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

PubMedDiabetes, obesity & metabolism2026-09-10

Dose-Normalised Time in Range (dn-TIR) Improves Following Hybrid Closed-Loop (HCL) Therapy in Type 1 Diabetes: A Real-World Cohort Study From Australia and the United Kingdom.

Wellens-Mensah Jude J, Konantambigi Akash A, Lopez Keimee K, Triay Jessica J et al.

To evaluate dose-normalised time in range (dn-TIR) and its log relative change (Δdn-TIR) as measures of within-person glycaemic change relative to total daily insulin exposure following hybrid closed-loop therapy (HCL/AID). We conducted a retrospective two-cohort study of people with type 1 diabetes commencing hybrid closed-loop/automated insulin delivery (HCL/AID) therapy in Australia and the United Kingdom (UK). dn-TIR was calculated as time in range (TIR) 3.9-10.0 mmol/L (70-180 mg/dL) divided by total daily insulin dose (TDD) and Δdn-TIR as log[(TIR/TDD)post/(TIR/TDD)pre]. The study comprised 86 people living with type 1 diabetes in Australia and 288 in the UK. In the fixed Australian dn-TIR cohort, TIR increased from 53.2% ± 20.7% to 70.4% ± 14.6% (n = 86; p < 0.001), whereas mean TDD changed from 53.3 to 52.0 units/day (n = 86; p = 0.724). Median Δdn-TIR was 0.224 [IQR: -0.033, 0.583]. In the UK cohort, TIR increased from a median 54% [34, 68] to 66% [54, 74] (n = 257; p < 0.001), whereas mean TDD changed from 44.1 to 46.3 units/day (n = 242; p = 0.152). Median Δdn-TIR was 0.194 [IQR: -0.097, 0.541]. HCL/AID therapy improved TIR relative to TDD in two real-world cohorts. dn-TIR and Δdn-TIR are not replacements for established CGM metrics or direct measures of insulin sensitivity; they may provide an adjunct longitudinal description of whether glycaemic improvement was accompanied by proportionately greater, similar or lower insulin exposure.

PMID 42717560
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PubMedJournal of medicinal chemistry2026-09-10

From Fragment Hit to Clinical Candidate: Discovery of Dual H1R/H4R Ligands with Superior Efficacy in Allergic Conjunctivitis.

Weber Peter P, Smits Rogier R, Lim Herman D HD, Andaloussi Mounir M et al.

Dual inhibition of the histamine H1 and H4 receptors (H1R and H4R) has been shown to provide superior anti-inflammatory efficacy in preclinical models of allergic disease compared to selective inhibition of either receptor alone. Building on this concept, we initiated a fragment-based discovery program and previously identified a quinazoline-containing fragment hit. Here, we describe the lead optimization toward compounds with unique dual H1R/H4R activity. Structure-activity relationship studies yielded potent and balanced ligands with nanomolar affinities for both receptors, as well as pharmacokinetic properties suitable for ocular administration. Among these, quinazoline 35.HCl (GD136) and tetrahydroquinazoline 72.HCl (GD134) demonstrate robust in vivo efficacy in a ragweed-induced mouse model of allergic conjunctivitis, significantly reducing hyperemia and outperforming selective H1R or H4R antagonists. Based on its pharmacological profile, ADME properties, ease of formulation, and in vivo efficacy, GD134 was selected as the clinical development candidate for a first-in-class dual-targeted therapy of allergic conjunctivitis.

PMID 42720497
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PubMedJournal of the International Society of Sports Nutrition2026-09-10

Creatine formulations and repeated sprint training: effects on physical and physiological adaptations in soccer players during the short-term preparation phase.

Duan Changyuan C, Wang Zaitao Z, Wang Qianjin Q

This research examined the impact of various creatine (Cr) supplementation formulations during a 4-week preparatory phase on the efficacy of repeated sprint training (RST) and on improvements in physical and physiological performance in male soccer athletes. A total of forty collegiate young soccer players volunteered for the study. They were randomly divided into four groups: creatine monohydrate (Cr-Mon, n = 10), creatine ethyl ester (Cr-Ee, n = 10), creatine hydrochloride (Cr-Hcl, n = 10), and placebo (PL, n = 10). All athletes engaged in a 4-week training intervention, three times a week (i.e. 12 sessions), and physical (countermovement vertical jump [CMVJ], 20-m sprint, and L-run) and physiological (Wingate anaerobic power and incremental exercise tests) performance were assessed both before and after the training period. All training groups improved physical and physiological performance following the 4-week intervention period (p < 0.05). Additionally, the groups receiving the Cr supplement exhibited significantly greater changes (p = 0.001) in physical performance, peak power output, and fatigue index compared to the PL group. However, no significant differences were found among the groups regarding mean power output and VO2max. Notably, the Ee and Hcl forms of Cr showed superior gains (p < 0.05) in physical performance and peak power compared to the Mon form after the 4-week intervention. The results underscore the importance of Cr ingestion in enhancing adaptations for short-term physical performance tasks, highlighting the effectiveness of the Ee and Hcl forms in further improving the CMVJ, 20-m sprint, L-run, and peak power among soccer players during the short-term preparation phase.

PMID 42720250
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PubMedThe Journal of chemical physics2026-09-09

Dynamically biased microcanonical treatment of HCl dissociative chemisorption on Au(111) yields thermal associative desorption dynamics by detailed balance.

