational prescribing practices and antimicrobial stewardship to optimize clinical outcomes and minimize resistance.

PMID 42504368
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PubMedMembranes2026-07-27

A Pseudoenzymatic Regulatory Role of the Noncatalytic Subunit of the Neurotoxin Vipoxin at Arachidonic-Acid-Containing Membrane Interfaces.

Petrova Svetla S, Mircheva Kristina K, Sotirovska Evgenia E, Grozev Nikolay Alexandrov NA et al.

Secreted phospholipases A2 (sPLA2s) act at lipid interfaces where enzymatic turnover is strongly influenced by membrane packing and interfacial physicochemical conditions. Vipoxin, a heterodimeric neurotoxin from Vipera ammodytes meridionalis, is one such complex, comprising a catalytically active sPLA2 subunit (VBC) and a catalytically impaired homolog, VAC, suggesting a pseudoenzymatic regulatory role. Using SAPC Langmuir monolayers as a model of arachidonic-acid-containing membranes, we monitored the compensated monolayer area change, ΔA(t), under barostatic conditions as an integrated readout of the interfacial behavior of Vipoxin and its isolated subunits. The responses revealed pronounced modulation by surface pressure and by the acidic acetate versus basic Tris-HCl subphase environment: VBC retained high catalytic competence under both conditions, whereas Vipoxin displayed greater environmental sensitivity, consistent with VAC-dependent modulation of enzyme-membrane coupling. VAC, although lacking canonical catalytic activity, produced measurable interfacial effects under acidic conditions and high lateral pressure. Analysis using the interfacial quality parameter Qm demonstrated that VAC modifies the pressure dependence of the heterodimer and stabilizes interfacial accommodation of VBC. These findings indicate that VAC functions as a pseudoenzymatic regulatory subunit whose role emerges from dynamic coupling between enzymatic activity and lipid interfacial organization.

PMID 42506206
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