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Selective Activation of hTRPV1 by N-Geranyl Cyclopropylcarboxamide, an Amiloride-Insensitive Salt Taste Enhancer
- Selective Activation of hTRPV1 by N-Geranyl Cyclopropylcarboxamide, an Amiloride-Insensitive Salt Taste Enhancer
- Kim, MJ[Kim, Min Jung]; Son, HJ[Son, Hee Jin]; Kim, Y[Kim, Yiseul]; Kweon, HJ[Kweon, Hae-Jin]; Suh, BC[Suh, Byung-Chang]; Lyall, V[Lyall, Vijay]; Rhyu, MR[Rhyu, Mee-Ra]
- DGIST Authors
- Kweon, HJ[Kweon, Hae-Jin]; Suh, BC[Suh, Byung-Chang]
- Issue Date
- PLoS ONE, 9(2)
- Article Type
- Acid-Sensing Ion Channel; Acid-Sensing Ion Channels; Amide; Amides; Amiloride; ASIC1 Protein, Human; Benzamil; Calcium Channel; Calcium Channels; Calcium Transport; Capsazepine; Cell Culture; Chemical Structure; Concentration Response; Controlled Study; Drug Effects; Epithelial Sodium Channel; Epithelial Sodium Channels; Genetic Transfection; Genetics; HEK293 Cell Line; HEK293 Cells; Human; Human Cell; Humans; Membrane Potential; Membrane Potentials; Metabolic Activation; Metabolism; Monoterpenes; N-Geranyl Cyclopropylcarboxamide; N Geranylcyclopropylcarboxamide; Nerve Protein; Nerve Tissue Proteins; Nucleotide Sequence; Pharmacology; Physiology; Ruthenium Red; Salt Intake; Sensory Nerve; Signal Transduction; Sodium Chloride, Dietary; Sodium Transport; Taste; Taste Bud; Taste Buds; Taste Perception; Terpene; Transfection; Transient Receptor Potential Channel (TRP Channel); Transient Receptor Potential Channels; TRPA1 Protein, Human; TRPV Cation Channels; TRPV1 Protein, Human; Unclassified Drug; Vanilloid Receptor; Vanilloid Receptor1; Vanilloid Receptor1 Antagonist
- TRPV1t, a variant of the transient receptor potential vanilloid-1 (TRPV1) has been proposed as a constitutively active, non-selective cation channel as a putative amiloride-insensitive salt taste receptor and shares many properties with TRPV1. Based on our previous chorda tympani taste nerve recordings in rodents and human sensory evaluations, we proposed that N- geranylcyclopropylcarboxamide (NGCC), a novel synthetic compound, acts as a salt taste enhancer by modulating the amiloride/benzamil-insensitive Na+ entry pathways. As an extension of this work, we investigated NGCC-induced human TRPV1 (hTRPV1) activation using a Ca2+-flux signaling assay in cultured cells. NGCC enhanced Ca2+ influx in hTRPV1-expressing cells in a dose-dependent manner (EC50 = 115 μM). NGCC-induced Ca 2+ influx was significantly attenuated by ruthenium red (RR; 30 mM), a non-specific blocker of TRP channels and capsazepine (CZP; 5 μM), a specific antagonist of TRPV1, implying that NGCC directly activates hTRPV1. TRPA1 is often co-expressed with TRPV1 in sensory neurons. Therefore, we also investigated the effects of NGCC on hTRPA1-expressing cells. Similar to hTRPV1, NGCC enhanced Ca2+ influx in hTRPA1-expressing cells (EC50 = 83.65 μM). The NGCC-induced Ca2+ influx in hTRPA1-expressing cells was blocked by RR (30 μM) and HC-030031 (100 μM), a specific antagonist of TRPA1. These results suggested that NGCC selectively activates TRPV1 and TRPA1 in cultured cells. These data may provide additional support for our previous hypothesis that NGCC interacts with TRPV1 variant cation channel, a putative amiloride/benzamil-insensitive salt taste pathway in the anterior taste receptive field. © 2014 Kim et al.
- Public Library of Science
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