北京若生智能科技有限公司
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naloxone HCl (REZENOPY)

✓ Approved

Scienture Inc. · OPRM1

什么是 naloxone HCl？

naloxone HCl 是一种治疗药物，由Scienture Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Inhaled。

药物档案

商品名REZENOPY
公司Scienture Inc.
分子靶点OPRM1
给药途径Inhaled
状态Approved
来源： ClinicalTrials.gov, Scienture Inc.

作用机制

分子靶点

naloxone HCl 作用于 1 个分子靶点：

OPRM1opioid receptor mu 1 (MOR1, LMOR)
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

naloxone HCl 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Injury, poisoning and procedural complicationsToxicity to various agents✓ Approved

相关研究文献

PubMedGels (Basel, Switzerland)2026-10-26

Insights into the Protonation State and Counterion Interactions of Linear Polyethyleneimine Materials.

Byrne Agustín J AJ, Vladimir Daniel D, Garro-Linck Yamila Y, Copello Guillermo J GJ et al.

Polyethyleneimine (PEI) polymers are widely used in the synthesis of nanoparticles, hydrogels and composite materials for biotechnological and environmental applications. However, the solid-state structural organization of linear PEI (L-PEI) materials, and how it is influenced by molecular weight, protonation state and counterion type, have not yet been comprehensively studied. In this work, solid-state nuclear magnetic resonance (ss-NMR), X-ray powder diffraction (XRD), small-angle X-ray scattering (SAXS) and time-domain NMR (TD-NMR) experiments were combined with theoretical calculations to analyze the local chemical environments, crystalline and nanoscale organization, and molecular mobility of L-PEI materials with different molecular weights. The analyzed materials were the free base (PEI·FB), the hydrochloride (PEI·HCl), the trifluoroacetate (PEI·TFA), and the sulfate-containing forms of L-PEI (PEI·Na2SO4 and PEI·H2SO4), as well as an intermediate protonation state obtained by the heterogeneous treatment with HCl-saturated isopropanol. Proton, 13C or 15N ss-NMR studies evidenced different chemical environments associated with changes in protonation state and counterion identity. Furthermore, XRD and SAXS showed that these variables, together with molecular weight and sample preparation conditions, influenced the crystalline arrangement and characteristic nanoscale organization of the polymer chains. Moreover, TD-NMR revealed the presence of three dynamically distinct proton populations, assigned to rigid, interfacial, and mobile domains, whose relative contributions and relaxation behavior varied among the PEI materials. Finally, high-resolution magic-angle spinning (HRMAS) NMR experiments were used to study different PEI-gel materials and films as well as the crosslinking of protonated PEI and sulfate ions.

PMID 42929946
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PubMedJournal of pharmacokinetics and pharmacodynamics2026-10-25

A mechanistic PK/PD model of fentanyl overdose and intranasal naloxone rescue incorporating receptor-level competition.

Hossain Jasmin A JA, Taft David R DR, Sweeney Kevin R KR, Khairuzzaman Akm A et al.

To develop and evaluate a PK/PD model that mechanistically describes the competitive interaction between intravenous (IV) fentanyl and intranasal (IN) naloxone at brain μ-opioid receptors (MORs) and simulates reversal of respiratory depression. A compartmental PK/PD model incorporating central, peripheral, brain and nasal compartments was parameterized sequentially using human plasma concentration, PET MOR-occupancy, and controlled isohypercapnic ventilation data, supplemented by literature-derived constraints where direct estimation was not supported. Fentanyl-MOR binding and release were modeled kinetically, whereas naloxone binding was represented by a rapid-equilibrium relationship. A 1,000-member virtual ensemble was used to propagate parameter uncertainty, and Sobol global sensitivity analysis evaluated determinants of ventilation recovery. The model reproduced the component clinical datasets used for calibration and simulated rapid ventilation recovery after IN naloxone. Simulations indicated that the apparent nasal-to-brain pathway was an important contributor to early rescue, whereas the systemic pathway contributed minimally during the first minutes after dosing. In nominal simulations, recovery began when the free brain naloxone:fentanyl molar concentration ratio reached approximately 0.063. Sobol analysis showed that fentanyl MOR affinity and brain disposition dominated very early recovery, while naloxone MOR affinity and apparent nasal-to-brain allocation became increasingly influential over the subsequent 10-15 minutes. This PK/PD framework links drug disposition, receptor competition and ventilation response in a unified model. It provides a mechanistic platform for evaluating naloxone dose, repeat-dosing, and formulation strategies while explicitly accounting for parameter uncertainty and the limitations of controlled isohypercapnic calibration data.

PMID 42927577
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PubMedBehavioural pharmacology2026-10-25

Reciprocal blockade of the opioid and D2-like dopamine receptors in the nucleus accumbens modulates the pain-related behaviors in an animal model of inflammatory pain.

Khodabakhsh Helia H, Ghalandari-Shamami Mohadeseh M, Barikrow Nooshin N, Yekta Batool Ghorbani BG et al.

Studies showed that dopamine and opioid systems in the brain have essential role in the modulation of pain perception. The evidence indicated that in the nucleus accumbens (NAc), both dopamine type 2 (D2) receptors and opioid receptors are highly expressed. However, the interaction of these systems in NAc was not investigated in the modulation of inflammatory pain. One hundred twenty-six adult male Wistar rats received unilateral microinjections of different doses of morphine (2.5, 5, 10, and 25 mmol/0.5 μl) and quinpirole (8, 16, and 32 mmol/0.5 μl) to assess their effects as opioid and D2-like receptor agonists in the NAc. In the next step, the rats were administered varying doses of sulpiride (3, 6, 12, and 24 mmol/0.5 μl), a D2-like receptor antagonist, before an effective dose of quinpirole (32 mmol/0.5 μl). They also received naloxone (1.5, 5, and 15 mmol/0.5 μl) before the same effective dose of quinpirole (32 mmol/0.5 μl). The formalin test was employed to evaluate their inflammatory pain thresholds. Results indicated that intra-accumbal administration of morphine- and quinpirole-induced antinociceptive responses. However, sulpiride significantly diminished these responses. Naloxone also reduced the quinpirole's antinociceptive effects. Interestingly, sulpiride was less effective in reversing the analgesic effects of morphine (η2 = 0.17 in the first phase and η2 = 0.37 in the late phase) than naloxone in reversing the quinpirole's analgesic effects (η2 = 0.4 in the first phase and η2 = 0.53 in the late phase). These findings suggest an interaction between the opioidergic and dopaminergic systems in pain relief.

