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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
来源： ClinicalTrials.gov, Clinigen Group

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

PubMedJournal of pineal research2026-09-10

Melatonin Inhibits Metastasis of Sunitinib-Resistant Renal Cell Carcinoma Cells Via the GRP78/p38/CTSD Expression.

Huang Po-Yu PY, Hsieh Yi-Hsien YH, Chen Yong-Syuan YS, Hung Tung-Wei TW et al.

Sunitinib resistance contributes to poor outcomes in advanced renal cell carcinoma (RCC). This study investigated the anti-metastatic effects and underlying mechanisms of melatonin in sunitinib-resistant (SR)-RCC. Melatonin significantly inhibited the migration and invasion of A498-SR and Caki-1-SR cells. SR-RCC cells exhibited elevated CTSD expression, impaired endoplasmic reticulum (ER) stress signaling with reduced GRP78 and IRE1α, and enhanced p38 MAPK activation, all of which were reversed by melatonin. Silencing p38 MAPK further potentiated the inhibitory effects of melatonin on cell migration and invasion. Mechanistically, CTSD expression was regulated through both GRP78/p38 MAPK-mediated ER stress. In vivo, melatonin markedly reduced lung metastasis of Caki-1-SR cells without causing significant toxicity to major organs. Collectively, these findings demonstrate that melatonin inhibited the metastatic potential of SR-RCC by decreasing CTSD expression, restoring ER stress response, and decreasing p38 MAPK expression, supporting its potential as an anti-metastatic therapeutic agent for SR-RCC.

PMID 42720349
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PubMedFrontiers in plant science2026-09-10

Melatonin-mediated alleviation of salinity stress in diverse mango (Mangifera indica L.) rootstock genotypes.

Kumari Ishu I, Prakash Jai J, Singh Kanhaiya K, Awasthi Om Prakash OP et al.

Mango (Mangifera indica L.), a tropical fruit crop with significant commercial value, is particularly vulnerable to salt stress. Salinity exposure causes severe physiological disruptions, including leaf burning, chlorosis, and stunted growth, especially in the early phases of plant development, and can be mitigated by salt tolerance. The current study evaluated the effectiveness of exogenous melatonin in mitigating salinity stress at 60 mM NaCl. The findings showed that applying melatonin at an optimal level of 150 μM improved photosynthetic efficiency, relative water content, and membrane stability index, thereby enhancing plant performance. Furthermore, melatonin treatment significantly reduced the build-up of malondialdehyde, a marker of membrane lipid peroxidation, while maintaining increased levels of phenol, proline, and total sugars. Increased activity of superoxide dismutase, catalase, peroxidase, and ascorbate peroxidase enzymes, which together reduced oxidative stress, indicated a stronger antioxidant defense system, strongly linked to enhanced tolerance. Correlation analysis further revealed strong positive relationships among physiological and biochemical parameters, whereas malondialdehyde exhibited negative correlations with all other traits. Also, principal component analysis of six rootstock genotypes under salinity showed that melatonin enhanced stress tolerance in Kurukkan, K 106, and Olour by boosting antioxidant enzymes and preserving photosynthetic pigments. Overall, our findings demonstrate that melatonin increases mango rootstock resilience in saline environments by preserving cellular stability and regulating redox equilibrium.

PMID 42718990
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PubMedJournal of biological rhythms2026-09-10

The Circadian System and Chronic Kidney Disease Risk: Epidemiological Evidence.

Zhang Jing J, Thien Tran Dat D, El Ghoul Tala T, Żebrowska Magdalena M et al.

Chronic kidney disease (CKD) affects roughly 10% of the world's population, and growing evidence suggests that disruption of the circadian system-now recognized as an important regulator of numerous physiological pathways, may contribute to impaired kidney function and increased CKD risk. This narrative review aims to synthesize the existing literature on the association between determinants of circadian rhythm (shift work, artificial light at night [ALAN], melatonin) as well as sleep health and CKD risk. Three databases (PubMed, Web of Science, and Embase) were searched for original articles published from 1966 through 28 February 2026. A total of 34 studies examined the association between circadian factors and CKD risk: 7 on shift work, 2 on ALAN, 4 on melatonin, 4 on chronotype, 2 on social jetlag, 2 on insomnia, and 18 on sleep duration. Taken together, these studies offer consistent evidence that shift work, evening chronotype, prolonged social jetlag, and both short and long sleep duration are associated with elevated CKD risk. Given the potential implications for early detection, risk stratification, and targeted behavioral interventions, future research should employ standardized approaches and improved measures using, for example, actigraphy, to clarify causal pathways and strengthen the evidence base.

