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Modulation of human TRPV1 receptor activity by extracellular protons and host cell expression system.
Eur J Pharmacol. 2006 May 10; 537(1-3):20-30.EJ

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.

Authors+Show Affiliations

Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. bruce.bianchi@abbott.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

16630609

Citation

Bianchi, Bruce R., et al. "Modulation of Human TRPV1 Receptor Activity By Extracellular Protons and Host Cell Expression System." European Journal of Pharmacology, vol. 537, no. 1-3, 2006, pp. 20-30.
Bianchi BR, Lee CH, Jarvis MF, et al. Modulation of human TRPV1 receptor activity by extracellular protons and host cell expression system. Eur J Pharmacol. 2006;537(1-3):20-30.
Bianchi, B. R., Lee, C. H., Jarvis, M. F., El Kouhen, R., Moreland, R. B., Faltynek, C. R., & Puttfarcken, P. S. (2006). Modulation of human TRPV1 receptor activity by extracellular protons and host cell expression system. European Journal of Pharmacology, 537(1-3), 20-30.
Bianchi BR, et al. Modulation of Human TRPV1 Receptor Activity By Extracellular Protons and Host Cell Expression System. Eur J Pharmacol. 2006 May 10;537(1-3):20-30. PubMed PMID: 16630609.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Modulation of human TRPV1 receptor activity by extracellular protons and host cell expression system. AU - Bianchi,Bruce R, AU - Lee,Chih-Hung, AU - Jarvis,Michael F, AU - El Kouhen,Rachid, AU - Moreland,Robert B, AU - Faltynek,Connie R, AU - Puttfarcken,Pamela S, Y1 - 2006/03/10/ PY - 2005/11/21/received PY - 2006/02/28/revised PY - 2006/03/06/accepted PY - 2006/4/25/pubmed PY - 2006/8/12/medline PY - 2006/4/25/entrez SP - 20 EP - 30 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 537 IS - 1-3 N2 - 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. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/16630609/Modulation_of_human_TRPV1_receptor_activity_by_extracellular_protons_and_host_cell_expression_system_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(06)00240-8 DB - PRIME DP - Unbound Medicine ER -