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melatonin

✓ Approved

Clinigen Group · MTNR1A · 小分子

什么是 melatonin?

melatonin 是一种小分子,由Clinigen Group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

公司Clinigen Group
药物类别小分子
分子靶点MTNR1A, MTNR1B
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

melatonin 作用于 2 个分子靶点:

MTNR1Amelatonin receptor 1A (MEL-1A-R, MT1)
MTNR1Bmelatonin receptor 1B (FGQTL2, MT2)
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

melatonin 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 disordersInsomnia✓ Approved
Psychiatric disordersSleep disorder✓ Approved

相关研究文献

PubMedBulletin of experimental biology and medicine2026-07-27

Melatonin Amplitude, but Not Phase, Is Associated with Sleep Efficiency in the Arctic.

Gubin D G DG, Kolomeychuk S N SN, Petrov I M IM, Markov A A AA et al.

This study investigated the relationship between the amplitude and phase of melatonin rhythm and sleep efficiency in 15 Arctic residents, accounting for the pronounced seasonal variations in the photic environment. Sleep efficiency was assessed using actigraphy across the winter and summer solstices, and the spring equinox. Analysis revealed no significant seasonal variations in sleep efficiency (p > 0.05). Multiple regression analysis, after adjusting for photoperiod, demonstrated a significant positive association between the melatonin amplitude and sleep efficiency (β = 0.317, p < 0.037, η2 = 0.10). Melatonin phase parameters (acrophase or dim light melatonin onset (DLMO)) had no significant relationship with sleep efficiency (p > 0.3). These findings suggest that melatonin amplitude plays a dominant role in determining sleep quality, and substantiate the potential efficacy of interventions aimed at augmenting melatonin rhythm amplitude.

PMID 42507091
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PubMedJournal of biological rhythms2026-07-27

Variable Morning Melatonin Profiles Limit Determination of Dim-Light Melatonin Offset in Preschool-Aged Children.

Hartstein Lauren E LE, Stowe Shelby R SR, Wright Kenneth P KP, Diniz Behn Cecilia C et al.

Circadian rhythms have been shown to regulate sleep-wake timing across the lifespan, yet many questions remain about early childhood circadian physiology. Understanding dim-light melatonin onset (DLMO) and offset (DLMOff), established markers of circadian phase, is essential for characterizing circadian rhythms in early childhood. We examined the distribution of salivary DLMO and DLMOff and their relationship with actigraphic sleep timing across 20 healthy preschoolers (M = 4.31 ± 0.34 years, 45% female). After maintaining a consistent sleep schedule for 7 days, children completed an in-home circadian assessment. Children were awoken 1.5 h before habitual wake time, and saliva samples were collected in 20- to 30-min intervals throughout the morning to determine DLMOff, then in the evening until 50 min past habitual bedtime to assess DLMO. A 4-pg/ml threshold was used to calculate each phase marker. DLMO ranged from 17:22 to 20:40 (M = 18:55 ± 0:54) and was positively associated with bedtime, sleep onset, and midsleep. In contrast, morning melatonin levels were highly variable, allowing DLMOff calculation in only 8 participants. Within this small subsample, later DLMOff was associated with later chronotype (r = 0.81), sleep offset (r = 0.84), and midsleep (r = 0.80). Across the full sample, interpolated melatonin levels at habitual wake remained ≥ 4 pg/ml for 45% of children, a pattern broadly consistent with findings in adults, in which a majority of participants exhibit DLMOff after habitual wake time. These findings indicate that although evening melatonin profiles were consistently well-defined, permitting reliable calculations of DLMO across all participants, morning melatonin patterns were often irregular in young children. When able to be calculated, DLMOff showed strong associations with sleep timing, suggesting it could be a reliable marker of circadian phase. However, high variability and fluctuating morning melatonin patterns make DLMOff difficult to determine in many preschool-aged children.

PMID 42504584
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PubMedBiomacromolecules2026-07-27

Supramolecular Nano-Assembly of Melatonin-Conjugated Peptide as a Multifunctional Scaffold for Wound Healing Applications.

Bundel Pruthviraj P, Shounak Pranjit P, Vashisth Ankit A, Singh Yashveer Y

Wounds are one of the major socioeconomic challenges globally, mainly arising from trauma, surgery, burns, and infections. In many cases, prolonged recovery time leads to complications and requires a multifunctional approach that can target tissue regeneration and prevents infection. The supramolecular assembly of peptides yield well-defined nanoassemblies that resemble the extracellular matrix and influence cellular interactions. The peptide-based systems allow structural fine-tuning, high biocompatibility, and the ability to incorporate bioactive signals. Despite advances in peptide-based supramolecular gels for wound treatment, multifunctional peptide-based scaffolds remain relatively unexplored. In this work, we have designed a melatonin-conjugated amphiphilic peptide that self-assembles into a viscoelastic, nanofibrous gel with antibacterial and wound-healing functions. The amphiphilic nanofibers effectively disrupted bacterial membranes, and conjugated melatonin enhanced the antioxidant activity and promoted M1 to M2 macrophage polarization. The structural and biological properties of the self-assembled gel provide a promising multifunctional platform for wound management.

PMID 42503848
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PubMedMetabolites2026-07-27

Correction: Holtkamp et al. Ultraviolet Radiation-Induced Mitochondrial Disturbances Are Attenuated by Metabolites of Melatonin in Human Epidermal Keratinocytes. Metabolites 2023, 13, 861.

Holtkamp Chantal E CE, Warmus Dawid D, Bonowicz Klaudia K, Gagat Maciej M et al.

Error in Figure [...].

PMID 42506468
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PubMedInternational journal of biological macromolecules2026-07-27

Chitosan-melatonin nanobiopolymer regulates miR398-mediated antioxidant defense and TaHKT1;5-SOS-NHX ion-homeostasis networks to enhance wheat salt tolerance.

