Targeting TRP channels for pain relief

European Journal of Pharmacology

Volumn 716, Issue 1-3, 2013, Pages 61-76

  Brederson, Jill Desiree ^a   Kym, Philip R ^a   Szallasi, Arpad ^b  

^a ABBVIE INC   (United States)

^b MONMOUTH MEDICAL CENTER   (United States)

Author keywords

Capsaicin; Resiniferatoxin; ThermoTRP channels; TRPA1; TRPM8; TRPV1; TRPV3

Indexed keywords

CAPSAICIN; RESINIFERATOXIN; TRANSIENT RECEPTOR POTENTIAL CHANNEL; TRANSIENT RECEPTOR POTENTIAL CHANNEL A1; TRANSIENT RECEPTOR POTENTIAL CHANNEL AFFECTING AGENT; TRANSIENT RECEPTOR POTENTIAL CHANNEL M8; TRPA1 ANTAGONIST; TRPM8 ANTAGONIST; TRPV3 ANTAGONIST; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 3; VANILLOID RECEPTOR ANTAGONIST;

ALLODYNIA; ANALGESIA; CANCER PAIN; CHRONIC PAIN; COLD ALLODYNIA; CONCENTRATION RESPONSE; DIABETIC NEUROPATHY; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG STRUCTURE; DRUG TARGETING; HUMAN; INFLAMMATORY PAIN; MOLECULAR DYNAMICS; NEUROMODULATION; NEUROPATHIC PAIN; NONHUMAN; POSTHERPETIC NEURALGIA; PRIORITY JOURNAL; PROTEIN FUNCTION; RECEPTOR DOWN REGULATION; REVIEW; TREATMENT OUTCOME; VISCERAL PAIN;

CAPSAICIN; RESINIFERATOXIN; THERMOTRP CHANNELS; TRPA1; TRPM8; TRPV1; TRPV3;

ANIMALS; HUMANS; HYPERALGESIA; MOLECULAR TARGETED THERAPY; PAIN; TRANSIENT RECEPTOR POTENTIAL CHANNELS;

EID: 84892537978     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2013.03.003     Document Type: Review

References (192)

