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Transient receptor potential vanilloid-1-mediated calcium responses are inhibited by the alkylamine antihistamines dexbrompheniramine and chlorpheniramine

Sadofsky, Laura R.; Sadofsky, Laura; Campi, Barbara; Morice, Alyn; Trevisani, Marcello; Compton, Steven J.; Morice, Alyn H.

Authors

Barbara Campi

Marcello Trevisani

Steven J. Compton



Abstract

American guidelines, unlike European guidelines, support the use of antihistamines as a first line of treatment for some causes of chronic cough. Transient receptor potential vanilloid-1 (TRPV1) is an ion channel activated by the tussive agents capsaicin, resiniferatoxin, and protons. It is predominantly expressed by C-fiber and some Aδ-fiber sensory neurons and is thought to be a cough receptor. By measuring increases in intracellular calcium as an indicator of TRPV1 activation, the authors sought to determine whether antihistamines could antagonise TRPV1 permanently expressed in HEK and Pro5 cells and TRPV1 endogenously expressed in rat dorsal root ganglia neurons. In human TRPV1-expressing HEK cells (hTRPV1-HEK), diphenhydramine and fexofenadine failed to inhibit capsaicin-triggered calcium responses. However, both dexbrompheniramine and chlorpheniramine significantly inhibited capsaicin-evoked responses in hTRPV1-HEK. Dexbrompheniramine also inhibited activation of rat TRPV1 expressed in HEK and Pro5 cells, without interfering with TRPA1 and proteinase-activated receptor-2 (PAR2) activation. Finally, in rat dorsal root ganglia neuron preparations, dexbrompheniramine dose-dependently inhibited capsaicin-evoked calcium responses. Thus, the inhibition of TRPV1 activation by dexbrompheniramine may provide one potential mechanism whereby this antihistamine exerts its therapeutic effect in chronic cough. Copyright © Informa Healthcare USA, Inc.

Citation

Sadofsky, L. R., Campi, B., Trevisani, M., Compton, S. J., & Morice, A. H. (2008). Transient receptor potential vanilloid-1-mediated calcium responses are inhibited by the alkylamine antihistamines dexbrompheniramine and chlorpheniramine. Experimental Lung Research, 34(10), 681-693. https://doi.org/10.1080/01902140802339623

Journal Article Type Article
Acceptance Date Jul 11, 2008
Online Publication Date Jul 2, 2009
Publication Date Dec 31, 2008
Publicly Available Date Mar 29, 2024
Journal EXPERIMENTAL LUNG RESEARCH
Print ISSN 0190-2148
Electronic ISSN 1521-0499
Publisher Taylor and Francis
Peer Reviewed Peer Reviewed
Volume 34
Issue 10
Pages 681-693
DOI https://doi.org/10.1080/01902140802339623
Keywords TRPV1; Antihistamines; Dexbrompheniramine; Chlorpheniramine; Dipheniramine; Fexofenadine
Public URL https://hull-repository.worktribe.com/output/396235