ArticleArteriosclerosis, thrombosis, and vascular biology2014
Nicotinic acid activates the capsaicin receptor TRPV1: Potential mechanism for cutaneous flushing.
Article in Arteriosclerosis, thrombosis, and vascular biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 42 citations in OpenAlex.
- TRPV1 deletion in male mice alters cardiomyocyte ultrastructure without affecting baseline cardiac function.Scientific reports · 2025Article
- Topical Steroid Withdrawal Is a Targetable Excess of Mitochondrial NAD.The Journal of investigative dermatology · 2025Article
- Diverse Physiological Roles of Kynurenine Pathway Metabolites: Updated Implications for Health and Disease.Metabolites · 2025Review
- The Promise of Niacin in Neurology.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2023Review
- Profile of precipitating factors and its implication in 160 Indian patients with Moyamoya angiopathy.Journal of neurology · 2023Observational
- A molecular perspective on identifying TRPV1 thermosensitive regions and disentangling polymodal activation.Temperature (Austin, Tex.) · 2023Review
- pH-Responsive Inorganic/Organic Nanohybrids System for Controlled Nicotinic Acid Drug Release.Molecules (Basel, Switzerland) · 2022Article
- Lipid-dependent sequential allosteric activation of heat-sensing TRPV1 channels by anchor-stereoselective "hot" vanilloid compounds and analogs.Biochemistry and biophysics reports · 2021Review
- A Luminescence-Based Human TRPV1 Assay System for Quantifying Pungency in Spicy Foods.Foods (Basel, Switzerland) · 2021Article
- Nicotinic acid suppresses sebaceous lipogenesis of human sebocytes via activating hydroxycarboxylic acid receptor 2 (HCAJournal of cellular and molecular medicine · 2019Article
- Nicotinic acid impairs assembly of leading edge in glioma cells.Oncology reports · 2017Article
- Measuring niacin-associated skin toxicity (NASTy) stigmata along with symptoms to aid development of niacin mimetics.Journal of lipid research · 2017Article
- Nicotinic acid inhibits glioma invasion by facilitating Snail1 degradation.Scientific reports · 2017Article
- Nicotinamide is an endogenous agonist for a C. elegans TRPV OSM-9 and OCR-4 channel.Nature communications · 2016Article
- Nicotinic acid is a common regulator of heat-sensing TRPV1-4 ion channels.Scientific reports · 2015Article
- TRPV1 channels are involved in niacin-induced cutaneous vasodilation in mice.Journal of cardiovascular pharmacology · 2015Article
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
objectiveNicotinic acid (also known as niacin or vitamin B3), widely used to treat dyslipidemias, represents an effective and safe means to reduce the risk of mortality from cardiovascular disease. Nonetheless, a substantial fraction of patients discontinue treatment because of a strong side effect of cutaneous vasodilation, commonly termed flushing. In the present study, we tested the hypothesis that nicotinic acid causes flushing partially by activating the capsaicin receptor TRPV1, a polymodal cellular sensor that mediates the flushing response on consumption of spicy food. APPROACH AND
resultsWe observed that the nicotinic acid-induced increase in blood flow was substantially reduced in Trpv1(-/-) knockout mice, indicating involvement of the channel in flushing response. Using exogenously expressed TRPV1, we confirmed that nicotinic acid at submillimolar to millimolar concentrations directly and potently activates TRPV1 from the intracellular side. Binding of nicotinic acid to TRPV1 lowers its activation threshold for heat, causing channel opening at physiological temperatures. The activation of TRPV1 by voltage or ligands (capsaicin and 2-aminoethoxydiphenyl borate) is also potentiated by nicotinic acid. We further demonstrated that nicotinic acid does not compete directly with capsaicin but may activate TRPV1 through the 2-aminoethoxydiphenyl borate activation pathway. Using live-cell fluorescence imaging, we observed that nicotinic acid can quickly enter the cell through a transporter-mediated pathway to activate TRPV1.
conclusionsDirect activation of TRPV1 by nicotinic acid may lead to cutaneous vasodilation that contributes to flushing, suggesting a potential novel pathway to inhibit flushing and to improve compliance.
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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 OpenQuestion graph.