Українська English

ISSN 2522-9028 (Print)
ISSN 2522-9036 (Online)
DOI: https://doi.org/10.15407/fz

Fiziologichnyi Zhurnal

is a scientific journal issued by the

Bogomoletz Institute of Physiology
National Academy of Sciences of Ukraine

Editor-in-chief: V.F. Sagach

The journal was founded in 1955 as
1955 – 1977 "Fiziolohichnyi zhurnal" (ISSN 0015 – 3311)
1978 – 1993 "Fiziologicheskii zhurnal" (ISSN 0201 – 8489)
1994 – 2016 "Fiziolohichnyi zhurnal" (ISSN 0201 – 8489)
2017 – "Fiziolohichnyi zhurnal" (ISSN 2522-9028)

Fiziol. Zh. 2018; 64(1): 91-102

PROPERTIES OF VANILLOID RECEPTOR TYPE 1

M.O. Petrushenko, E.A. Petrushenko, E.A. Lukyanetz

    O.O. Bogomoletz Institute of Physiology, NASU, Kyiv, Ukraine
DOI: https://doi.org/10.15407/fz64.01.091


Abstract

The review summarizes the current data on the functioning and characteristics of the vanilloid receptors of the transient potential of the TRPV1 type. Possible mechanisms of processes of sensitization and desentization of TRPV1 receptors, role of phosphorylation/dephosphorylation processes in channel activity, role of calcium/calmodulin dependent modulation, a role of phosphatidylinositol are indicated. Attention is paid to the structure of TRPV1 channels and the peculiarities of agonist and antagonist activity of these channels. The functions of these channels are described.

Keywords: TRPV1 receptors; TRPV1 channels; calcium; cationic channels; nociception; sensitization of receptors; desensitization of receptors.

Full text: (PDF, in Ukrainian)

