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propafenone hydrochloride (propafenone, SR / propafenone SR / Rythmol SR)

✓ Approved

GSK · SCN5A · 小分子

什么是 propafenone hydrochloride?

propafenone hydrochloride 是一种小分子,由GSK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propafenone, SR, propafenone SR, Rythmol SR
公司GSK
药物类别小分子
分子靶点SCN5A
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

propafenone hydrochloride 作用于 1 个分子靶点:

SCN5Asodium voltage-gated channel alpha subunit 5 (CMD1E, SSS1)
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

propafenone hydrochloride 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
Cardiac disordersAtrial fibrillation✓ Approved
Cardiac disordersVentricular fibrillation✓ Approved

相关研究文献

PubMedPrimary health care research & development2026-09-11

Self-reported physical activity in a randomized study from Norwegian Healthy Life Centres.

Iglebæk Martin Svege MS, Espeland Jardar J, Meland Eivind E, Mildestvedt Thomas T

This study examines firstly if participation in a three-month intervention at Norwegian Healthy Life Centres (HLCs) improved self-reported physical activity (SR-PA), and secondly to what extent physical activity (PA) status at six months and changes from baseline were associated with demographic and motivational predictors. Regular PA is promoted as a central component of public health initiatives aimed at preventing noncommunicable diseases. This randomized controlled trial included 118 participants (57 in the intervention group) recruited from HLCs in South-western Norway. The intervention effect was assessed by comparing the intervention group with the waiting-list control group after six months. We examined sociodemographic and motivational predictors of change combining both groups into a single cohort. This trial was registered at ClinicalTrials.gov (ID: NCT02247219). At six-month follow-up, participants in the intervention group reported higher levels of SR-PA compared with the control group. The estimated effect was modest (B = 0.26, 95% CI -0.01 to 0.53), equivalent to ≈0.37 SD. Although the confidence interval included zero, the estimate remained compatible with a modest positive effect. Autonomous motivation and social support were positively associated with SR-PA after 6 months, while psychological defiance showed a negative association. Autonomous motivation and psychological defiance impacted PA change during the 6-month period in opposite directions.

PMID 42723291
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PubMedMolecular therapy : the journal of the American Society of Gene Therapy2026-09-11

D-Amino Acid Prodrug DLMEH Activates mTORC1 via Sestrin2 to Restore Muscle Protein Synthesis in Sarcopenia.

Shim Jae Ho JH, Lee Ji Yeon JY, Ahn Byung Kook BK, Woo Sang Woo SW et al.

Sarcopenia, the age-related loss of skeletal muscle mass and function, lacks FDA-approved pharmacotherapy. The mechanistic target of rapamycin complex 1 (mTORC1), activated by leucine via Sestrin2, is the master regulator of muscle protein synthesis, but L-leucine suffers from rapid catabolism and poor bioavailability. Here, we report D-leucine methyl ester hydrochloride (DLMEH), a metabolically stabilized prodrug incorporating D-stereoisomer conversion, methyl esterification, and hydrochloride salt formation. Three orthogonal biophysical methods demonstrate that DLMEH directly binds Sestrin2 (Kd 28.3 μM), equivalent to L-leucine. Sestrin2 siRNA knockdown and rapamycin co-treatment confirm Sestrin2-dependent, mTORC1-specific activation. In human primary myotubes, DLMEH (100 μM) restores dexamethasone-suppressed protein synthesis by 58.2%, significantly exceeding L-leucine (800 μM, 28.5%). In a rat dexamethasone-induced atrophy model, intravenous DLMEH (100 mg/kg/day, 14 days) preserves gastrocnemius mass (19.3% rescue), grip strength (90% of normal), and treadmill endurance (85% of normal), all superior to oral L-leucine. RNA-seq reveals 41.7% reversal of dexamethasone-induced transcriptomic changes with enrichment in mTOR signaling, ribosome biogenesis, and oxidative phosphorylation. Safety profiling establishes NOAEL at 2000 mg/kg with therapeutic index greater than 30. DLMEH represents a first-in-class Sestrin2-targeting mTORC1 activator for sarcopenia.

PMID 42723280
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PubMedJournal of the Association for Research in Otolaryngology : JARO2026-09-11

Structural and Molecular Evidence for a Frequency-Dependent Electrochemical Gradient in the Human Cochlear Lateral Wall.

Creff Gwenaelle G, Staxäng Karin K, Ladak Hanif M HM, Agrawal Sumit S et al.

The stria vascularis (SV) is a tripartite epithelium lining the lateral wall (LW) of the human cochlea, generating a positive endocochlear potential (EP) essential for auditory sensory transduction. There remains limited information about its variable structure and organization along the cochlear spiral or whether an electrochemical gradient exists. Here, we used three-dimensional (3D) synchrotron radiation phase-contrast imaging (SR-PCI) and light and transmission electron microscopy (LM and TEM) to examine the human SV and spiral ligament (SL) at different frequency locations based on the SR-PCI. Results were compared with recent molecular analyses performed in our laboratory. Volumetric and microanatomic analyses of the LW and SV, including critical K+ recycling pathways were made at different frequency locations on matched cochlear frequency maps based on Greenwood's formula. TEM analyses were correlated with previous results obtained on the expression of ion transporter and channels including the multiplex RNAscope® technique. The LW diminished in volume a 100-fold and the SV 14-fold in the cochlear apical turn. Ultrastructural analyses showed reduced cellularity in the SV and SL. Moreover, the organization and architecture of the SV cell and vascular pattern modified along the cochlear spiral. Claudius cell outline, TEM, and prior results of Na/K-ATPase activity and GJB2 gene transcript distribution suggest there is a reduced K+ recycling potential and water flux in the LW of the apical cochlea. Macro-, micro-, and recent molecular anatomical studies suggest that the human cochlear "battery" may be less potent in the apex. This could indicate that sensory transduction at low frequencies may be partially power-driven by more basal regions. Frequency-dependent variations in electrochemistry may have pathophysiological significance in connection with metabolic hearing loss and surgical treatments such as cochlear implantation.

