Skip to main content
SpringerLink
Log in

Temperature-Sensitive Transient Receptor Potential Channels as Ionotropic Cannabinoid Receptors

  • Chapter
  • First Online:
endoCANNABINOIDS

Part of the book series: The Receptors ((REC,volume 24))

Abstract

Since the discovery that the endocannabinoid anandamide could activate the transient receptor potential vanilloid-1 (TRPV1) channel, and that some synthetic TRPV1 agonists could also inhibit anandamide cellular re-uptake, reports of interactions between TRP channels, particularly the temperature-sensitive members of this family, and cannabinoids have intensified. Evidence now exists to suggest that TRPV1 is an ionotropic receptor for some endocannabinoids, and that this as well as other “Thermo-TRPs” can act as transducers for some of the pharmacological actions of phytocannabinoids, including those devoid of significant activity at cannabinoid CB1 and CB2 receptors. Such evidence, and its possible implications in the potential therapeutic applications of endogenous, plant and synthetic cannabimimetic compounds, is reviewed in this chapter.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution
eBook
USD 16.99
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 119.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 169.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  • Ahluwalia J, Urban L, Capogna M, Bevan S, Nagy I (2000) Cannabinoid 1 receptors are expressed in nociceptive primary sensory neurons. Neuroscience 100:685–688

    Article  CAS  PubMed  Google Scholar 

  • Akopian AN, Ruparel NB, Patwardhan A, Hargreaves KM (2008) Cannabinoids desensitize capsaicin and mustard oil responses in sensory neurons via TRPA1 activation. J Neurosci 28:1064–1075

    Article  CAS  PubMed  Google Scholar 

  • Alenmyr L, Greiff L, Andersson M, Sterner O, Zygmunt PM, Högestätt ED (2012) Effect of mucosal TRPV1 inhibition in allergic rhinitis. Basic Clin Pharmacol Toxicol 110:264–268

    Article  CAS  PubMed  Google Scholar 

  • Appendino G, Cascio MG, Bacchiega S, Moriello AS, Minassi A, Thomas A, Ross R, Pertwee R, De Petrocellis L, Di Marzo V (2006) First “hybrid” ligands of vanilloid TRPV1 and cannabinoid CB2 receptors and non-polyunsaturated fatty acid-derived CB2-selective ligands. FEBS Lett 580:568–574

    Article  CAS  PubMed  Google Scholar 

  • Appendino G, Bacchiega S, Minassi A, Cascio MG, De Petrocellis L, Di Marzo V (2007) The 1,2,3-triazole ring as a peptido- and olefinomimetic element: discovery of click vanilloids and cannabinoids. Angew Chem Int Ed Engl 46:9312–9315

    Article  CAS  PubMed  Google Scholar 

  • Bari M, Bonifacino T, Milanese M, Spagnuolo P, Zappettini S, Battista N, Giribaldi F, Usai C, Bonanno G, Maccarrone M (2011) The endocannabinoid system in rat gliosomes and its role in the modulation of glutamate release. Cell Mol Life Sci 68:833–845

    Article  CAS  PubMed  Google Scholar 

  • Bhaskaran MD, Smith BN (2010) Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy. Exp Neurol 223:529–536

    Article  CAS  PubMed  Google Scholar 

  • Bisogno T, Melck D, Bobrov MYu, Gretskaya NM, Bezuglov VV, De Petrocellis L, Di Marzo V (2000) N-acyl-dopamines: novel synthetic CB(1) cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimimetic activity in vitro and in vivo. Biochem J 351:817–824

    Article  CAS  PubMed  Google Scholar 

  • Bisogno T, Hanus L, De Petrocellis L, Tchilibon S, Ponde DE, Brandi I, Moriello AS, Davis JB, Mechoulam R, Di Marzo V (2001) Molecular targets for cannabidiol and its synthetic analogues: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide. Br J Pharmacol 134:845–852

    Article  CAS  PubMed  Google Scholar 

  • Boesmans W, Owsianik G, Tack J, Voets T, Vanden Berghe P (2011) TRP channels in neurogastroenterology: opportunities for therapeutic intervention. Br J Pharmacol 162:18–37

    Article  CAS  PubMed  Google Scholar 

  • Campos AC, Guimarães FS (2009) Evidence for a potential role for TRPV1 receptors in the dorsolateral periaqueductal gray in the attenuation of the anxiolytic effects of cannabinoids. Prog Neuropsychopharmacol Biol Psychiatry 33:1517–1521

    Article  CAS  PubMed  Google Scholar 

  • Casarotto PC, Terzian AL, Aguiar DC, Zangrossi H, Guimarães FS, Wotjak CT, Moreira FA (2012) Opposing roles for cannabinoid receptor type-1 (CB1) and transient receptor potential vanilloid type-1 channel (TRPV1) on the modulation of panic-like responses in rats. Neuropsychopharmacology 37:478–486

    Article  CAS  PubMed  Google Scholar 

  • Cella M, Leguizamón GF, Sordelli MS, Cervini M, Guadagnoli T, Ribeiro ML, Franchi AM, Farina MG (2008) Dual effect of anandamide on rat placenta nitric oxide synthesis. Placenta 29:699–707

    Article  CAS  PubMed  Google Scholar 

  • Chávez AE, Chiu CQ, Castillo PE (2010) TRPV1 activation by endogenous anandamide triggers postsynaptic long-term depression in dentate gyrus. Nat Neurosci 13:1511–1518