References

  1. Clapham DE. TRP channels as cellular sensors. Nature. 2003 Dec 4;426(6966):517-24. CrossRef PubMed
    2.  
  2. Caterina MJ, Schumacher MA, Tominaga M, Rosen TA, Levine JD, Julius D. The capsaicin receptor: a heatactivated ion channel in the pain pathway. Nature. 1997 Oct 23;389(6653):816-24. CrossRef PubMed
    3.  
  3. Nagy I, Santha P, Jancso G, Urban L. The role of the vanilloid (capsaicin) receptor (TRPV1) in physiology and pathology. Eur J Pharmacol. 2004 Oct 1;500(1-3):351-69. CrossRef PubMed
    4.  
  4. Clapham DE, Julius D, Montell C, Schultz G. International Union of Pharmacology. XLIX. Nomenclature and structure-function relationships of transient receptor potential channels. Pharmacol Rev. 2005 Dec;57(4):427-50. CrossRef PubMed
    5.  
  5. Everaerts W, Gees M, Alpizar YA, Farre R, Leten C, Apetrei A, et al. The capsaicin receptor TRPV1 is a crucial mediator of the noxious effects of mustard oil. Curr Biol.2011 Feb 22;21(4):316-21. CrossRef PubMed
    6.  
  6. Cui M, Honore P, Zhong C, Gauvin D, Mikusa J, Hernandez G, et al. TRPV1 receptors in the CNS play a key role in broadspectrum analgesia of TRPV1 antagonists. J Neurosci. 2006 Sep 13; 26(37): 9385-93. CrossRef PubMed
    7.  
  7. Huang SM, Bisogno T, Trevisani M, AlHayani A, De PL, Fezza F, et al. An endogenous capsaicinlike substance with high potency at recombinant and native vanilloid VR1 receptors. Proc Natl Acad Sci U S A. 2002 Jun 11;99(12):8400-5. CrossRef PubMed PubMedCentral
    8.  
  8. Conway SJ. TRPing the switch on pain: an introduction to the chemistry and biology of capsaicin and TRPV1. Chem Soc Rev. 2008;37(8):1530-45. CrossRef PubMed
    9.  
  9. Messeguer A, PlanellsCases R, FerrerMontiel A. Physiology and pharmacology of the vanilloid receptor. Curr Neuropharmacol. 2006 Jan;4(1):1-15. CrossRef PubMed PubMedCentral
    10.  
  10. Xue Q, Yu Y, Trilk SL, Jong BE, Schumacher MA. The genomic organization of the gene encoding the vanilloid receptor: evidence for multiple splice variants. Genomics. 2001 Aug;76(13): 14-20. CrossRef PubMed
    11.  
  11. Szallasi A, Blumberg PM. Vanilloid (Capsaicin) receptors and mechanisms. Pharmacol Rev. 1999 Jun;51(2):159-212. PubMed
    12.  
  12. Sterner O, Szallasi A. Novel natural vanilloid receptor agonists: new therapeutic targets for drug development. Trends Pharmacol Sci. 1999 Nov;20(11):459-65. CrossRef  
  13. Raisinghani M, Pabbidi RM, Premkumar LS. Activation of transient receptor potential vanilloid 1 (TRPV1) by resiniferatoxin. J Physiol. 2005 Sep 15;567(Pt 3):771-86. CrossRef PubMed PubMedCentral
    14.  
  14. Kumar R, Hazan A, Basu A, Zalcman N, Matzner H, Priel A. Tyrosine Residue in the TRPV1 Vanilloid Binding Pocket Regulates Deactivation Kinetics. J Biol Chem. 2016 Jun 24;291(26):13855-63. CrossRef PubMed PubMedCentral
    15.  
  15. Dragan AV, Petrushenko OA, Burlak OP, Lukyanetz EA. Effect of TRPA1 receptor activation on TRPV1 channel desensitization in rat dorsal ganglion neurons . Fiziol Zh. 2016;62(1):16-24. CrossRef PubMed
    16.  
  16. Jung J, Hwang SW, Kwak J, Lee SY, Kang CJ, Kim WB, et al. Capsaicin binds to the intracellular domain of the capsaicinactivated ion channel. J Neurosci. 1999 Jan 15;19(2):529-38. CrossRef PubMed
    17.  
  17. Koplas PA, Rosenberg RL, Oxford GS. The role of calcium in the desensitization of capsaicin responses in rat dorsal root ganglion neurons. J Neurosci. 1997 May 15;17(10):3525-37. CrossRef PubMed
    18.  
  18. Kostyk PG, Kostyuk E, Lukyanetz EA. Calcium ions in brain function - from physiology to pathology. Kyiv: Naukova Dumka; 2005.
    19.  
  19. Kostyk PG, Kostyuk EP, Lukyanetz EA. Intracellular calcium signalling: structure and function. Kyiv: Naukova Dumka; 2009.
    20.  
  20. Kostyuk PG, Lukyanetz EA. Mechanisms of antagonistic action of internal Ca2+ on serotonininduced potentiation of Ca2+ currents in Helix neurones. Pflugers Arch. 1993 Jun;424(1):73-83. CrossRef PubMed
    21.  
  21. Shkryl VM, Kostyuk PG, Lukyanetz EA. Dual action of cytosolic calcium on calcium channel activity during hypoxia in hippocampal neurones. Neuroreport. 2001;12(18):4035-9. CrossRef PubMed
    22.  
  22. Shkryl VM, Nikolaenko LM, Kostyuk PG, Lukyanetz EA. Highthreshold calcium channel activity in rat hippocampal neurones during hypoxia. Brain Res.1999;833(2):319-28. CrossRef  
  23. Liu B, Zhang C, Qin F. Functional recovery from desensitization of vanilloid receptor TRPV1 requires resynthesis of phosphatidylinositol 4,5-bisphosphate. J Neurosci. 2005 May 11;25(19):4835-43. CrossRef PubMed
    24.  
  24. Doroshenko PA, Kostyuk PG, Luk'yanetz EA. Modulation of calcium current by calmodulin antagonists. Neuroscience. 1988;27(3):1073-80. CrossRef  
  25. Rosenbaum T, Gordon-Shaag A, Munari M, Gordon SE. Ca2+/calmodulin modulates TRPV1 activation by capsaicin. J Gen Physiol. 2004 Jan;123(1):53-62. CrossRef PubMed PubMedCentral
    26.  
  26. Kostyuk PG, Lukyanetz EA, Doroshenko PA. Effects of serotonin and cAMP on calcium currents in different neurones of Helix pomatia. Pfluegers Arch /Eur J Physiol. 1992;420(1):9-15. CrossRef  
  27. Kostyuk PG, Lukyanetz EA, Ter-Markosyan AS. Parathyroid hormone enhances calcium current in snail neurones - Simulation of the effect by phorbol esters. Pfluegers Arch. 1992;420(2):146-52. CrossRef  
  28. Lukyanetz EA, Kostyuk PG. Two distinct receptors operate the cAMP cascade to upregulate Ltype Ca channels. Pflugers Arch. 1996;432(2):174-81. CrossRef  
  29. Lukyanetz EA, Sotkis AV, Kostyuk PG. Mechanisms of upregulation of single calcium channels by serotonin in Helix pomatia neurons. Biochem Biophys Res Commun. 2002;293(1):132-8. CrossRef  
  30. Lukacs V, Thyagarajan B, Varnai P, Balla A, Balla T, Rohacs T. Dual regulation of TRPV1 by phosphoinositides. J Neurosci. 2007 Jun 27;27(26):7070-80. CrossRef PubMed
    31.  
  31. Szallasi A, Cortright DN, Blum CA, Eid SR. The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proofofconcept. Nat Rev Drug Discov. 2007 May;6(5):357-72. CrossRef PubMed
    32.  
  32. Numazaki M, Tominaga T, Toyooka H, Tominaga M. Direct phosphorylation of capsaicin receptor VR1 by protein kinase Cepsilon and identification of two target serine residues. J Biol Chem. 2002 Apr 19;277(16):1337-8. CrossRef PubMed
    33.  
  33. Lukyanetz EA. Evidence for colocalization of calcineurin and calcium channels in dorsal root ganglion neurons. Neuroscience. 1997;78(3):625-8. CrossRef  
  34. Lukyanetz EA, Piper TP, Sihra TS. Calcineurin involvement in the regulation of highthreshold Ca<sup>2+</ sup> channels in NG108-15 (rodent neuroblastoma x glioma hybrid) cells. J Physiol. 1998;510(2):371-85. CrossRef PubMed PubMedCentral
    35.  
  35. Lopshire JC, Nicol GD. The cAMP transduction cascade mediates the prostaglandin E2 enhancement of the capsaicinelicited current in rat sensory neurons: wholecell and single-channel studies. J Neurosci. 1998 Aug 15;18(16):6081-92. CrossRef PubMed
    36.  
  36. Gavva NR, Treanor JJ, Garami A, Fang L, Surapaneni S, Akrami A, et al. Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. Pain. 2008 May;136(1-2):202-10. CrossRef PubMed
    37.  
  37. Mohapatra DP, Nau C. Regulation of Ca2+dependent desensitization in the vanilloid receptor TRPV1 by calcineurin and cAMP-dependent protein kinase. J Biol Chem. 2005 Apr 8;280(14):13424-32. CrossRef PubMed
    38.  
  38. Docherty RJ, Yeats JC, Bevan S, Boddeke HW. Inhibition of calcineurin inhibits the desensitization of capsaicinevoked currents in cultured dorsal root ganglion neurones from adult rats. Pflugers Arch. 1996 Apr;431(6):828-37. CrossRef PubMed 
  39. 39. Zhang X, Huang J, McNaughton PA. NGF rapidly increases membrane expression of TRPV1 heat-gated ion channels. EMBO J. 2005 Dec 21;24(24):4211-23. CrossRef PubMed PubMedCentral 
    40.  
  40. Studer M, McNaughton PA. Modulation of singlechannel properties of TRPV1 by phosphorylation. J Physiol. 2010 Oct 1;588(Pt 19):3743-56. CrossRef PubMed PubMedCentral
    41.  
  41. Silva M, CostaPereira JT, Martins D, Tavares I. Pain modulation from the brain during diabetic neuropathy: Uncovering the role of the rostroventromedial medulla. Neurobiol Dis. 2016 Dec;96:346-56. CrossRef PubMed
    42.  
  42. Basso L, Altier C. Transient Receptor Potential Channels in neuropathic pain. Curr Opin Pharmacol. 2017 Feb;32:9-15. CrossRef PubMed
    43.  
  43. Szolcsanyi J. Effect of capsaicin on thermoregulation: an update with new aspects. Temperature (Austin) . 2015 Apr;2(2):277-96. CrossRef PubMed PubMedCentral
    44.  
  44. Steiner AA, Turek VF, Almeida MC, Burmeister JJ, Oliveira DL, Roberts JL, et al. Nonthermal activation of transient receptor potential vanilloid1 channels in abdominal viscera tonically inhibits autonomic colddefense effectors. J Neurosci. 2007 Jul 11;27(28):7459-68. CrossRef PubMed
    45.  
  45. Gavva NR. Bodytemperature maintenance as the predominant function of the vanilloid receptor TRPV1. Trends Pharmacol Sci. 2008 Nov;29(11):550-7. CrossRef PubMed
    46.  
  46. Chizh BA, O'Donnell MB, Napolitano A, Wang J, Brooke AC, Aylott MC, et al. The effects of the TRPV1 antagonist SB705498 on TRPV1 receptormediated activity and inflammatory hyperalgesia in humans. Pain. 2007 Nov;132(1-2):132-41. CrossRef PubMed
    47.  
  47. Pareek TK, Keller J, Kesavapany S, Agarwal N, Kuner R, Pant HC, et al. Cyclindependent kinase 5 modulates nociceptive signaling through direct phosphorylation of transient receptor potential vanilloid 1. Proc Natl Acad Sci U S A. 2007 Jan 9;104(2):660-5. CrossRef PubMed PubMedCentral
    48.  
  48. Knotkova H, Pappagallo M, Szallasi A. Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival? Clin J Pain. 2008 Feb;24(2):142-54. CrossRef PubMed
    49.  
  49. Moriyama T, Higashi T, Togashi K, Iida T, Segi E, Sugimoto Y, et al. Sensitization of TRPV1 by EP1 and IP reveals peripheral nociceptive mechanism of prostaglandins. Mol Pain. 2005;1:1-13. CrossRef PubMed PubMedCentral
    50.  
  50. Tominaga M. The Role of TRP Channels in Thermosensation. In: Liedtke WB, Heller S, editors. TRP Ion Channel Function in Sensory Transduction and Cellular Signaling Cascades, Frontiers in neuroscience.Boca Raton: CRC Press; 2007:p. 1-22. PubMed
    51.  
  51. Chung MK, Campbell JN. Use of Capsaicin to Treat Pain: Mechanistic and Therapeutic Considerations. Pharmaceuticals (Basel). 2016 Nov 1;9(4):pii: E66. CrossRef PubMed
    52.  
  52. Sun WH, Chen CC. Roles of Proton-Sensing Receptors in the Transition from Acute to Chronic Pain. J Dent Res. 2016 Feb;95(2):135-42. CrossRef PubMed
    53.  
  53. Moran MM, Szallasi A. Targeting nociceptive TRP channels to treat chronic pain: current state of the field. Br J Pharmacol. 2017 Sep 19;1-20.
    54.  
  54. Ruggiero RN, Rossignoli MT, De Ross JB, Hallak JEC, Leite JP, BuenoJunior LS. Cannabinoids and Vanilloids in Schizophrenia: Neurophysiological Evidence and Directions for Basic Research. Front Pharmacol. 2017;8:1-26. CrossRef PubMed PubMedCentral
    55.  
  55. Naziroglu M, Demirdas A. Psychiatric Disorders and TRP Channels: Focus on Psychotropic Drugs. Curr Neuropharmacol. 2015;13(2):248-57. CrossRef PubMed PubMedCentral
    56.  
  56. Smutzer G, Devassy RK. Integrating TRPV1 Receptor Function with Capsaicin Psychophysics. Adv Pharmacol Sci. 2016;15(1):24-57. CrossRef  
  57. Derbenev AV, Zsombok A. Potential therapeutic value of TRPV1 and TRPA1 in diabetes mellitus and obesity. Semin Immunopathol. 2016 May;38(3):397-406. CrossRef PubMed PubMedCentral
    58.  
  58. Alawi KM, Aubdool AA, Liang L, Wilde E, Vepa A, Psefteli MP, et al. The sympathetic nervous system is controlled by transient receptor potential vanilloid 1 in the regulation of body temperature. FASEB J. 2015 Oct;29(10):4285-98. CrossRef PubMed PubMedCentral
    59.  
  59. Wang H, Siemens J. TRP ion channels in thermosensation, thermoregulation and metabolism. Temperature (Austin). 2015 Apr 26;2(2):178-87. CrossRef PubMed PubMedCentral
    60.  
  60. JancsoGabor A, Szolcsanyi J, Jancso N. Irreversible impairment of thermoregulation induced by capsaicin and similar pungent substances in rats and guineapigs. J Physiol. 1970 Mar;206(3):495-507. CrossRef PubMed PubMedCentral
    61.  
  61. Jancso G, Dux M, Oszlacs O, Santha P. Activation of the transient receptor potential vanilloid-1 (TRPV1) channel opens the gate for pain relief. Br J Pharmacol. 2008 Dec;155(8):1139-41. CrossRef PubMed PubMedCentral
    62.  
  62. Szallasi A, Sheta M. Targeting TRPV1 for pain relief: limits, losers and laurels. Expert Opin Investig Drugs. 2012 Sep;21(9):1351-69. CrossRef PubMed
    63.  
  63. Zsombok A. Vanilloid receptors - do they have a role in whole body metabolism? Evidence from TRPV1. J Diabetes Complications. 2013 May;27(3):287-92. CrossRef PubMed PubMedCentral
    64.  
  64. Razavi R, Chan Y, Afifiyan FN, Liu XJ, Wan X, Yantha J, et al. TRPV1+ sensory neurons control beta cell stress and islet inflammation in autoimmune diabetes. Cell. 2006 Dec 15;127(6):1123-35. CrossRef PubMed
    65.  
  65. Suri A, Szallasi A. The emerging role of TRPV1 in diabetes and obesity. Trends Pharmacol Sci. 2008 Jan;29(1):2936. CrossRef PubMed
    66.  
  66. Tsui H, Paltser G, Chan Y, Dorfman R, Dosch HM. 'Sensing' the link between type 1 and type 2 diabetes. Diabetes Metab Res Rev. 2011 Nov;27(8):913-8. CrossRef PubMed
    67.  
  67. Wang P, Yan Z, Zhong J, Chen J, Ni Y, Li L, et al. Transient receptor potential vanilloid 1 activation enhances gut glucagonlike peptide1 secretion and improves glucose homeostasis. Diabetes. 2012 Aug;61(8):2155-65. CrossRef PubMed PubMedCentral
    68.  
  68. WesterterpPlantenga MS, Smeets A, Lejeune MP. Sensory and gastrointestinal satiety effects of capsaicin on food intake. Int J Obes (Lond). 2005 Jun;29(6):682-8. CrossRef PubMed
    69.  
  69. Gram DX, Ahren B, Nagy I, Olsen UB, Brand CL, Sundler F, et al. Capsaicinsensitive sensory fibers in the islets of Langerhans contribute to defective insulin secretion in Zucker diabetic rat, an animal model for some aspects of human type 2 diabetes. Eur J Neurosci.2007 Jan;25(1):213-23. CrossRef PubMed
    70.  
  70. Kang JH, Tsuyoshi G, Le NH, Kim HM, Tu TH, Noh HJ, et al. Dietary capsaicin attenuates metabolic dysregulation in genetically obese diabetic mice. J Med Food. 2011 Mar;14(3):310-5. CrossRef PubMed
    71.  
  71. Lee E, Jung DY, Kim JH, Patel PR, Hu X, Lee Y, et al. Transient receptor potential vanilloid type1 channel regulates dietinduced obesity, insulin resistance, and leptin resistance. FASEB J. 2015 Aug;29(8):3182-92. CrossRef PubMed PubMedCentral
    72.  
  72. Gao H, Miyata K, Bhaskaran MD, Derbenev AV, Zsombok A. Transient receptor potential vanilloid type 1dependent regulation of liverrelated neurons in the paraventricular nucleus of the hypothalamus diminished in the type 1 diabetic mouse. Diabetes. 2012 Jun;61(6):1381-90. CrossRef PubMed PubMedCentral
    73.  
  73. Jordt SE, Tominaga M, Julius D. Acid potentiation of the capsaicin receptor determined by a key extracellular site. Proc Natl Acad Sci U S A. 2000;97(14):8134-9. CrossRef PubMed PubMedCentral
    74.  
  74. Bevan S, Yeats J. Protons activate a cation conductance in a subpopulation of rat dorsal root ganglion neurones. J Physiol. 1991 Feb;433:145-61. CrossRef PubMed PubMedCentral
    75.  
  75. Hellwig N, Plant TD, Janson W, Schafer M, Schultz G, Schaefer M. TRPV1 acts as proton channel to induce acidification in nociceptive neurons. J Biol Chem. 2004 Aug 13;279(33):34553-61. CrossRef PubMed
    76.  
  76. Tominaga M, Caterina MJ, Malmberg AB, Rosen TA, Gilbert H, Skinner K, et al. The cloned capsaicin receptor integrates multiple pain-producing stimuli. Neuron. 1998 Sep;21(3):531-43. CrossRef  
  77. Ryu S, Liu B, Qin F. Low pH potentiates both capsaicin binding and channel gating of VR1 receptors. J Gen Physiol. 2003 Jul;122(1):45-61. CrossRef PubMed PubMedCentral
    78.  
  78. Petersen M, LaMotte RH. Effect of protons on the inward current evoked by capsaicin in isolated dorsal root ganglion cells. Pain. 1993 Jul;54(1):37-42. CrossRef  
  79. Martenson ME, Ingram SL, Baumann TK. Potentiation of rabbit trigeminal responses to capsaicin in a low pH environment. Brain Res. 1994 Jul 18;651(1-2):143-7. CrossRef  
  80. Baumann TK, Burchiel KJ, Ingram SL, Martenson ME. Responses of adult human dorsal root ganglion neurons in culture to capsaicin and low pH. Pain. 1996;65(1):31-8. CrossRef

© National Academy of Sciences of Ukraine, Bogomoletz Institute of Physiology, 2014-2024.