Bernard Mark E ME, Harrison Ian I

A dynamically biased microcanonical transition state theory model of HCl dissociative chemisorption on Au(111) was recently developed for Shirhatti et al.'s [J. Phys. Chem. Lett. 7, 1346 (2016)] non-equilibrium supersonic molecular beam experiments where normal translational energies varied over a 50-250 kJ/mol range. Model parameters include a relatively low threshold energy for reaction, E0 = 30.88 kJ/mol; an efficiency, εn = 0.26, for molecular normal translational energy to contribute to the active exchangeable energy capable of promoting reaction; and one surface oscillator, s = 1, involved in the local gas-surface collision complex wherein energy was taken as microcanonically exchangeable, although potentially subject to dynamical bias through efficiencies. To validate the model, detailed balance was used to predict the desorbing HCl product state distributions from thermal associative desorption of H(c) + Cl(c) on Au(111) that have been measured by Rettner and Auerbach [Science 263, 365 (1994)] while impinging a H atom beam onto a chlorinated Au(111) surface. Modeling of Rettner's [J. Chem. Phys. 101, 1529 (1994)] rovibrationally resolved HCl product state distributions allowed for the additional establishment of a rotational efficiency of εr = 0.23 that led to consistent prediction of both the thermal associative desorption and the supersonic molecular beam experimental results. The HCl(g) ⇄ H(c) + Cl(c) reactivity on Au(111) is thereby identified as a new benchmark system for gas-surface reactivity where highly detailed experimental data are available coming from both sides of the reaction barrier. The activation energy for thermal associative desorption was estimated as Ea,assoc = 5.6 ± 1.3 kJ/mol based on four independent kinds of measurement. The effect of dynamics on the thermal dissociative sticking coefficient, S(T), of interest in practical catalysis, was quantitatively assessed. As compared to a statistically behaving HCl/Au(111) system with Ea = 31 kJ/mol, dynamics reduced S(T) by a factor of 10 at 800 K, equivalent to an increase in activation energy of ΔEa = 15 kJ/mol.

PMID 42713950
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PubMedThe AAPS journal2026-09-09

Investigating the Impact of Food Induced Fluid Viscosity on Disintegration and Dissolution of Immediate Release Midodrine HCl Tablet.

Doole Fathima T FT, Don Ranganath Wahalathantrige RW, Poudel Ishwor I, Lex Timothy T et al.

The prediction of bioavailability (BA) and bioequivalence (BE) for immediate-release (IR) solid oral dosage forms is critical during development and post-approval phases of drug products. ICH M13A provides the option of using in vitro tests, such as disintegration and dissolution in biorelevant media, pilot studies, and modeling to justify not conducting in vivo fed BE studies. The gastrointestinal (GI) tract environment changes significantly after food intake, including variations in pH, enzyme activity, and fluid viscosity that influence drug dissolution and absorption. Existing biorelevant dissolution media (FeSSIF, FeSSGF etc.) simulate human GI fluid composition but do not account for food-induced viscosity changes. This study explored impacts of food-induced fluid viscosity (pH 1.2 buffer containing hydroxypropyl methylcellulose (HPMC)) on disintegration and dissolution profiles of midodrine HCl tablets. Using USP Apparatus II and disintegration testing, we evaluated dissolution and disintegration of five approved generic midodrine HCl tablets with demonstrated BE. High-viscosity media significantly delayed tablet disintegration and drug dissolution compared to low-viscosity fasting conditions. We modified dissolution methods to closely simulate fed state GI conditions by varying agitation speed, prolonging dissolution time, adding medium stagewise to simulate dilution of gastric fluid, and adding water to mimic co-administered drinks. Results showed increased dissolution with higher agitation speeds and continued dissolution in viscous media over extended time. Stagewise dissolution in medium with reduced viscosity to mimic gastric secretion did not accelerate drug release compared to viscous media. In contrast, co-administered water enabled tablet swelling and disintegration, leading to complete drug release within 15 min, which is more consistent with the in vivo PK data under fed conditions. These findings may help refine in vitro dissolution conditions to better mimic fed-state.

PMID 42711604
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PubMedAAPS PharmSciTech2026-09-09

Mechanistic Insights into Moxifloxacin HCl Permeability from Nitrocellulose-Based In Situ Gels via Confocal Imaging and DFT Modeling.

Lertsuphotvanit Nutdanai N, Senarat Setthapong S, Puapermpoonsiri Utsana U, Jungsuttiwong Siriporn S et al.

This study reports the development and multiscale evaluation of a nitrocellulose (Nc)-based in situ gel (ISG) system for localized delivery of moxifloxacin HCl (Mx) in periodontitis therapy. The formulations, composed of 15% w/w Nc dissolved in glycerol formal (Gf) or dimethyl sulfoxide (DMSO), exhibited rapid gelation within 1-3 min upon exposure to simulated crevicular media. SEM revealed solvent-dependent matrix morphology, with DMSO-based ISG forming denser and more porous structures, while Gf-based systems showed smoother, lamellar-like architectures. In vitro drug release through porcine mucosa membrane studies using Franz diffusion demonstrated sustained release profiles. CLSM imaging confirmed depth-restricted tissue penetration of sodium fluorescein (Sf), with fluorescence limited to < 50 µm in Nc-based ISGs versus > 100 µm Sf-loaded solvent controls. Drug distribution analysis further showed increased retention in Nc matrix and porcine mucosa in which Nc-formulations retarded diffusion into the receptor medium. DFT analysis revealed that Nc-Mx complex exhibited the most apparent binding energy (-2.43 eV) compared to Mx-solvent and Nc-solvent interactions, supporting a polymer-drug affinity-driven release mechanism. Collectively, these results establish Nc-based ISG as a promising platform for targeted mucosa-retentive delivery of antibiotics in periodontal therapy, combining tunable matrix formation with molecular-level control over drug diffusion.

PMID 42711593
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