    Article  PubMed  CAS  Google Scholar 

  • Chu CJ, Huang SM, De Petrocellis L, Bisogno T, Ewing SA, Miller JD, Zipkin RE, Daddario N, Appendino G, Di Marzo V, Walker JM (2003) N-oleoyldopamine, a novel endogenous capsaicin-like lipid that produces hyperalgesia. J Biol Chem 278:13633–13639

    Article  CAS  PubMed  Google Scholar 

  • Comelli F, Giagnoni G, Bettoni I, Colleoni M, Costa B (2008) Antihyperalgesic effect of a Cannabis sativa extract in a rat model of neuropathic pain: mechanisms involved. Phytother Res 22:1017–1024

    Article  PubMed  Google Scholar 

  • Costa B, Giagnoni G, Franke C, Trovato AE, Colleoni M (2004) Vanilloid TRPV1 receptor mediates the antihyperalgesic effect of the nonpsychoactive cannabinoid, cannabidiol, in a rat model of acute inflammation. Br J Pharmacol 143:247–250

    Article  CAS  PubMed  Google Scholar 

  • Costa B, Trovato AE, Comelli F, Giagnoni G, Colleoni M (2007) The non-psychoactive cannabis constituent cannabidiol is an orally effective therapeutic agent in rat chronic inflammatory and neuropathic pain. Eur J Pharmacol 556:75–83

    Article  CAS  PubMed  Google Scholar 

  • Costa B, Comelli F, Bettoni I, Colleoni M, Giagnoni G (2008) The endogenous fatty acid amide, palmitoylethanolamide, has anti-allodynic and anti-hyperalgesic effects in a murine model of neuropathic pain: involvement of CB(1), TRPV1 and PPARgamma receptors and neurotrophic factors. Pain 139:541–550

    Article  CAS  PubMed  Google Scholar 

  • Cristino L, de Petrocellis L, Pryce G, Baker D, Guglielmotti V, Di Marzo V (2006) Immunohistochemical localization of cannabinoid type 1 and vanilloid transient receptor potential vanilloid type 1 receptors in the mouse brain. Neuroscience 139:1405–1415

    Article  CAS  PubMed  Google Scholar 

  • Cristino L, Starowicz K, De Petrocellis L, Morishita J, Ueda N, Guglielmotti V, Di Marzo V (2008) Immunohistochemical localization of anabolic and catabolic enzymes for anandamide and other putative endovanilloids in the hippocampus and cerebellar cortex of the mouse brain. Neuroscience 151:955–968

    Article  CAS  PubMed  Google Scholar 

  • Davies JW, Hainsworth AH, Guerin CJ, Lambert DG (2010) Pharmacology of capsaicin-, anandamide-, and N-arachidonoyl-dopamine-evoked cell death in a homogeneous transient receptor potential vanilloid subtype 1 receptor population. Br J Anaesth 104:596–602

    Article  CAS  PubMed  Google Scholar 

  • De Petrocellis L, Di Marzo V (2009) Role of endocannabinoids and endovanilloids in Ca2+ signalling. Cell Calcium 45:611–624

    Article  PubMed  CAS  Google Scholar 

  • De Petrocellis L, Bisogno T, Davis JB, Pertwee RG, Di Marzo V (2000) Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity. FEBS Lett 483:52–56

    Article  PubMed  Google Scholar 

  • De Petrocellis L, Bisogno T, Maccarrone M, Davis JB, Finazzi-Agro A, Di Marzo V (2001a) The activity of anandamide at vanilloid VR1 receptors requires facilitated transport across the cell membrane and is limited by intracellular metabolism. J Biol Chem 276:12856–12863

    Article  PubMed  Google Scholar 

  • De Petrocellis L, Davis JB, Di Marzo V (2001b) Palmitoylethanolamide enhances anandamide stimulation of human vanilloid VR1 receptors. FEBS Lett 506:253–256

    Article  PubMed  Google Scholar 

  • De Petrocellis L, Chu CJ, Moriello AS, Kellner JC, Walker JM, Di Marzo V (2004) Actions of two naturally occurring saturated N-acyldopamines on transient receptor potential vanilloid 1 (TRPV1) channels. Br J Pharmacol 143:251–256

    Article  PubMed  CAS  Google Scholar 

  • De Petrocellis L, Starowicz K, Moriello AS, Vivese M, Orlando P, Di Marzo V (2007) Regulation of transient receptor potential channels of melastatin type 8 (TRPM8): effect of cAMP, cannabinoid CB(1) receptors and endovanilloids. Exp Cell Res 313:1911–1920

    Article  PubMed  CAS  Google Scholar 

  • De Petrocellis L, Vellani V, Schiano-Moriello A, Marini P, Magherini PC, Orlando P, Di Marzo V (2008) Plant-derived cannabinoids modulate the activity of transient receptor potential channels of ankyrin type-1 and melastatin type-8. J Pharmacol Exp Ther 325:1007–1015

    Article  PubMed  CAS  Google Scholar 

  • De Petrocellis L, Ligresti A, Moriello AS, Allarà M, Bisogno T, Petrosino S, Stott CG, Di Marzo V (2011) Effects of cannabinoids and cannabinoid-enriched Cannabis extracts on TRP channels and endocannabinoid metabolic enzymes. Br J Pharmacol 163:1479–1494

    Article  PubMed  CAS  Google Scholar 

  • De Petrocellis L, Orlando P, Moriello AS, Aviello G, Stott C, Izzo AA, Di Marzo V (2012) Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation. Acta Physiol 204:255–266

    Article  CAS  Google Scholar 

  • Devane WA, Hanus L, Breuer A, Pertwee RG, Stevenson LA, Griffin G, Gibson D, Mandelbaum A, Etinger A, Mechoulam R (1992) Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 258:1946–1949

    Article  CAS  PubMed  Google Scholar 

  • Di Marzo V (2008) Targeting the endocannabinoid system: to enhance or reduce? Nat Rev Drug Discov 7:438–455

    Article  PubMed  CAS  Google Scholar 

  • Di Marzo V (2010) Anandamide serves two masters in the brain. Nat Neurosci 13:1446–1448

    Article  PubMed  CAS  Google Scholar 

  • Di Marzo V, Bisogno T, Melck D, Ross R, Brockie H, Stevenson L, Pertwee R, De Petrocellis L (1998) Interactions between synthetic vanilloids and the endogenous cannabinoid system. FEBS Lett 436:449–454

    Article  PubMed  Google Scholar 

  • Di Marzo V, De Petrocellis L, Bisogno T, Melck D (1999) Metabolism of anandamide and 2-arachidonoylglycerol: an historical overview and some recent developments. Lipids 34:S319–S325

    Article  PubMed  Google Scholar 

  • Di Marzo V, Breivogel CS, Tao Q, Bridgen DT, Razdan RK, Zimmer AM, Zimmer A, Martin BR (2000) Levels, metabolism, and pharmacological activity of anandamide in CB(1) cannabinoid receptor knockout mice: evidence for non-CB(1), non-CB(2) receptor-mediated actions of anandamide in mouse brain. J Neurochem 75:2434–2444

    Article  PubMed  Google Scholar 

  • Di Marzo V, Bisogno T, De Petrocellis L (2001) Anandamide: some like it hot. Trends Pharmacol Sci 22:346–349

    Article  PubMed  Google Scholar 

  • Engel MA, Izydorczyk I, Mueller-Tribbensee SM, Becker C, Neurath MF, Reeh PW (2011) Inhibitory CB1 and activating/desensitizing TRPV1-mediated cannabinoid actions on CGRP release in rodent skin. Neuropeptides 45:229–237

    Article  CAS  PubMed  Google Scholar 

  • Francavilla F, Battista N, Barbonetti A, Vassallo MR, Rapino C, Antonangelo C, Pasquariello N, Catanzaro G, Barboni B, Maccarrone M (2009) Characterization of the endocannabinoid system in human spermatozoa and involvement of transient receptor potential vanilloid 1 receptor in their fertilizing ability. Endocrinology 150:4692–4700

    Article  CAS  PubMed  Google Scholar 

  • Garami A, Pakai E, Oliveira DL, Steiner AA, Wanner SP, Almeida MC, Lesnikov VA, Gavva NR, Romanovsky AA (2011) Thermoregulatory phenotype of the Trpv1 knockout mouse: thermoeffector dysbalance with hyperkinesis. J Neurosci 31:1721–1733

    Article  CAS  PubMed  Google Scholar 

  • García Mdel C, Adler-Graschinsky E, Celuch SM (2009) Enhancement of the hypotensive effects of intrathecally injected endocannabinoids by the entourage compound palmitoylethanolamide. Eur J Pharmacol 610:75–80

    Article  PubMed  CAS  Google Scholar 

  • Gavva NR, Klionsky L, Qu Y, Shi L, Tamir R, Edenson S, Zhang TJ, Viswanadhan VN, Toth A, Pearce LV, Vanderah TW, Porreca F, Blumberg PM, Lile J, Sun Y, Wild K, Louis JC, Treanor JJ (2004) Molecular determinants of vanilloid sensitivity in TRPV1. J Biol Chem 279:20283–20295

    Article  CAS  PubMed  Google Scholar 

  • Geppetti P, Nassini R, Materazzi S, Benemei S (2008) The concept of neurogenic inflammation. BJU Int 101(suppl 3):2–6

    Article  CAS  PubMed  Google Scholar 

  • Gervasi MG, Osycka-Salut C, Caballero J, Vazquez-Levin M, Pereyra E, Billi S, Franchi A, Perez-Martinez S (2011) Anandamide capacitates bull spermatozoa through CB1 and TRPV1 activation. PLoS One 6:e16993

    Article  CAS  PubMed  Google Scholar 

  • Gibson HE, Edwards JG, Page RS, Van Hook MJ, Kauer JA (2008) TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons. Neuron 57:746–759

    Article  CAS  PubMed  Google Scholar 

  • Golech SA, McCarron RM, Chen Y, Bembry J, Lenz F, Mechoulam R, Shohami E, Spatz M (2004) Human brain endothelium: coexpression and function of vanilloid and endocannabinoid receptors. Brain Res Mol Brain Res 132:87–92

    Article  CAS  PubMed  Google Scholar 

  • Goswami C, Rademacher N, Smalla KH, Kalscheuer V, Ropers HH, Gundelfinger ED, Hucho T (2010) TRPV1 acts as a synaptic protein and regulates vesicle recycling. J Cell Sci 123:2045–2057

    Article  CAS  PubMed  Google Scholar 

  • Grueter BA, Brasnjo G, Malenka RC (2010) Postsynaptic TRPV1 triggers cell type-specific long-term depression in the nucleus accumbens. Nat Neurosci 13:1519–1525

    Article  CAS  PubMed  Google Scholar 

  • Han P, McDonald HA, Bianchi BR, Kouhen RE, Vos MH, Jarvis MF, Faltynek CR, Moreland RB (2007) Capsaicin causes protein synthesis inhibition and microtubule disassembly through TRPV1 activities both on the plasma membrane and intracellular membranes. Biochem Pharmacol 73:1635–1645

    Article  CAS  PubMed  Google Scholar 

  • Hegde VL, Nagarkatti PS, Nagarkatti M (2011) Role of myeloid-derived suppressor cells in amelioration of experimental autoimmune hepatitis following activation of TRPV1 receptors by cannabidiol. PLoS One 6:e18281

    Article  CAS  PubMed  Google Scholar 

  • Ho WS, Barrett DA, Randall MD (2008) ‘Entourage’ effects of N-palmitoylethanolamide and N-oleoylethanolamide on vasorelaxation to anandamide occur through TRPV1 receptors. Br J Pharmacol 155:837–846

    Article  CAS  PubMed  Google Scholar 

  • Hsu CC, Bien MY, Huang YT, Ruan T, Kou YR, Lin YS (2009) N-arachidonyl dopamine sensitizes rat capsaicin-sensitive lung vagal afferents via activation of TRPV1 receptors. Respir Physiol Neurobiol 167:323–332

    Article  CAS  PubMed  Google Scholar 

  • Huang SM, Walker JM (2006) Enhancement of spontaneous and heat-evoked activity in spinal nociceptive neurons by the endovanilloid/endocannabinoid N-arachidonoyldopamine (NADA). J Neurophysiol 95:1207–1212

    Article  CAS  PubMed  Google Scholar 

  • Huang SM, Bisogno T, Trevisani M, Al-Hayani A, De Petrocellis L, Fezza F, Tognetto M, Petros TJ, Krey JF, Chu CJ, Miller JD, Davies SN, Geppetti P, Walker JM, Di Marzo V (2002) An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors. Proc Natl Acad Sci U S A 99:8400–8405

    Article  CAS  PubMed  Google Scholar 

  • Huang C, Hu ZL, Wu WN, Yu DF, Xiong QJ, Song JR, Shu Q, Fu H, Wang F, Chen JG (2010) Existence and distinction of acid-evoked currents in rat astrocytes. Glia 58:1415–1424

    PubMed  Google Scholar 

  • Iwata Y, Katanosaka Y, Arai Y, Shigekawa M, Wakabayashi S (2009) Dominant-negative inhibition of Ca2+ influx via TRPV2 ameliorates muscular dystrophy in animal models. Hum Mol Genet 18:824–834

    CAS  PubMed  Google Scholar 

  • Jacobsson SO, Wallin T, Fowler CJ (2001) Inhibition of rat C6 glioma cell proliferation by endogenous and synthetic cannabinoids. Relative involvement of cannabinoid and vanilloid receptors. J Pharmacol Exp Ther 299:951–959

    CAS  PubMed  Google Scholar 

  • Jeske NA, Patwardhan AM, Gamper N, Price TJ, Akopian AN, Hargreaves KM (2006) Cannabinoid WIN 55,212-2 regulates TRPV1 phosphorylation in sensory neurons. J Biol Chem 281:32879–32890

    Article  CAS  PubMed  Google Scholar 

  • Jin K, Xie L, Kim SH, Parmentier-Batteur S, Sun Y, Mao XO, Childs J, Greenberg DA (2004) Defective adult neurogenesis in CB1 cannabinoid receptor knockout mice. Mol Pharmacol 66:204–208

    Article  CAS  PubMed  Google Scholar 

  • Jordt SE, Julius D (2002) Molecular basis for species-specific sensitivity to “hot” chili peppers. Cell 108:421–430

    Article  CAS  PubMed  Google Scholar 

  • Jordt SE, Bautista DM, Chuang HH, McKemy DD, Zygmunt PM, Högestätt ED, Meng ID, Julius D (2004) Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1. Nature 427:260–265

    Article  CAS  PubMed  Google Scholar 

  • Kawahara H, Drew GM, Christie MJ, Vaughan CW (2011) Inhibition of fatty acid amide hydrolase unmasks CB1 receptor and TRPV1 channel-mediated modulation of glutamatergic synaptic transmission in midbrain periaqueductal grey. Br J Pharmacol 163:1214–1222

    Article  CAS  PubMed  Google Scholar 

  • Kim SR, Chung YC, Chung ES, Park KW, Won SY, Bok E, Park ES, Jin BK (2007) Roles of transient receptor potential vanilloid subtype 1 and cannabinoid type 1 receptors in the brain: neuroprotection versus neurotoxicity. Mol Neurobiol 35:245–254

    Article  PubMed  CAS  Google Scholar 

  • Kim YH, Park CK, Back SK, Lee CJ, Hwang SJ, Bae YC, Na HS, Kim JS, Jung SJ, Oh SB (2009) Membrane-delimited coupling of TRPV1 and mGluR5 on presynaptic terminals of nociceptive neurons. J Neurosci 29:10000–10009

    Article  CAS  PubMed  Google Scholar 

  • Kogan NM, Blázquez C, Alvarez L, Gallily R, Schlesinger M, Guzmán M, Mechoulam R (2006) A cannabinoid quinone inhibits angiogenesis by targeting vascular endothelial cells. Mol Pharmacol 70:51–59

    CAS  PubMed  Google Scholar 

  • Landucci E, Scartabelli T, Gerace E, Moroni F, Pellegrini-Giampietro DE (2011) CB1 receptors and post-ischemic brain damage: studies on the toxic and neuroprotective effects of cannabinoids in rat organotypic hippocampal slices. Neuropharmacology 60:674–682

    Article  CAS  PubMed  Google Scholar 

  • Lever IJ, Robinson M, Cibelli M, Paule C, Santha P, Yee L, Hunt SP, Cravatt BF, Elphick MR, Nagy I, Rice AS (2009) Localization of the endocannabinoid-degrading enzyme fatty acid amide hydrolase in rat dorsal root ganglion cells and its regulation after peripheral nerve injury. J Neurosci 29:3766–3780

    Article  CAS  PubMed  Google Scholar 

  • Liao HT, Lee HJ, Ho YC, Chiou LC (2011) Capsaicin in the periaqueductal gray induces analgesia via metabotropic glutamate receptor-mediated endocannabinoid retrograde disinhibition. Br J Pharmacol 163:330–345

    Article  CAS  PubMed  Google Scholar 

  • Lin YS, Lin RL, Bien MY, Ho CY, Kou YR (2009) Sensitization of capsaicin-sensitive lung vagal afferents by anandamide in rats: role of transient receptor potential vanilloid 1 receptors. J Appl Physiol 106:1142–1152

    Article  CAS  PubMed  Google Scholar 

  • Lisboa SF, Guimarães FS (2012) Differential role of CB1 and TRPV1 receptors on anandamide modulation of defensive responses induced by nitric oxide in the dorsolateral periaqueductal gray. Neuropharmacology 62:2455–2462. http://dx.doi.org/10.1016/j.neuropharm.2012.02.008

    Google Scholar 

  • Long LE, Malone DT, Taylor DA (2006) Cannabidiol reverses MK-801-induced disruption of prepulse inhibition in mice. Neuropsychopharmacology 31:795–803

    Article  CAS  PubMed  Google Scholar 

  • Maccarrone M, Barboni B, Paradisi A, Bernabò N, Gasperi V, Pistilli MG, Fezza F, Lucidi P, Mattioli M (2005) Characterization of the endocannabinoid system in boar spermatozoa and implications for sperm capacitation and acrosome reaction. J Cell Sci 118:4393–4404

    Article  CAS  PubMed  Google Scholar 

  • Maccarrone M, Rossi S, Bari M, De Chiara V, Fezza F, Musella A, Gasperi V, Prosperetti C, Bernardi G, Finazzi-Agrò A, Cravatt BF, Centonze D (2008) Anandamide inhibits metabolism and physiological actions of 2-arachidonoylglycerol in the striatum. Nat Neurosci 11:152–159

    Article  CAS  PubMed  Google Scholar 

  • Maione S, Bisogno T, de Novellis V, Palazzo E, Cristino L, Valenti M, Petrosino S, Guglielmotti V, Rossi F, Di Marzo V (2006) Elevation of endocannabinoid levels in the ventrolateral periaqueductal grey through inhibition of fatty acid amide hydrolase affects descending nociceptive pathways via both cannabinoid receptor type 1 and transient receptor potential vanilloid type-1 receptors. J Pharmacol Exp Ther 316:969–982

    Article  CAS  PubMed  Google Scholar 

  • Maione S, De Petrocellis L, de Novellis V, Moriello AS, Petrosino S, Palazzo E, Rossi FS, Woodward DF, Di Marzo V (2007) Analgesic actions of N-arachidonoyl-serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors. Br J Pharmacol 150:766–781

    Article  CAS  PubMed  Google Scholar 

  • Maione S, Starowicz K, Cristino L, Guida F, Palazzo E, Luongo L, Rossi F, Marabese I, de Novellis V, Di Marzo V (2009) Functional interaction between TRPV1 and micro-opioid receptors in the descending antinociceptive pathway activates glutamate transmission and induces analgesia. J Neurophysiol 101:2411–2422

    Article  CAS  PubMed  Google Scholar 

  • Manna SS, Umathe SN (2012) Involvement of transient receptor potential vanilloid type 1 channels in the pro-convulsant effect of anandamide in pentylenetetrazole-induced seizures. Epilepsy Res 100:113–124. http://dx.doi.org/10.1016/j.eplepsyres.2012.02.003

  • Marinelli S, Di Marzo V, Florenzano F, Fezza F, Viscomi MT, van der Stelt M, Bernardi G, Molinari M, Maccarrone M, Mercuri NB (2007) N-arachidonoyl-dopamine tunes synaptic transmission onto dopaminergic neurons by activating both cannabinoid and vanilloid receptors. Neuropsychopharmacology 32:298–308

    Article  CAS  PubMed  Google Scholar 

  • McVey DC, Schmid PC, Schmid HH, Vigna SR (2003) Endocannabinoids induce ileitis in rats via the capsaicin receptor (VR1). J Pharmacol Exp Ther 304:713–722

    Article  CAS  PubMed  Google Scholar 

  • Medvedeva YV, Kim MS, Usachev YM (2008) Mechanisms of prolonged presynaptic Ca2+ signaling and glutamate release induced by TRPV1 activation in rat sensory neurons. J Neurosci 28:5295–5311

    Article  CAS  PubMed  Google Scholar 

  • Melck D, Bisogno T, De Petrocellis L, Chuang H, Julius D, Bifulco M, Di Marzo V (1999) Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors. Biochem Biophys Res Commun 262:275–284

    Article  CAS  PubMed  Google Scholar 

  • Micale V, Cristino L, Tamburella A, Petrosino S, Leggio GM, Drago F, Di Marzo V (2009) Anxiolytic effects in mice of a dual blocker of fatty acid amide hydrolase and transient receptor potential vanilloid type-1 channels. Neuropsychopharmacology 34:593–606

    Article  CAS  PubMed  Google Scholar 

  • Moran MM, McAlexander MA, Bíró T, Szallasi A (2011) Transient receptor potential channels as therapeutic targets. Nat Rev Drug Discov 10:601–620

    Article  CAS  PubMed  Google Scholar 

  • Musella A, De Chiara V, Rossi S, Prosperetti C, Bernardi G, Maccarrone M, Centonze D (2009) TRPV1 channels facilitate glutamate transmission in the striatum. Mol Cell Neurosci 40:89–97

    Article  CAS  PubMed  Google Scholar 

  • Nelson PL, Beck A, Cheng H (2011) Transient receptor proteins illuminated: current views on TRPs and disease. Vet J 187:153–164

    Article  CAS  PubMed  Google Scholar 

  • Nieri P, Martinotti E, Testai L, Adinolfi B, Calderone V, Breschi MC (2003) R+-methanandamide inhibits tracheal response to endogenously released acetylcholine via capsazepine-sensitive receptors. Eur J Pharmacol 459:75–81

    Article  CAS  PubMed  Google Scholar 

  • Panlilio LV, Mazzola C, Medalie J, Hahn B, Justinova Z, Drago F, Cadet JL, Yasar S, Goldberg SR (2009) Anandamide-induced behavioral disruption through a vanilloid-dependent mechanism in rats. Psychopharmacology 203:529–538

    Article  CAS  PubMed  Google Scholar 

  • Patil M, Patwardhan A, Salas MM, Hargreaves KM, Akopian AN (2011) Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology 61:778–788

    Article  CAS  PubMed  Google Scholar 

  • Patwardhan AM, Jeske NA, Price TJ, Gamper N, Akopian AN, Hargreaves KM (2006) The cannabinoid WIN 55,212-2 inhibits transient receptor potential vanilloid 1 (TRPV1) and evokes peripheral antihyperalgesia via calcineurin. Proc Natl Acad Sci U S A 103:11393–11398

    Article  CAS  PubMed  Google Scholar 

  • Pegorini S, Zani A, Braida D, Guerini-Rocco C, Sala M (2006) Vanilloid VR1 receptor is involved in rimonabant-induced neuroprotection. Br J Pharmacol 147:552–559

    Article  CAS  PubMed  Google Scholar 

  • Pertwee R, Griffin G, Hanus L, Mechoulam R (1994) Effects of two endogenous fatty acid ethanolamides on mouse vasa deferentia. Eur J Pharmacol 259:115–120

    Article  CAS  PubMed  Google Scholar 

  • Pertwee RG, Howlett AC, Abood ME, Alexander SP, Di Marzo V, Elphick MR, Greasley PJ, Hansen HS, Kunos G, Mackie K, Mechoulam R, Ross RA (2010) International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB1 and CB2. Pharmacol Rev 62:588–631

    Article  CAS  PubMed  Google Scholar 

  • Petrosino S, Cristino L, Karsak M, Gaffal E, Ueda N, Tüting T, Bisogno T, De Filippis D, D’Amico A, Saturnino C, Orlando P, Zimmer A, Iuvone T, Di Marzo V (2010) Protective role of palmitoylethanolamide in contact allergic dermatitis. Allergy 65:698–711

    Article  CAS  PubMed  Google Scholar 

  • Pollastro F, Taglialatela-Scafati O, Allarà M, Muñoz E, Di Marzo V, De Petrocellis L, Appendino G (2011) Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa). J Nat Prod 74:2019–2022

    Article  CAS  PubMed  Google Scholar 

  • Potenzieri C, Brink TS, Simone DA (2009) Excitation of cutaneous C nociceptors by intraplantar administration of anandamide. Brain Res 1268:38–47

    Article  CAS  PubMed  Google Scholar 

  • Price TJ, Patwardhan A, Akopian AN, Hargreaves KM, Flores CM (2004) Modulation of trigeminal sensory neuron activity by the dual cannabinoid-vanilloid agonists anandamide, N-arachidonoyl-dopamine and arachidonyl-2-chloroethylamide. Br J Pharmacol 141:1118–1130

    Article  CAS  PubMed  Google Scholar 

  • Puente N, Cui Y, Lassalle O, Lafourcade M, Georges F, Venance L, Grandes P, Manzoni OJ (2011) Polymodal activation of the endocannabinoid system in the extended amygdala. Nat Neurosci 14:1542–1547

    Article  CAS  PubMed  Google Scholar 

  • Qin N, Neeper MP, Liu Y, Hutchinson TL, Lubin ML, Flores CM (2008) TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons. J Neurosci 28:6231–6238

    Article  CAS  PubMed  Google Scholar 

  • Ramer R, Merkord J, Rohde H, Hinz B (2010a) Cannabidiol inhibits cancer cell invasion via upregulation of tissue inhibitor of matrix metalloproteinases-1. Biochem Pharmacol 79:955–966

    Article  CAS  PubMed  Google Scholar 

  • Ramer R, Rohde A, Merkord J, Rohde H, Hinz B (2010b) Decrease of plasminogen activator inhibitor-1 may contribute to the anti-invasive action of cannabidiol on human lung cancer cells. Pharm Res 27:2162–2174

    Article  CAS  PubMed  Google Scholar 

  • Ross RA (2003) Anandamide and vanilloid TRPV1 receptors. Br J Pharmacol 140:790–801

    Article  CAS  PubMed  Google Scholar 

  • Ross HR, Gilmore AJ, Connor M (2009) Inhibition of human recombinant T-type calcium channels by the endocannabinoid N-arachidonoyl dopamine. Br J Pharmacol 156:740–750

    Article  CAS  PubMed  Google Scholar 

  • Rossi F, Siniscalco D, Luongo L, De Petrocellis L, Bellini G, Petrosino S, Torella M, Santoro C, Nobili B, Perrotta S, Di Marzo V, Maione S (2009) The endovanilloid/endocannabinoid system in human osteoclasts: possible involvement in bone formation and resorption. Bone 44:476–484

    Article  CAS  PubMed  Google Scholar 

  • Rossi F, Bellini G, Luongo L, Torella M, Mancusi S, De Petrocellis L, Petrosino S, Siniscalco D, Orlando P, Scafuro M, Colacurci N, Perrotta S, Nobili B, Di Marzo V, Maione S (2011) The endovanilloid/endocannabinoid system: a new potential target for osteoporosis therapy. Bone 48:997–1007

    Article  CAS  PubMed  Google Scholar 

  • Roy A, Mandadi S, Fiamma MN, Rodikova E, Ferguson EV, Whelan PJ, Wilson RJ (2012) Anandamide modulates carotid sinus nerve afferent activity via TRPV1 receptors increasing response to heat. J Appl Physiol 112:212–224

    Article  CAS  PubMed  Google Scholar 

  • Rubino T, Realini N, Castiglioni C, Guidali C, Viganó D, Marras E, Petrosino S, Perletti G, Maccarrone M, Di Marzo V, Parolaro D (2008) Role in anxiety behavior of the endocannabinoid system in the prefrontal cortex. Cereb Cortex 18:1292–1301

    Article  CAS  PubMed  Google Scholar 

  • Ruparel NB, Patwardhan AM, Akopian AN, Hargreaves KM (2011) Desensitization of transient receptor potential ankyrin 1 (TRPA1) by the TRP vanilloid 1-selective cannabinoid arachidonoyl-2 chloroethanolamine. Mol Pharmacol 80:117–123

    Article  CAS  PubMed  Google Scholar 

  • Sagar DR, Smith PA, Millns PJ, Smart D, Kendall DA, Chapman V (2004) TRPV1 and CB(1) receptor-mediated effects of the endovanilloid/endocannabinoid N-arachidonoyl-dopamine on primary afferent fibre and spinal cord neuronal responses in the rat. Eur J Neurosci 20:175–184

    Article  PubMed  Google Scholar 

  • Saunders CI, Fassett RG, Geraghty DP (2009) Up-regulation of TRPV1 in mononuclear cells of end-stage kidney disease patients increases susceptibility to N-arachidonoyl-dopamine (NADA)-induced cell death. Biochim Biophys Acta 1792:1019–1026

    Article  CAS  PubMed  Google Scholar 

  • Schuelert N, McDougall JJ (2008) Cannabinoid-mediated antinociception is enhanced in rat osteoarthritic knees. Arthritis Rheum 58:145–153

    Article  CAS  PubMed  Google Scholar 

  • Sharkey KA, Cristino L, Oland LD, Van Sickle MD, Starowicz K, Pittman QJ, Guglielmotti V, Davison JS, Di Marzo V (2007) Arvanil, anandamide and N-arachidonoyl-dopamine (NADA) inhibit emesis through cannabinoid CB1 and vanilloid TRPV1 receptors in the ferret. Eur J Neurosci 25:2773–2782

    Article  CAS  PubMed  Google Scholar 

  • Silveira PE, Silveira NA, Morini Vde C, Kushmerick C, Naves LA (2010) Opposing effects of cannabinoids and vanilloids on evoked quantal release at the frog neuromuscular junction. Neurosci Lett 473:97–101

    Article  CAS  PubMed  Google Scholar 

  • Smart D, Jonsson KO, Vandevoorde S, Lambert DM, Fowler CJ (2002) ‘Entourage’ effects of N-acyl ethanolamines at human vanilloid receptors. Comparison of effects upon anandamide-induced vanilloid receptor activation and upon anandamide metabolism. Br J Pharmacol 136:452–458

    Article  CAS  PubMed  Google Scholar 

  • Starowicz K, Maione S, Cristino L, Palazzo E, Marabese I, Rossi F, de Novellis V, Di Marzo V (2007) Tonic endovanilloid facilitation of glutamate release in brainstem descending antinociceptive pathways. J Neurosci 27:13739–13749

