ArticleThe Journal of general physiology2016
High membrane permeability for melatonin.
Article in The Journal of general physiology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.
What it found
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Who cites it
53 citing papers in PubMed, 90 citations in OpenAlex.
- Circadian rhythm of melatonin receptors under monochromatic light and their regulatory effect on clock genes in the chick liver.Poultry science · 2026Article
- Article
- Upregulated Expression and Shifted Distribution of Melatonin and Its Synthesizing Enzymes From Postnatal to Young Adult Rat Cochleae.Developmental neurobiology · 2025Article
- The roles of melatonin and potassium channels in relaxation response to ang 1-7 in diabetic rat isolated aorta.Cytotechnology · 2025Article
- Lipidomic and Instrumental Evaluation of a Melatonin-Based In & Out Strategy Versus Topical Treatment in Skin Aging: A Randomized Prospective Trial.Metabolites · 2025Article
- Melatonin in Chemo/Radiation Therapy; Implications for Normal Tissues Sparing and Tumor Suppression: An Updated Review.Current medicinal chemistry · 2025Review
- Clinical Studies Using Topical Melatonin.International journal of molecular sciences · 2024Review
- Pharmacokinetic Model-Based Control across the Blood-Brain Barrier for Circadian Entrainment.International journal of molecular sciences · 2023Article
- Melatonin improves behavioral parameters and oxidative stress in zebrafish submitted to a leucine-induced MSUD protocol.Metabolic brain disease · 2023Article
- Why did glutamate, GABA, and melatonin become intercellular signalling molecules in plants?eLife · 2023Review
- Melatonin: Facts, Extrapolations and Clinical Trials.Biomolecules · 2023Review
- Melatonin in Combination with Albendazole or Albendazole Sulfoxide Produces a Synergistic Cytotoxicity against Malignant Glioma Cells through Autophagy and Apoptosis.Brain sciences · 2023Article
- Selective Serotonin Reuptake Inhibitors within Cells: Temporal Resolution in Cytoplasm, Endoplasmic Reticulum, and Membrane.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2023Article
- All the brain's a stage for serotonin: the forgotten story of serotonin diffusion across cell membranes.Proceedings. Biological sciences · 2022Review
- Review
- GPCRs in Intracellular Compartments: New Targets for Drug Discovery.Biomolecules · 2022Review
- Luminogenic HiBiT Peptide-Based NanoBRET Ligand Binding Assays for Melatonin Receptors.ACS pharmacology & translational science · 2022Article
- Seasonal vascular plasticity in the mediobasal hypothalamus of the adult ewe.Histochemistry and cell biology · 2022Article
- Revisiting the role of melatonin in human melanocyte physiology: A skin context perspective.Journal of pineal research · 2022Review
- Free-Energy Simulations Support a Lipophilic Binding Route for Melatonin Receptors.Journal of chemical information and modeling · 2022Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
The pineal gland, an endocrine organ in the brain, synthesizes and secretes the circulating night hormone melatonin throughout the night. The literature states that this hormone is secreted by simple diffusion across the pinealocyte plasma membrane, but a direct quantitative measurement of membrane permeability has not been made. Experiments were designed to compare the cell membrane permeability to three indoleamines: melatonin and its precursors N-acetylserotonin (NAS) and serotonin (5-HT). The three experimental approaches were (1) to measure the concentration of effluxing indoleamines amperometrically in the bath while cells were being dialyzed internally by a patch pipette, (2) to measure the rise of intracellular indoleamine fluorescence as the compound was perfused in the bath, and (3) to measure the rate of quenching of intracellular fura-2 dye fluorescence as indoleamines were perfused in the bath. These measures showed that permeabilities of melatonin and NAS are high (both are uncharged molecules), whereas that for 5-HT (mostly charged) is much lower. Comparisons were made with predictions of solubility-diffusion theory and compounds of known permeability, and a diffusion model was made to simulate all of the measurements. In short, extracellular melatonin equilibrates with the cytoplasm in 3.5 s, has a membrane permeability of ∼1.7 µm/s, and could not be retained in secretory vesicles. Thus, it and NAS will be "secreted" from pineal cells by membrane diffusion. Circumstances are suggested when 5-HT and possibly catecholamines may also appear in the extracellular space passively by membrane diffusion.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.