PMID 42924872
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PubMedSubstance use & addiction journal2026-10-25

Initiatives to Prevent Fatal Drug Overdose Mortality After Incarceration.

Brickner Shanon S SS, Lopez Alexa A AA, Boch Samantha J SJ, LeBel Thomas P TP et al.

There is a direct relationship between fatal drug overdose and individuals who have been involved with the United States criminal legal system. Fatal drug overdose in the United States has reached unprecedented levels in the last decade, disproportionately affecting individuals involved with the criminal legal system and those who experience intersecting social and structural determinants of health. In addition, evidence shows that the immediate post-release period after incarceration is characterized by elevated overdose mortality. However, current policy structures, including the federal Medicaid Inmate Exclusion Policy, fragmented reentry systems, and inconsistent access to medications for opioid use disorder (MOUD), leave justice-involved populations without essential supports during this high-risk transition. This commentary synthesizes national evidence and proposes 3 policy initiatives to reduce post-incarceration overdose deaths: (1) adoption of the Section 1115 Medicaid Reentry Demonstration Waiver to provide prerelease screening, treatment initiation, care coordination, and bridge medication; (2) implementation of statewide carceral-based recovery support programs that integrate peer recovery coaches, trauma-informed care principles, naloxone training, and warm handoffs to community services; and (3) development of low-threshold community harm reduction hubs offering naloxone distribution, same-day and telehealth-enabled MOUD access, housing navigation, and peer support. These initiatives strengthen care continuity and target the transition periods where risk is greatest. Implementing these evidence-informed strategies is both a public health imperative and a critical step toward advancing health equity for criminal legal system-involved populations.

PMID 42921798
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PubMedTelemedicine journal and e-health : the official journal of the American Telemedicine Association2026-10-25

Teleoncology Implementation in a Low-Resource Setting: A Retrospective Cohort Study From Lubango, Angola.

Salamanca Paulo P, Antunes Maria Lina ML, Cangoma Cristina C, Garcia Teresa T et al.

We evaluated whether structured teleoncology could support the safe and affordable delivery of systemic oncology treatment at a provincial Angolan hospital without such installed capacity previously. Retrospective cohort study at Lubango Central Hospital (HCL), Angola, as a proof of principle, September 2024-May 2025. The initial analysis covered 85 patients discussed at a multidisciplinary tumor board (MTB) by videoconference; a second analysis assessed safety, outcomes, and costs in 23 patients treated at HCL. Efficacy was judged against palliative-intent indicators. In a cohort presenting overwhelmingly with advanced disease (87.0% stage III-IV), 93 cycles were delivered under remote supervision with no preparation errors, no contamination, no grade 4-5 adverse events (95% confidence interval 0-4.0%), no toxicity admissions, and no treatment-related deaths. Course completion reached 89.5%. The MTB processed 156 consultations and met all technical and operational targets; grade 1-3 events occurred in 16.1% of cycles, and partial remission reached 52.6%. Symptom onset to first presentation had a median of 6 months (range 1-11.7); the program-attributable interval was 1-2 weeks. Unit cost was 223,000 US dollars (USD); the drug cost was 251.93 USD per patient, against 643-794 USD averted per course in travel, lodging, and subsistence, and 533 USD per cycle in personnel costs (base salary). This program showed that systemic treatment under remote supervision was delivered safely and feasibly without a resident medical oncologist, with household savings of two and a half to three times the drug cost. This proof of principle suggests that the model may be workable elsewhere, though the small sample and absence of a control group limit firmer conclusions.

PMID 42922165
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PubMedJournal of food science and technology2026-10-25

Formulation and characterization of novel acid-induced spray-dried milk protein hydrogel.

Malik Bhawna B, Chawla Rekha R, Khatkar Sunil Kumar SK, Sihag Manvesh Kumar MK et al.

In this work, a suitable pH and temperature for the fabrication of hydrogels were optimised, and the effects of different pH on the functional characteristics of the hydrogels were studied. To create acid-induced hydrogels, sodium caseinate solutions (10%w/v) were acidified at pH 1.5, 1.75, 2.0, 2.25 and 2.5 using a 1 M HCl solution following heating at 70 °C for 5 min to form solid hydrogels. The hydrogel formed at pH 2.5 exhibited the maximum gel strength, however, reducing pH from 2.5 subsequently decreased the gel strength. The hydrogel was further processed into powder of which functional properties were investigated employing FTIR, DSC, swelling ratio and in-vitro protein digestibility. The swelling ratio, water-holding capacity (WHC) and the in-vitro digestibility of the protein hydrogel developed at pH 1.5 were greater than those of the hydrogels formed at higher pH. The FTIR micrographs confirmed that a slight shift of bonds in the restructured hydrogel was there compared to the non-gelled casein powder (control), nonetheless, non-significant differences were seen between pH 1.5-2.5. DSC results displayed that the high melting endothermic peaks in casein gels might be due to hydrogen bonds developed due to strong interactions with the water molecules during gelation.

PMID 42923475
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