    Article  CAS  PubMed  Google Scholar 

  • Starowicz K, Nigam S, Di Marzo V (2007) Biochemistry and pharmacology of endovanilloids. Pharmacol Ther 114:13–33

    Article  CAS  PubMed  Google Scholar 

  • Starowicz K, Makuch W, Osikowicz M, Piscitelli F, Petrosino S, Di Marzo V, Przewlocka B (2012) Spinal anandamide produces analgesia in neuropathic rats: possible CB(1)- and TRPV1-mediated mechanisms. Neuropharmacology 62(4):1746–1755

    Article  CAS  PubMed  Google Scholar 

  • Thomas A, Stevenson LA, Wease KN, Price MR, Baillie G, Ross RA, Pertwee RG (2005) Evidence that the plant cannabinoid Delta9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist. Br J Pharmacol 146:917–926

    Article  CAS  PubMed  Google Scholar 

  • Tóth A, Blumberg PM, Boczán J (2009) Anandamide and the vanilloid receptor (TRPV1). Vitam Horm 81:389–419

    Article  PubMed  CAS  Google Scholar 

  • Tóth BI, Dobrosi N, Dajnoki A, Czifra G, Oláh A, Szöllosi AG, Juhász I, Sugawara K, Paus R, Bíró T (2011) Endocannabinoids modulate human epidermal keratinocyte proliferation and survival via the sequential engagement of cannabinoid receptor-1 and transient receptor potential vanilloid-1. J Invest Dermatol 131:1095–1104

    Article  PubMed  CAS  Google Scholar 

  • Umathe SN, Manna SS, Jain NS (2012) Endocannabinoid analogues exacerbate marble-burying behavior in mice via TRPV1 receptor. Neuropharmacology 62:2024–2033

    Article  CAS  PubMed  Google Scholar 

  • Wang Y, Wang DH (2007) Increased depressor response to N-arachidonoyl-dopamine during high salt intake: role of the TRPV1 receptor. J Hypertens 25:2426–2433

    Article  CAS  PubMed  Google Scholar 

  • Wojtalla A, Herweck F, Granzow M, Klein S, Trebicka J, Huss S, Lerner R, Lutz B, Schildberg FA, Knolle PA, Sauerbruch T, Singer MV, Zimmer A, Siegmund SV (2012) The endocannabinoid N-arachidonoyl dopamine (NADA) selectively induces oxidative stress-mediated cell death in hepatic stellate cells, but not in hepatocytes. Am J Physiol Gastrointest Liver Physiol 302:G873–G887 doi:10.1152/agifi.00241.2011

    Article  CAS  PubMed  Google Scholar 

  • Woo DH, Jung SJ, Zhu MH, Park CK, Kim YH, Oh SB, Lee CJ (2008) Direct activation of transient receptor potential vanilloid 1(TRPV1) by diacylglycerol (DAG). Mol Pain 4:42

    Article  PubMed  CAS  Google Scholar 

  • Woudenberg-Vrenken TE, Bindels RJ, Hoenderop JG (2009) The role of transient receptor potential channels in kidney disease. Nat Rev Nephrol 5:441–449

    Article  CAS  PubMed  Google Scholar 

  • Yamada T, Ueda T, Shibata Y, Ikegami Y, Saito M, Ishida Y, Ugawa S, Kohri K, Shimada S (2010) TRPV2 activation induces apoptotic cell death in human T24 bladder cancer cells: a potential therapeutic target for bladder cancer. Urology 76:509.e1–509.e7

    Article  Google Scholar 

  • Zygmunt PM, Petersson J, Andersson DA, Chuang H, Sørgård M, Di Marzo V, Julius D, Högestätt ED (1999) Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide. Nature 400:452–457

    Article  CAS  PubMed  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Endocannabinoid Research Group, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Pozzuoli, NA, Italy

    Vincenzo Di Marzo

  2. Endocannabinoid Research Group, Institute of Cybernetics, Consiglio Nazionale delle Ricerche, Pozzuoli, NA, Italy

    Luciano De Petrocellis

Authors
  1. Vincenzo Di Marzo
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Luciano De Petrocellis
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Vincenzo Di Marzo .

Editor information

Editors and Affiliations

  1. , Anatomy and Cell Biology, Temple University School of Medicine, 3500 N. Broad Street, Philadelphia, 19140, Pennsylvania, USA

    Mary E. Abood

  2. National Institutes of Health, Division of Basic Neuroscience and Behav, National Institute on Drug Abuse, 6001 Executive Blvd, Bethesda, 20892, Maryland, USA

    Roger G Sorensen

  3. , Pharmacology and Psychiatry and Behavior, University of Washington, Box 357280, Seattle, 98195, Washington, USA

    Nephi Stella

Rights and permissions

Reprints and permissions

Copyright information

© 2013 Springer Science+Business Media New York

About this chapter

Cite this chapter

Di Marzo, V., De Petrocellis, L. (2013). Temperature-Sensitive Transient Receptor Potential Channels as Ionotropic Cannabinoid Receptors. In: Abood, M., Sorensen, R., Stella, N. (eds) endoCANNABINOIDS. The Receptors, vol 24. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-4669-9_8

Download citation

Publish with us

Policies and ethics

Search

Navigation