Journal article
Expression-dependent pharmacology of transient receptor potential vanilloid subtype 1 channels in Xenopus laevis oocytes
Channels (Austin, Tex.), Vol.7(1), pp.47-50
01/01/2013
DOI: 10.4161/chan.23105
PMCID: PMC3589282
PMID: 23428812
Abstract
Transient receptor potential vanilloid subfamily member 1 channels are polymodal sensors of noxious stimuli and integral players in thermosensation, inflammation and pain signaling. It has been shown previously that under prolonged stimulation, these channels show dynamic pore dilation, providing a pathway for large and otherwise relatively impermeant molecules. Further, we have shown recently that these nonselective cation channels, when activated by capsaicin, are potently and reversibly blocked by external application of quaternary ammonium compounds and local anesthetics. Here we describe a novel phenomenon in transient receptor potential channel pharmacology whereby their expression levels in
Xenopus laevis
oocytes, as assessed by the magnitude of macroscopic currents, are negatively correlated with extracellular blocker affinity: small current densities give rise to nanomolar blockade by quaternary ammoniums and this affinity decreases linearly as current density increases. Possible mechanisms to explain these data are discussed in light of similar observations in other channels and receptors.
Details
- Title: Subtitle
- Expression-dependent pharmacology of transient receptor potential vanilloid subtype 1 channels in Xenopus laevis oocytes
- Creators
- Ricardo E Rivera-Acevedo - Department of Anesthesiology, Pharmacology & Therapeutics; The University of British Columbia; Vancouver, BC CanadaStephan A Pless - Department of Anesthesiology, Pharmacology & Therapeutics; The University of British Columbia; Vancouver, BC CanadaStephan K.W Schwarz - Department of Anesthesiology, Pharmacology & Therapeutics; The University of British Columbia; Vancouver, BC CanadaChristopher A Ahern - Department of Anesthesiology, Pharmacology & Therapeutics; The University of British Columbia; Vancouver, BC Canada
- Resource Type
- Journal article
- Publication Details
- Channels (Austin, Tex.), Vol.7(1), pp.47-50
- Publisher
- Landes Bioscience
- DOI
- 10.4161/chan.23105
- PMID
- 23428812
- PMCID
- PMC3589282
- ISSN
- 1933-6950
- eISSN
- 1933-6969
- Language
- English
- Date published
- 01/01/2013
- Academic Unit
- Molecular Physiology and Biophysics; Iowa Neuroscience Institute
- Record Identifier
- 9984070821102771
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