Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-3
pubmed:dateCreated
2006-5-8
pubmed:abstractText
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
10
pubmed:volume
537
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
20-30
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Modulation of human TRPV1 receptor activity by extracellular protons and host cell expression system.
pubmed:affiliation
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. bruce.bianchi@abbott.com
pubmed:publicationType
Journal Article, Comparative Study