Vanilloid Reseptör 1 (VR1) (Capsaicin Reseptörü)

Vanilloid Reseptör-1, capsaicin ve capsaicine benzer etki oluşturabilen, ısı ve asit ile aktive olan bir iyon kanal reseptörüdür. Vanilloidlerin bağlandığı reseptörlere vanilloid reseptör denir. Vanilloidler ekzojen ve endojen olarak ikiye ayrılır. TRPV1 (Transient receptor potential vanilloid receptor-1) ilk olarak dorsal root, trigeminal ve nodos gangliyonlarda eksprese edilmiş, seçici olmayan iyon kanal proteinidir. Capsaicin’in spesifik olarak bağlandığı reseptöre capsaicin reseptörü ya da vanilloid reseptör 1 (TRPV1 ya da VR1) adı verilmiştir. VR1, 426 aminoasit içeren ve ~ 95 kDa ağırlığında bir proteindir. VR1, 430C’nin üzerindeki sıcaklıkta ve düşük pH’da (pH≤5) oluşan membran depolarizasyonu ve iyon kanallarının açılması sonucu capsaicin tarafından aktive edilir. VR1 ilk olarak santral sinir sistemindeki nöyronlarda ortaya konulmuştur. Ancak son zamanlarda yapılan çalışmalar VR1’in mast hücreleri, derideki keratinositler ve idrar kesesi epitel hücreleri gibi nöyron içermeyen çeşitli hücrelerde de bulunduğunu göstermiştir

Vanilloid Receptor

Vanilloid receptor-1 is a heat-and acid-activated ion channel receptor, which creates capsaicin and can create an effect like-capsaicin. Connected to vanilloid receptors are called vanilloid receptor. The vanilloids are divided to exogenous and endogenous. TRPV1 (transient receptor potential vanilloid receptor-1) is a nonselective ion channel protein that has firstly been expressed on dorsal root, trigeminal and nodos ganglia. The receptor which is connected specifically by capsaicin is called Capsaicin receptor or vanilloid receptor. VR1 is a ~ 95 kDa protein which includes 426 aminoacide. As a result of over 430C and low pH (pH≤5) ,VR1 is activated by capsaicin. Because at that time membrane is depolarized and ion channels are opened. VR1 was first shown in the neurons of the central nervous system. However, recent studies show that VR1 is expressed in non neuronal various cells; mast cells, keratinocytes in the skin and epithelial cells in the bladder .

___

  • Ahluwalia J, Urba´N.L., Capogna M., Bevans S., Nagy I., 2000. Cannabinoid 1 receptors are expressed in nociceptive primary sensory neu- rons. Neuroscience, 100: 685-688.
  • Anavi-Goffer S., Coutts A.A,2003. Cellular distri- bution of vanilloid VR1 receptor immunoreacti- vity in the Guinea-pig myenteric plexus. Euro- pean Journal of Pharmacology, 458: 61-71.
  • Avelino A., Dinis P., Charrua A., Nagy I., Yaqoob M., Cruz F., 2003. The endogenous TRPV1 li- gand anandamide increases in the rat inflamed ürinary bladder and may contribute to inflamma- tory pain. Social neuroscience, 33: 603-8,
  • Birder L.A., Kanai A.J., De Groat W.C., Kiss S., Nealen M.L., Burke N.E., Dineley K.E., Watkins S., Reynolds I.J., Caterina M.J., 2001. Vanilloid receptor expression suggests a sensory role for ürinary bladder epithelial cells. Proceedings of the National Academy of Sciences of the United States of America, 98: 13396-13401.
  • Caterina M.J., Schumacher M.A., Tominaga M., Rosen T.A., Levine J.D., Julius D.,1997. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature, 389: 816-824.
  • Caterina M.J., Julius D.,1999. Sense and spesifi- city: A molecular identity for nociceptors current opinionin. Neurobiology, 9: 525-530.
  • Caterina M.J., Leffler A., Malberg A.B., Martin W.J., Trafton J., Petersen-Zeitz K.R., Koltzen- burg M., Basbaum A.I., Julius D., 2000. İmpaired nociception and pain sensation in mice lacking the capsaicin receptor. Science, 288: 306-313.