Algopishi Uthman Balgith UB, Alshegaihi Rana M RM, Khan M Nasir MN, Fayad Eman E et al.

In recent years, the application of nanobiomaterials and phytohormone-based nano-delivery systems has gained considerable attention for enhancing plant tolerance to abiotic stresses. Among these approaches, melatonin (MLT) and chitosan nanoparticles (CS-NPs) have emerged as promising biostimulants due to their ability to regulate antioxidant defense systems, ion homeostasis, photosynthetic performance, and stress-responsive molecular networks. Although the individual effects of MLT and CS-NPs on stress mitigation have been investigated in different crop species, their combined application through a nanobiopolymer delivery system and its influence on microRNA-mediated antioxidant regulation and ion-homeostasis pathways under salinity stress remain insufficiently explored. Therefore, the present study was conducted to evaluate the effectiveness of melatonin-loaded chitosan nanoparticles (MLT-CSNPs) in improving salt tolerance in wheat (Triticum aestivum L.) exposed to 100 mM NaCl. T. aestivum plants were treated with free MLT, CS-NPs, and MLT-CSNPs, where T7 represented NaCl + MLT-CSNPs equivalent to 100 μM melatonin. Our results demonstrated that salt stress significantly reduced plant growth and biomass, photosynthetic pigments, gas exchange characteristics, and ionic balance in T. aestivum plants. Moreover, salinity markedly increased Na+ accumulation, the Na+/K+ ratio, oxidative stress biomarkers, and cellular damage. However, the application of MLT-CSNPs significantly improved plant growth, photosynthetic efficiency, antioxidant defense, osmolyte accumulation, and ion homeostasis under saline conditions. In particular, T7 enhanced plant height and shoot dry weight by 40.6% and 85.5%, respectively, compared with salt-stressed plants. Likewise, total chlorophyll content and photosynthetic rate increased by 79.6% and 95.1%, respectively, indicating substantial protection of the photosynthetic machinery. Furthermore, MLT-CSNP treatment decreased Na+ accumulation by 56.5% and reduced the Na+/K+ ratio to 0.38 compared with 2.01 in salt-stressed plants. In addition, T7 markedly reduced H₂O₂ and MDA contents by 59.8% and 56.6%, respectively, while significantly enhancing the activities of SOD, CAT, POD, and APX. Molecular investigations further revealed that MLT-CSNPs strongly upregulated TaHKT1;5, TaSOS1, TaNHX1, antioxidant-related genes, and miR398 expression, suggesting coordinated regulation of ion exclusion, intracellular ion compartmentalization, and microRNA-mediated antioxidant defense mechanisms. These findings provide new insights into the role of MLT-CSNPs nano-delivery systems in modulating TaHKT1;5-SOS-NHX ion-homeostasis networks and miR398-associated antioxidant responses under salinity stress. Overall, MLT-CSNPs represent a sustainable and efficient nano-biostimulant strategy for enhancing T. aestivum resilience and productivity in saline environments.

PMID 42503381
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PubMedCureus2026-07-27

Impact of Core Circadian Gene Variants on Glycemic Parameters and Insulin Resistance in Type 2 Diabetes: A Systematic Review.

Mokhtar Osman Alaa Fathelrahman AF, Taha Ezdehar E, Hamid Mohammed Islam Mustafa IM, Bakriy Mohamed Najwa Mohamed NM et al.

Circadian rhythm disruption is increasingly implicated in the pathophysiology of type 2 diabetes mellitus (T2DM). Variants in core circadian clock genes - CLOCK (circadian locomotor output cycles kaput), BMAL1/ARNTL (brain and muscle ARNT-like protein 1), CRY1/2 (cryptochrome 1 and 2), PER1-3 (period 1-3), and NR1D1 (REV-ERBα) - and associated melatonin receptor genes may influence glycaemic homeostasis and insulin resistance. This systematic review synthesises evidence published between 2020 and 2025 on associations between these variants and key glycaemic parameters. A systematic search of PubMed/MEDLINE, Embase, Web of Science, and the Cochrane Library was performed following PRISMA 2020 (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines. Studies published from January 2020 to December 2025 that examined circadian gene variants or expression in T2DM or at-risk human populations and reported glycaemic or insulin-resistance outcomes were included. Risk of bias was independently assessed using the Newcastle-Ottawa Scale (NOS). Owing to substantial heterogeneity, a narrative synthesis following the Synthesis Without Meta-analysis (SWiM) framework was undertaken; no meta-analysis, formal heterogeneity (I²) metric, or GRADE certainty rating was performed. Six studies of diverse design (case control, cross-sectional, narrative review, and systematic review with meta-analysis) from China, South Africa, Croatia/multi-ethnic, and Spain, collectively involving more than 18,000 participants, met the inclusion criteria. A CLOCK rs1801260 × MTNR1A rs2119882 gene-gene interaction, CRY2 rs11605924, and BMAL1 rs3789327 were significantly associated with elevated fasting plasma glucose (FPG), higher Homeostatic Model Assessment of Insulin Resistance (HOMA-IR), and increased T2DM risk. Reduced expression of core clock genes (BMAL1, CRY1, and PER2) correlated negatively with glycated haemoglobin (HbA1c) and HOMA-IR. BMAL1 rs7950226 was confirmed as a metabolic-syndrome susceptibility variant. Across 2020-2025, circadian gene variants were consistently associated with impaired glycaemic control and insulin resistance in T2DM. Because the available evidence is observational and heterogeneous, these findings suggest potential value in incorporating circadian genetic profiling into precision diabetes risk stratification rather than established causal utility, and prospective validation is required.

PMID 42504374
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