1. Aasvang, EK, Hansen, JB, Malmstrøm, J, Asmussen, T, Gennevois, D, Struys, MM, Kehlet, H., 2008. The effect of wound instillation of a novel purified capsaicin formulation on postherniotomy pain: a double-blind, randomized, placebocontrolled study. Anesth. Analg. 107, 282-291.
2. Anand, U, Otto, WR, Facer, P, Zebda, N, Selmer, I, Gunthorpe, MJ, Chessell, IP, Sinisi, M, Birch, R, Anand, P., 2008. TRPA1 receptor localisation in the human peripheral nervous system and functional studies in cultured human and rat sensory neurons. Neurosci. Lett. 438, 221-227.
3. Anand, U, Otto, WR, Anand, P., 2010. Sensitization of capsaicin and icilin responses in oxaliplatin treated adult rat DRG neurons. Mol. Pain 6, 82.
4. Asakawa, M, Yoshioka, T, Matsutani, T, Hikita, I, Suzuki, M, Oshima, I, Tsukahara, K, Arimura, A, Horikawa, T, Hirasawa, T, Sakata, T., 2006. Association of a mutation in TRPV3 with defective hair growth in rodents. J. Invest. Dermatol. 126, 2664-2672.
5. Athanasiou, A, Smith, PA, Vakilpour, S, Kumaran, NM, Turner AEm Bagiokou, D, Layfield, E, Ray, DE, Westwell, AD, Alexander, SP, Kendall, DA, Lobo, DN, Watson, SA, Lophatanon, A, Muir, KA, Guo, DA, Bates, TE., 2007. Vanilloid receptor agonists and antagonists are mitochondrial inhibitors: how vanilloids cause non-vanilloid receptor mediated cell death. Biochem. Biophys. Res. Commun. 354, 50-55.
6. Atoyan, R, Shander, D, Botchkareva, NV., 2008. Non-neuronal expression of transient receptor potential type A1 (TRPA1) in human skin. J. Invest. Dermatol. 129, 2312-2315.
7. Bang, S, Yoo, S, Yang, TJ, Cho, H, Hwang, SW., 2010. Farnesyl pyrophosphate is a novel pain-producing molecule via specific activation of TRPV3. J. Biol. Chem. 285, 19362-19375.
8. Bautista, DM, Jordt, SE, Nikai, T, Tsuruda, PR, Read, AJ, Poblete, J, Yamoah, EN, Basbaum, AI, Julius, D., 2006. TRPA1 mediates the inflammatory actions of environmental irritants and proalgesic agents. Cell 124, 1269-1282.
9. Bautista, DM, Siemens, J, Glazer, JM, Tsuruda, PR, Basbaum, AI, Stucky, CL, Jordt, SE, Julius, D., 2007. The menthol receptor TRPM8 is the principal detector of environmental cold. Nature 448, 204-208.
10. Berthelot DJ, Gijsen H, Zaja M, Rech J, Lebsack A, Xiao W, Breitenbucher J, Branstetter B. Preparation of Heterocyclic Amides as Modulators of TRPA1. WO141805, 2010.
11. Bevan S, Ganju P, McIntyre P, Patapoutian A, Peier A, Song C. Transient Receptor Potential Channel TRPV3 and Its Use. US7396910B2, 2009.
12. th, RW, 2002. cAMP-dependent protein kinase regulates desensitization of the capsaicin receptor VR1 by direct phosphorylation. Neuron 35, 721-731.
13. Bianchi, P, Ribet, V, Casas, C, Lejeune, O, Schmitt, AM, Redoulès, D., 2011. Analysis of gene expression in atopic dermatitis using a microabrasive method. J. Invest. Dermatol. 132, 469-472.
14. Bilodeau, M.T., Egbertson, M., Green, A., Li, Y., Hartnett, J.C. Novel TRPA1 Antagonists for the Treatment of Pain and Other TRPA1-associated diseases. WO 043954, 2011.
15. Binder, A, May, D, Baron, R, Maier, C, Tölle, TR, Treede, RD, Berthele, A, Faltraco, F, Flor, H, Gierthmühlen, J, Haenisch, S, Huge, V, Magerl, W, Maihöfner, C, Richter, H, Rolke, R, Scherens, A, Uçeyler, N, Ufer, M, Wasner, G, Zhu, J, Cascorbi, I., 2011. Transient receptor potential channel polymorphisms are associated with the somatosensory function in neuropathic pain patients. PLoS One 6, e17387.
16. Bishnoi, M, Premkumar, LS., 2012. Changes in TRP channel expression in painful conditions. Open Pain J., Epub ahead of print.
17. Bley, K., 2012. Effects of topical capsaicin on cutaneous innervation: implications for pain management. Open Pain J., Epub ahead of print.
18. Bodding, M, Wissenbach, U, Flockerzi, V., 2007. Characterisation of TRPM8 as a pharmacophore receptor. Cell Calcium 42, 618-628.
19. Borbíró, I, Lisztes, E, Tóth, BI, Czifra, G, Oláh, A, Szöllosi, AG, Szentandrássy, N, Náná si, PP, Péter, Z, Paus, R, Kovács, L, Bíró, T., 2011. Activation of transient receptor potential vanilloid-3 inhibits human hair growth. J. Invest. Dermatol. 131, 1605-1614.
20. Bölcskei, K, Helyes, Z, Szabó, A, Sándor, K, Elekes, K, Németh, J, Almási, R, Pintér, E, Pethö, G, Szolcsányi, J., 2005. Investigation of the role of TRPV1 receptors in acute and chronic nociceptive processes using gene-deficient mice. Pain 117, 368-376.
21. Branum, ST, Colburn, RW, Dax, SL, Flores, CM, Jetter, MC, Liu, Y, Ludovici, D, Macielag, MJ, Matthews, JM, Mcnally, JJ, Reaney, LM, Russell, RK, Qin, N, Wells, KM, Youells, SC, Youngman, MA., 2009. N-benzothienyl sulfonamides as TRPM8 modulators and their preparation, pharmaceutical compositions and use in the treatment of diseases. Chem. Abstr. 150, 168153.
22. Brederson, JD, Chu, KL, Reilly, RM, Brown, BS, Kym, PR, Jarvis, MF, McGaraughty, S., 2012. TRPV1 antagonist, A-889425, inhibits mechanotransmission in a subclass of rat primary afferent neurons following peripheral inflammation. Synapse 66, 187-195.
23. Brown, DC, Iadarola, MJ, Perkowski, SZ, Erin, H, Shofer, F, Laszlo, KJ, Olah, Z, Mannes, AJ., 2005. Physiologic and antinociceptive effects of intrathecal resiniferatoxin in a canine bone cancer model. Anesthesiology 103, 1052-1059.
24. Calvo, RR, Meegalla, SK, Parks, DJ, Parsons, WH, Ballentine, SK, Lubin, ML, Schneider, C, Colburn, RW, Flores, CM, Player, MR., 2012. Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia. Bioorg. Med. Chem. Lett. 22, 1903-1907.
25. Caspani, O, Zurborg, S, Labuz, D, Heppenstall, PA., 2009. The contribution of TRPM8 and TRPA1 channels to cold allodynia and neuropathic pain. PLoS One 4, e7383.
26. