Modulation of human TRPV1 receptor activity by extracellular protons and host cell expression system

European Journal of Pharmacology
Bruce R BianchiPamela S Puttfarcken

Abstract

The transient receptor potential vanilloid 1 (TRPV1) receptor is a ligand-gated cation channel that can be activated by capsaicin, heat, protons and cytosolic lipids. We compared activation of recombinant human TRPV1 receptors stably expressed in human 293 cells, derived from kidney embryonic cells, and in human 1321N1 cells, derived from brain astrocytes. Cellular influx of calcium was measured in response to acid, endovanilloids (N-arachidonoyl-dopamine, N-oleoyl-dopamine and anandamide), capsaicin and other traditional vanilloid agonists under normal (pH 7.4) and acidic (pH 6.7 and 6.0) assay conditions. The host cell expression system altered the agonist profile of endogenous TRPV1 receptor agonists without affecting the pharmacological profile of either exogenous TRPV1 receptor agonists or antagonists. Our data signify that the host cell expression system plays a modulatory role in TRPV1 receptor activity, and suggests that activation of native human TRPV1 receptors in vivo will be dependent on cell-specific regulatory factors/pathways.

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Citations

Oct 7, 2010·Pflügers Archiv : European journal of physiology·Maxime G Blanchard, Stephan Kellenberger
Nov 3, 2009·European Journal of Pharmacology·Jun Peng, Yuan-Jian Li
Aug 30, 2008·European Journal of Pharmacology·Heath A McDonaldPamela S Puttfarcken
Mar 14, 2007·Pharmacology & Therapeutics·Katarzyna StarowiczVincenzo Di Marzo
Aug 5, 2015·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Éva SághyJános Szolcsányi
Sep 25, 2014·Journal of Neuroscience Research·Kevin P CarlinVictor I Ilyin
Aug 6, 2010·Biological & Pharmaceutical Bulletin·Susumu OhkawaraHideto Jinno
Jun 11, 2009·Anesthesiology·Sinyoung Kang, Timothy J Brennan
May 1, 2021·International Journal of Molecular Sciences·Marina Ramal-SanchezBarbara Barboni

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