Nicotinic acid is a common regulator of heat-sensing TRPV1-4 ion channels

Ma, Linlin, Lee, Bo Hyun, Clifton, Heather, Schaefer, Saul and Zheng, Jie (2015) Nicotinic acid is a common regulator of heat-sensing TRPV1-4 ion channels. Scientific Reports, 5 Art No.: 8906: . doi:10.1038/srep08906

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Author Ma, Linlin
Lee, Bo Hyun
Clifton, Heather
Schaefer, Saul
Zheng, Jie
Title Nicotinic acid is a common regulator of heat-sensing TRPV1-4 ion channels
Journal name Scientific Reports   Check publisher's open access policy
ISSN 2045-2322
Publication date 2015
Year available 2015
Sub-type Article (original research)
DOI 10.1038/srep08906
Open Access Status DOI
Volume 5
Issue Art No.: 8906
Total pages 8
Place of publication London United Kingdom
Publisher Nature Publishing Group
Collection year 2016
Language eng
Formatted abstract
Nicotinic acid (NA, a.k.a. vitamin B3 or niacin) can reduce blood cholesterol and low-density lipoproteins whereas increase high-density lipoproteins. However, when NA is used to treat dyslipidemias, it causes a strong side effect of cutaneous vasodilation, commonly called flushing. A recent study showed that NA may cause flushing by lowering activation threshold temperature of the heat-sensitive capsaicin receptor TRPV1 ion channel, leading to its activation at body temperature. The finding calls into question whether NA might also interact with the homologous heat-sensitive TRPV2–4 channels, particularly given that TRPV3 and TRPV4 are abundantly expressed in keratinocytes of the skin where much of the flushing response occurs. We found that NA indeed potentiated TRPV3 while inhibited TRPV2 and TRPV4. Consistent with these gating effects, NA lowered the heat-activation threshold of TRPV3 but elevated that of TRPV4. We further found that activity of TRPV1 was substantially prolonged by extracellular NA, which may further enhance the direct activation effect. Consistent with the broad gating effect on TRPV1–4 channels, evidence from the present study hints that NA may share the same activation pathway as 2-aminoethoxydiphenyl borate (2-APB), a common agonist for these TRPV channels. These findings shed new light on the molecular mechanism underlying NA regulation of TRPV channels
Keyword Vasodilation
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2016 Collection
Institute for Molecular Bioscience - Publications
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