PMID 42717437
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PubMedPhysiologia plantarum2026-09-10

CaCl2 Priming Boosts Salinity-Alkalinity Tolerance in Germinating Soybean by Reducing DNA Oxidative Damage and Enhancing Ca2+ -ROS Signaling Crosstalk.

Sun Ran R, Zhao Qiang Q, Wang Weiyu W, Yao Yuan Y et al.

Soybean (Glycine max) seed germination is highly sensitive to saline-alkaline stress. Seed priming represents an effective strategy to mitigate its detrimental effects. However, the optimal priming conditions (agent, concentration, duration) and the underlying molecular mechanisms remain poorly understood. This study investigated the effects of priming with distilled water (Control), calcium chloride (CaCl2), melatonin (MT), and proline (Pro) under saline-alkaline stress on soybean seed germination and the molecular basis of enhanced tolerance. Evaluation of ten germination-related parameters revealed that priming with 100 mM CaCl2 for 12 h significantly enhanced the germination rate. Physiological analyses demonstrated that CaCl2 priming effectively reduced reactive oxygen species (ROS) accumulation by increasing the activities of superoxide dismutase (SOD), peroxidase (POD), and catalase (CAT), while decreasing malondialdehyde (MDA) content. Furthermore, CaCl2 priming activated the Ca2+ signaling pathway by increasing radicle Ca2+ content and upregulating the expression levels of Ca2+ signaling-related genes (e.g., GmCAM7, GmCNGC2, GmCNGC19, GmMPK2, and GmMKK2). Additionally, CaCl2 priming significantly enhanced DNA damage repair capacity of soybean cultivars with differing saline-alkaline tolerance. This was manifested by reduced DNA oxidative damage and decreased random amplified polymorphic DNA (RAPD) polymorphism, thereby enhancing genomic stability and alleviating cell cycle arrest. These findings deepen our understanding of the complex regulatory role of calcium signaling in plant abiotic stress responses and provide important novel theoretical insights for improving crop resilience.

PMID 42717712
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PubMedACS sensors2026-09-09

Structure-Switching Aptamer-Based Molecular Pendulum for Profiling Melatonin Circadian Dynamics in Humans.

Riordan Kimberly T KT, Brazelton Ethan E, Nashner Audrey A, Juska Vuslat V et al.

Continuous electrochemical monitoring of small molecules remains difficult due to their small size and lack of enzymatic sensing strategies. Here, we develop a structure-switching aptamer molecular pendulum platform for reagentless electrochemical detection of small molecules, including melatonin and cortisol. Target binding induces a conformational change in the receptor, which increases the hydrodynamic diameter of the construct, thereby slowing electron transfer kinetics and resulting in a measurable time-resolved electrochemical current. To explore the feasibility of melatonin sensing in vivo, we validated the presence and circadian dynamics of melatonin in human interstitial fluid using mass spectrometry. We then demonstrated quantitative electrochemical detection of melatonin directly in human ISF, with signals that mirror the circadian profile observed by mass spectrometry. This work provides a foundation for continuous, minimally invasive monitoring of circadian biomarkers using electrochemical sensors.

PMID 42712226
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PubMedIndian journal of cancer2026-09-09

Effect of oral melatonin on sleep quality, fatigue, and caregiver sleep perception in patients with head and neck cancer: A randomized double-blind placebo-controlled trial.

Pushpa, Dayal Madhu M, Khandelwal Sakshi S, Khandelwal Rohan R et al.

Sleep disturbances and fatigue are common in patients with head and neck cancer and adversely affect quality of life. Melatonin may improve sleep quality with minimal adverse effects. This study evaluated the effect of oral melatonin on sleep quality, fatigue, and caregiver sleep perception in patients with head and neck cancer. In this prospective, randomised, placebo-controlled trial, 70 patients aged 18-65 years with head and neck cancer and sleep disturbances for >1 month were randomised to oral melatonin 3 mg (Group M, n = 35) or multivitamin (placebo) (Group P, n = 35) once daily for 14 days. Pittsburgh sleep quality index (PSQI), fatigue assessment scale (FAS), and satisfaction, alertness, timing, efficiency, and duration scores were assessed at baseline and day 14. Day-14 PSQI scores were lower in Group M than Group P (8.11 ± 1.55 versus 9.66 ± 1.83; P = 0.0003), with significant improvement only in Group M ( P < 0.001). FAS scores were also lower in Group M (12.66 ± 2.44 versus 14.69 ± 1.94; P = 0.0003). Caregiver sleep perception improved significantly with melatonin ( P < 0.0001). Oral melatonin improved sleep quality and reduced fatigue in patients with head and neck cancer and was associated with better caregiver sleep perception.

PMID 42714195
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