  • Chuang H.H., Prescott E.D., Kong H., Shields S., Jordt S.E., Basbaum A.I., Chao M.V., Juliıus D., 2001. Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5)p2- mediated ınhibition. Nature, 411: 957-962.
  • Coderre T.J., Grimes R.W., Melzack R., 1986. Autotomy following sciatic and saphenous nerve sections: sparing of the medial toes after treat- ment of the sciatic nerve with capsaicin. Experi- mental Neurology, 91: 355-365.
  • Corey D.P., 2003. New trp channels in hearing and mechanosensation. Neuron, 39: 585- 588.
  • Davis J.B., Gray J., Gunthorpe M.J., Hatcher J.P., Davey P.T., Overend P., Harries M.H., Latcham J., Clapham C., Atkinson K., Hughes S.A., Rance K., Grau E., Harper A.J., Pugh P.L., Rogers D.C., Bıngham S., Randall A., Shear- down S.A., 2000. Vanilloid receptor-1 is essen- tial for ıinflammatory thermal hyperalgesia. Na- ture, 405: 183-187.
  • De Lago E., De Miguel R., Lastres-Becker I., Ramos J.A., Fernandez-Ruiz J., 2004. Involve- ment of vanilloid-like receptors in the effects of anandamide on motor behavior and nigrostriatal dopaminergic activity: ın vivo and ın vitro evi- dence. Brain Research, 1007: 152-159.
  • Ding Q.W., Zhang Y., Wang Y., Wang Y.N., Zhang L., Ding C., Wu L.L. and Yu G.Y., 2010. Functional vanilloid receptor-1 in human sub- mandibular glands, Journal of Dental Research, 89(7):711-716.
  • Dominquez R., Riboni L., 1971. failure of ovula- tion in autographed ovary of the hemispayed rat, Neuroendocrinology, 7: 164-170.
  • Dray A., 1992. Neuropharmacological mecha- nism of Capsaicin and related substances. Bioc- hemical Pharmacology, 44: 611-615.
  • Dvorakova M., Kummer W., 2001. Transient expression of vanilloid receptor subtype 1 in rat cardiomyocytes during development. Histoche- mistry and Cell Biology, 116: 223-225.
  • Erdost H., Özfiliz N., Özgüden C., Güneş N., Önen Ş., İlhan T., Özer A., 2007. Expression of a capsaicin receptor (VR1) in the testes of mice af- ter an application of capsaicin. Bulletin of the Ve- terinary Institute in Pulawy, 51, 649-653
  • Ferguson D.R., Kennedy I., Burton T.J., 1997. ATP is released from rabbit urinary bladder epit- helial cells by hydrostatic pressure changes—a possible sensory mechanism. The Journal of phy- siology, 505 (Pt. 2): 503-511.
  • Gepetti P., Trevısoni M., 2004. Activation and sensitisation of the vanilloid receptor: role in gastrointestinal ınflammation and fuction. British Journal of Pharmacology, 141: 1313-1320.
  • Gulbenkıan S., Barroso C.P., Cunha S.A, Ed- vinsson L., 1995. The peptidergic innervation of human coronary and cerebral vessels. Italian Jo- urnal of Anatomy and Embryology, 100 (Suppl 1): 317-327.
  • Gunthorpe M.J., Harries M.H., Prinjha R.K., Davis J.B., Randall A., 2000. Voltage- and time- depent properties of the recombinant rat vanilloid receeptor (rvr1). Journal of Physiology, 3: 747- 759.
  • Guo A., Vulchanova L., Wang J., Li X., Elde R., 1999. Immunocytochemical localization of the vanilloid receptor 1 (vr1): relationship to neuro- peptides, the p2x3 purinoceptor and ıb4 binding sites. The European Journal of Neuroscience, 11: 946-958.
  • Harada N., Okajima K., Uchiba M., Katsuragi T., 2003. Contribution of capsaicin-sensitive sensory neurons to stress-ınduced ıncreases in gastric tis- sue levels of prostaglandins in rats. American Jo- urnal of Physiology Gastrointestinal and Liver Physiology, 285: 1214-1224.
  • Huang Y., Wang D.H., 2001. Role of renin– angiotensin–aldosterone system in salt-sensitive hypertension ıinduced by sensory denervation. American Journal of Physiology Heart and Cir- culatory Physiology, 281: H2143-H2149.
