H89 dihydrochloride hydrate and calphostin C lower the body temperature through TRPV1

Bao,Dongyan; Zhao,Wenqing; Dai,Congcong; Wan,Hongmei; Cao,Yu

doi:10.3892/mmr.2017.8078

H89 dihydrochloride hydrate and calphostin C lower the body temperature through TRPV1

Authors:
- Dongyan Bao
- Wenqing Zhao
- Congcong Dai
- Hongmei Wan
- Yu Cao
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Affiliations: Department of Physiology, China Medical University, Shenyang, Liaoning 110000, P.R. China
Published online on: November 15, 2017 https://doi.org/10.3892/mmr.2017.8078
Pages: 1599-1608
Copyright: © Bao et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

The transient receptor potential vanilloid (TRPV1) serves as a negative regulator of body temperature, and during fever conditions its expression can lead to a decrease in temperature. TRPV1 is regulated by a variety of enzymes; however, it is currently unclear whether the regulation of TRPV1 phosphorylation may serve a role in the increase in TRPV1 expression during fever. In the present study, using an in vivo experimental method, rat brain ventricles were injected with the protein kinase A (PKA) antagonist, H89, and the protein kinase C (PKC) antagonist, calphostin C, and fever was induced using lipopolysaccharide (LPS) in order to detect the expression of TRPV1 and phosphorylated (p‑)TRPV1, the intracellular Ca2+ concentration [(Ca2+)i] of hypothalami and rat body temperature. The results demonstrated that following the generation of fever using LPS, the expressions of TRPV1 and p‑TRPV1, and hypothalamic [Ca2+]i markedly increased. In addition, following an injection with the PKA or PKC antagonist, the temperature increased further due to the inhibition of p‑TRPV1. Thus, it was hypothesized that PKA and PKC may be involved in TRPV1 phosphorylation, resulting in a temperature reduction during LPS‑induced fever conditions.

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