Potentiation of acid-sensing ion channel activity by the activation of 5-HT₂ receptors in rat dorsal root ganglion neurons

Neuropharmacology
Fang QiuWang-Ping Hu

Abstract

Acid-sensing ion channels (ASICs), as key sensors for extracellular protons, are expressed in nociceptive sensory neurons and contribute to signalling pain caused by tissue acidosis. ASICs are also the subject of various factors. Here, we further provide evidence that the activity of ASICs is potentiated by the activation of 5-HT₂ receptors in rat dorsal root ganglion neurons. A specific 5-HT₂ receptor agonist, α-methyl-5-HT, dose-dependently enhanced proton-gated currents with an EC₅₀ of 0.13 ± 0.07 nM. The α-methyl-5-HT enhancing effect on proton-gated currents was blocked by cyproheptadine, a 5-HT₂ receptor antagonist, and removed by intracellular dialysis of either GDP-β-S or protein kinase C inhibitor GF109203X. Moreover, α-methyl-5-HT altered acid-evoked membrane excitability of rat DRG neurons and caused a significant increase in the amplitude of the depolarization and the number of spikes induced by acid stimuli. Finally, α-methyl-5-HT increased nociceptive responses to injection of acetic acid in rats. These results suggest that α-methyl-5-HT up-regulates the activity of ASICs via 5-HT₂ receptor and protein kinase C dependent signal pathways in rat primary sensory neurons and this potentiation contributed to acid- medi...Continue Reading

References

Jan 1, 1980·Neuroscience·O A Krishtal, V I Pidoplichko
Aug 1, 1995·British Journal of Anaesthesia·A Dray
Apr 5, 1996·The Journal of Biological Chemistry·M P PriceM J Welsh
Mar 13, 1997·Nature·R WaldmannM Lazdunski
Dec 31, 1997·The Journal of Biological Chemistry·E LinguegliaM Lazdunski
Dec 23, 1999·Neuropharmacology·T Varming
Feb 14, 2002·Proceedings of the National Academy of Sciences of the United States of America·Diego Alvarez de la RosaCecilia M Canessa
Mar 28, 2002·Pharmacology & Therapeutics·J R RaymondM N Garnovskaya
Oct 26, 2002·The Journal of Biological Chemistry·Anne BaronMichel Lazdunski
Sep 2, 2003·Trends in Neurosciences·Oleg Krishtal
Dec 3, 2004·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Nicholas G JonesStephen B McMahon
Nov 12, 2005·The Journal of Biological Chemistry·Marija VukicevicStephan Kellenberger
Mar 7, 2006·The Journal of Pharmacology and Experimental Therapeutics·Curtis R Kelly, Najam A Sharif
Jul 19, 2006·Proceedings of the National Academy of Sciences of the United States of America·Volodymyr I Pidoplichko, John A Dani
Aug 8, 2006·Trends in Neurosciences·John A WemmieMichael J Welsh
Feb 27, 2007·Journal of Bone and Mineral Metabolism·Maho NagaeToshiyuki Yoneda
Apr 14, 2007·The Journal of Biological Chemistry·Eric Lingueglia
Nov 30, 2007·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Hervé CadiouPeter A McNaughton
Oct 17, 2008·The EMBO Journal·Emmanuel DevalEric Lingueglia
Oct 30, 2009·The Journal of Pharmacology and Experimental Therapeutics·Aníbal GarzaEnrique Soto
Nov 18, 2009·British Journal of Pharmacology·Zhi-Wang LiWang-Ping Hu
Sep 3, 2010·Pharmacology & Therapeutics·Emmanuel DevalEric Lingueglia
Jan 29, 2011·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Shih-Yuan LinWei-Hsin Sun
Apr 22, 2011·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Emmanuel DevalEric Lingueglia

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Citations

Mar 20, 2014·European Journal of Pharmacology·Fang QiuWang-Ping Hu
Sep 12, 2013·Headache·Lachlan D Rash
Feb 21, 2014·Clinical and Experimental Pharmacology & Physiology·Zhen LeiJingxin Li
Nov 15, 2014·Journal of Neuroscience Research·Ting-Ting LiuWang-Ping Hu
Jan 24, 2015·Neuropharmacology·Anne Baron, Eric Lingueglia
Mar 1, 2015·Neuropharmacology·Emmanuel Deval, Eric Lingueglia
Oct 30, 2016·Trends in Immunology·Felipe A Pinho-RibeiroIsaac M Chiu
Jun 27, 2019·Journal of Neuroscience Research·Chun-Yu QiuWang-Ping Hu
Feb 29, 2020·Acta Pharmacologica Sinica·Lei WuWang-Ping Hu
May 30, 2019·International Journal of Molecular Sciences·Isabella SalzerStefan Boehm
Oct 28, 2021·Channels·Megan M CullinanJohn R Bankston

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