PMID 42722797
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PubMedAnnals of medicine and surgery (2012)2026-09-11

Neuroprotective effects of chrysin in a rat model of Parkinson's disease.

Moradi Sana S, Rajaei Farzad F, Darabi Shahram S

Chrysin, or 5,7-dihydroxyflavone, is a flavonoid with antioxidant, anti-inflammatory, and anti-apoptotic effects, which are significant in Parkinson's disease. The objective of the study is to investigate the protective effects of chrysin in Parkinson's disease. Wistar strain rats were divided into three groups: treatment (receiving chrysin before and after OHDA-6 injection), control (injected with 0.9% normal saline into the left striatum), and lesion (injected with 0.9% normal saline and OHDA-6 into the left striatum). Behavioral testing with apomorphine hydrochloride was conducted 1 week before and 4 weeks after surgery. For histological examination, black blocks of tissue were prepared, and Nissl staining was used for neuron counting. Microscopic studies were performed by capturing images of the slides. In the behavioral test conducted after apomorphine injection and before surgery, there was no significant difference in the number of rotations among the control, lesion, and treatment groups. However, after surgery, this difference was significant between the lesion and treatment groups (P ≤ 0.05). In Nissl staining, a significant difference in the number of neurons in the substantia nigra was observed between the treatment and lesion groups. According to the results obtained from this study, chrysin prevented the neurodegeneration caused by OHDA-6, leading to a lower rate of mortality in the neurons of the midbrain substantia nigra.

PMID 42724797
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PubMedGlobal advances in integrative medicine and health2026-09-11

Efficacy and Safety of Laser Acupuncture in the Treatment of Children With Autism Spectrum Disorder: A Systematic Review.

Dong Deborah D, Xu Lujie L, Thompson-Hodgetts Sandy S, Jou Hsing H et al.

Preliminary evidence suggests acupuncture may be helpful for pediatric autism; however, needles may be a source of healthcare trauma, so non-needle options should be prioritized. To conduct a systematic review (SR) to synthesize the current evidence on the efficacy and safety of laser acupuncture for pediatric autism. We searched the following databases from inception until Nov 14, 2024: MEDLINE, CINAHL, EMBASE, Scopus, PsycINFO, Cochrane Library, SinoMed and China National Knowledge Infrastructure and J-Stage. Randomised controlled trials of laser acupuncture on children up to age 18 years of age with ASD were included. Outcomes were autism symptoms, adverse effects and language development indicators. The PRISMA-A checklist was used to guide conduct and reporting. A total of two trials (n=76) were included. The quality of evidence for most indicators were considered low to very low by GRADE criteria. Meta-analysis was not possible due to heterogeneity in populations and outcomes. Results suggest acupuncture groups benefited compared to no treatment. There were no adverse effects reported by parents of the participants in either trial. Two studies indicate benefits of laser acupuncture in children with autism but given the low quality of evidence, results should be regarded with caution. Additional well conducted randomized controlled trials with larger sample sizes are required to build evidence. This protocol is registered in the International Prospective Register of Systematic Reviews (PROSPERO), registration number: CRD42024576887.

PMID 42724412
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PubMedPhysical chemistry chemical physics : PCCP2026-09-11

Synergistic non-metal doping and heterojunction engineering in B-doped Bi2MoO6/MIL-88B(Fe) for efficient photocatalytic tetracycline degradation under visible light.

Song Linjie L, Chigan Tonglin T, Ma Jingfang J, Hui Yaguang Y et al.

Among diverse photocatalytic materials, Bi2MoO6 (BMO) has attracted significant attention by virtue of its unique layered structure, narrow bandgap, and tunable energy band configuration. However, its practical application was hindered by inefficient separation of photogenerated carriers and inadequate visible-light utilization. To overcome these limitations, synergistic modification through elemental doping and heterojunction construction was implemented in this study. Herein, boron-doped Bi2MoO6 (B-BMO)/MIL-88B(Fe) composites with Z-scheme heterojunctions were fabricated via a facile solvothermal method. Boron doping effectively modulated the energy band structure, reduced the bandgap, enhanced the light absorption capacity, and induced lattice distortion. Meanwhile, the staggered energy band alignment between MIL-88B(Fe) and B-BMO facilitated Z-scheme heterojunction formation, which strengthened charge carrier separation while maintaining a strong redox capability. Under visible-light irradiation, the B-BMO/MIL-88B(Fe) composite achieved 91.26% degradation efficiency for tetracycline hydrochloride (TCH) within 120 min, with a reaction rate constant of 0.0129 min-1. Compared to pristine B-BMO, the degradation rate improved by 10.2%. The composite maintained over 80% degradation efficiency after three consecutive cycles and retained favorable activity after five successive cycles. Sacrificial agent experiments identified superoxide anion radicals (˙O2-) as the dominant reactive species during the degradation process. Liquid chromatography-mass spectrometry (LC-MS) analysis enabled identification of degradation intermediates, leading to the proposal of a plausible TCH degradation pathway. This study provides insights into subsequent non-metallic element doping and heterojunction engineering strategies for BMO-based photocatalysts.

PMID 42723574
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