  • Ichikawa H., Gouty S., Regalia J., Helke C.J., Sugimoto T., 2004. Ca(2+)/calmodulin- dependent protein kinase ıı in the rat cranial sen- sory ganglia. Brain Research, 1005: 36–43.
  • Inoue K., Koizumi S., Fuziwara S., Denda S., Inoue K., Denda M., 2002. Functional vanilloid receptors in cultured normal human epidermal keratinocytes. Biochemical and Biophysical Re- search Communications, 291: 124-129.
  • Karai L., Russell J.T., Iadarola M.J., Olah Z., 2004. Vanilloid receptor 1 regulates multiple cal- cium compartments and contributes to ca2+- induced ca2+-release in sensory neurons. The Jo- urnal of Biological Chemistry, 279: 16377- 16387.
  • Kato S., Aihara E., Nakamura A., Xin H., Matsui H., Kohama K., Takeuchi K., 2003. Expression of vanilloid receptors in rat gastric epithelial cells: role in cellular protection. Biochemical Pharmacology, 66: 1115- 1121.
  • Kilo S., Harding-Rosea C., Hargreavesa K.M., Flores C.M., 1997. Peripheral CGRP release as a marker for neurogenic ınflammation: a model system for the study of neuropeptide secretion in rat paw skin, Pain, 73: 201–207.
  • Kwak J.Y., Jung J.Y., Hwang S.W., Lee W.T., Oh U., A capsaicin receptor antagonist, capsaze- pine, reduces ınflammation-ınduced hyperalgesic responses in the rat: evidence for an endogenous capsaicin-like substance. Neuroscience, 86: 619- 626.
  • Liang Y.F., Haake B., Reeh P.W., Sustained sensitization and recruitment of rat cutaneous no- ciceptors by bradykinin and a novel theory of its excitatory action. The Journal of physiology, 523:
  • Lin W., Ogura T., Kinnaman S.C., 2002. Asid- activated cation currents in rat vallate taste recep- tor cells. Journal of Neurophysiology, 88: 133- 141.
  • Liu L., Simon S.A., 2001. Asidic stimuli activa- tes two distinct patways in taste receptor cells from rat fungiform papillae. Brain Research, 923: 58-70.
  • Lopez-Hernandez J., Oruna-Concha M.J., Simal- Lozane J., Gonzales-Castro M.J., Varquez- Blanco M.E., Determination of capsaicin and dihydrocapsaicin in cayenne pepper and pardon peppers by HPLC. Deutsche Lebenmittel- Rundschau, 92: 393- 395.
  • Maggi C.A., Santicioli P., Meli A., 1984. The effects of topical capsaicin on rat urinary bladder motility ın vivo. European Journal of Pharmaco- logy, 103: 41-50.
  • Maggi C.A, Lippe I.T., Giuliani S., Abelli L., Somma V., Geppetti P., Jancso´ G., Santicioli P., Meli A., 1989. Topical versus systemic capsaicin desensitization: specific and unspecific effects as ındicated by modification or reflex micturition in rats. Neuroscience 31: 745-756.
  • Marshall I.C., Owen D.E., Crıpps T.V., Davis J.B., Mcnulty S., Smart D., 2003. Activation of vanilloid receptor 1 by resiniferatoxin mobilizes calcium from ınositol 1, 4, 5-trisphosphate- sensitive stores. British Journal of Pharmaco- logy, 138: 172-176.
  • Mcıntyre P., Mclatchıe L.M., Chambers A., Phil- lips E., Clarke M., Savidge J., Toms C., Peacock M., Shah K., Winter J., Weerasakera N., Webb M., Rang H.P., Bevan S., Jamnes I.F., 2001. Pharmacological diferences between the human and rat vanilloid receptor 1 (vr1). British Journal of Pharmacology, 132:1084±1094ã.
  • Mezey E., Toth Z.E., Cortright D.N., Arzubi M.K., Krause J.E., Elde R., Guo A., Blumberg P.M., Szallasi A., 2000. Distribution of mRNA for vanilloid receptor subtype 1 (vr1), and vr1- like ıimmunoreactivity, in the central nervous system of the rat and human. Proceedings of the National Academy of Sciences of the United Sta- tes of America, 97: 3655-3660.
  • Moreniılla-Palao C., Planells-Cases R., Garcia- Sanz N., Ferrer-Montıel A., 2004. Regulated exocytosis contributes to protein kinase c poten- tiation of vanilloid receptor activity. The Journal of Biological Chemistry, 279: 25665-25672.
  • Nagy I, Rang H., 1999. Noxious heat activates all capsaicin-sensitive and also a subpopulation of capsaicin-insensitive dorsal root ganglion neu- rons. Neuroscience,88: 995-997.
  • Nagy I., S´antha P., Jancs´o G., Urb´an L., 2004. The role of the vanilloid (capsaicin) receptor (trpv1) in physiology and pathology. Europan Journal of Pharmacology, 500: 351-369.
  • Nathan J.D., Peng R.Y., Wang Y., Mcvey D.C., Vigna S.R., Lddle R.A., 2002. Primary sensory neurons: A common final pathway for ınflamma- tion in experimental pancreatitis in rats. Ameri- can Journal of Physiology Gastrointestinal and Liver Physiology, 283: 938-946.
  • Oliveros L., Forneris M., Aguado L., 2001. Sec- retion from neuropeptide-treated splenocytes modifies ovarian steroidogenesis. Medicina, 61: 35-39.
  • Olson L., Jones C.H., Jablonka-Shariff A., 1996. Nitric oxide decreases estradiol synthesis of rats luteinized ovarian cells: possible role for nitric oxide in functional luteal regression. Endocrino- logy, 137: 3531-3536.
  • Ost D., Roskams T., Van Der A.F., De Ridder D., 2002. Topography of the vanilloid receptor in the human bladder: more than just the nerve fi- bers. The Journal of Urology, 168: 293-297.
  • Pare M., Elde R., Mazurkiewicz J.E., Smith A.M., Rice F.L., 2001. The meissner corpuscle revised: a multiafferented mechanoreceptor with nociceptor ımmunochemical properties. The Jo- urnal of Neuroscience 21: 7236-7246.
  • Poonyachoti S., Kulkarni-Narla A., Brown D.R., 2002. Chemical coding of neurons expressing delta- and kappa-opioid receptor and type 1 va- nilloid receptor immunoreactivities in the porcine ıleum. Cell and Tissue Research, 307: 23-33.
  • Pothoulakis C., Castagliuolo I., Lamont J.T., Jaffer A., O’keane J.C., Snider R.M., Leeman S.E., 1994. CP-96,345, A substance p antagonist, ınhibits rat ıntestinal responses to clostridium dif- ficile toxin a but not cholera toxin. Proceedings of the National Academy of Sciences of the Uni- ted States of America, 91: 947-951.
  • Prescott E.D., Julius D., 2003. A modular PIP2 binding site as a determinant of capsaicin recep- tor sensitivity. Science, 300: 1284-1288.
  • Quartara L., Maggi C.A., 1998. The tachykinin Nk1 receptor: Part II. distribution and pathophy- siological roles. Neuropeptides, 32: 1-49.
  • Saeki T., Ohno T., Kamata K., Arai K., Mi- zuguchi S., Katori M., Saigenji K., Majima M.. 2004. Mild ırritant prevents ethanol-ınduced gast- ric mucosal microcirculatory disturbances thro- ugh actions of calcitonin gene-related peptide and PGL2 in rats. American Journal of Physiology Gastrointestinal and Liver Physiology, 286: 68- 75.
  • Smith M.S., Freeman M.E., Neill J.D., 1975. The control of progesterone secretion during the cycle and early pseudopregnancy. Endocrinology, 96: 219-226.
  • Sosa Z.Y., Casais M., Rastrilla A.M., Aguado L.I., 2000. Adrenergic ınfluences on coeliac ganglion affect the release of progesterone from cycling ovaries. Characterization of an ın vitro system. The Journal of Endocrinology, 166: 307- 318.
  • Southall M.D., Li T., Gharibova L.S., Pei Y., Nicol G.D., Travers J.B., 2003. Activation of epidermal vanilloid receptor-1 ınduces release of proinflammatory mediators in human keratinocy- tes. The Journal of Pharmacology and Experi- mental Therapeutics, 304: 217-222.
  • Sugiura T., Tominaga M., Katsuya H., Mizumura K., 2002. Bradykinin lowers the threshold tempe- rature for heat activation of vanilloid receptor 1. Journal of Neurophysiology, 88: 544- 548.
  • Szallasi A., Blumberg P.M., 1990. Resinifera- toxin and its analogs provide novel ınsights into the pharmacology of the vanilloid (capsaicin) re- ceptor. Life Science, 47: 1399- 1408.
  • Szallasi A., 1994. The vanilloid receptor: recep- tor types and species differences. General Phar- macology, 25(2): 223-43.
  • Szallasi A., Blumberg P.M., 1999. Vanilliod (capsaicin) receptors and mechanisms. Pharma- cological Reviews, 51: 159-211.
  • Szallasi A., 2001. Vanilloid receptor ligands: hopes and realities for the future. Drugs and Aging, 18: 561-573.
  • Szolcsa´nyı J., Mozsik G., 1984. Effects of cap- saicin on the development of gastric mucosal damage by different necrotizing agents and of gastric cytoprotection by PGL2 atropine and ci- metidine on rats. Acta Physiologica Hungarica, 64: 287-291.
  • Theriault E., Otsuka M., Jessel T., 1979. Capsai- cin-evoked release of Substance P from primary sensory neurones. Brain Research, 170: 209-213.
  • Tominaga M., Caterina M.J., Malmberg A.B., Rosen T.A., Gilbert H., Skinner K., Raumann B.E., Basbaum A.I., Julius D., 1998. The cloned capsaicin receptor ıntegrates multiple pain- producing stimuli. Neuron, 21: 531-543.
  • Tominaga M., Wada M., Masu M., 2001. Poten- tiation of capsaicin receptor activity by metabot- ropic atp receptors as a possible mechanism for atp-evoked pain and hyperalgesia. Proceedings of the National Academy of Sciences of the United States of America, 98: 6951-6956.
  • Traurig H.H., Saria A., Lembeck F., 1984. The effects of neonatal capsaicin treatment on growth and subsequent reproductive function in the rat. Naunyn-Schmiedeberg’s Archives of Pharmaco- logy, 327: 254-259.
  • Trujillo A., Morales L., Dominquez R., 2002. Effects of capsaicin administration into the bursa ovarica in the regulation of ovarion functions. The third five annual meeting of society for the study of reproduction. Baltimore, USA, July 28- 31, 2002. Biology of Reproduction, 66(272): 207.
  • Tütüncü Ş., Özfiliz N., 2010 Distribution of the vanilloid (capsaicin) receptor type 1 in the rat ovaries on different sexual development period. Revue De Medicine Veterinaire, 161, 6, 272-276.
  • Valtschanoff J.G., Rustioni A., Guo A., Hwang S.J., 2001. Vanilloid receptor VR1 is both presynaptic and postsynaptic in the superficial laminae of the rat dorsal horn. The Journal of Comparative Neurology, 436: 225-235.
  • Van Der A.F., Roskams T., Blyweert W., De Ridder D., 2003. İnterstitial cells in the human prostate: a new therapeutic target?, Prostate, 56: 250-255.
  • Vyklicky L., Lyfenko A., Kuffler D.P., Vlachova V., 2003. Vanilloid receptor TRPV1 is not acti- vated by vanilloids applied ıntracellularly. Neu- roreport, 14: 1061-1065.
  • Walker K.M., Urba´n L., Medhurst S.J., Patel S., Panesar M., Fox A.J., Mcintyre P., 2003. The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neu- ropathic pain. The Journal of Pharmacology and Experimental Therapeutics, 304: 56-62.
  • Ward S.M., Bayguınov J., Won K.J., Grundy D., Berthoud H.R., 2003. Distribution of the vanil- loid receptor (VR1) in the gastrointestinal tract. The Journal of Comparative Neurology, 465: 121-135.
  • Wang H.D., 2005. The vanilloid receptor and hypertension. Acta Pharmacologica Sinica 26(3):
  • Winter J,. Dray A., Wood J.N., Yeats J.C., Bevan S., 1990. Cellular mechanism of action of resini- feratoxin: a potent sensory neuron excitotoxin. Brain Research, 520: 131-140.
  • Zhang Y., Xiang B., Li Y., Wang Y., Wang X., Wang Y.N., Wu L., Yu G., 2006. Expression and characteristics of vanilloid receptor 1 in the rabbit submandibular gland. Biochemical and Biophysi- cal Research Communications. 345: 467-773.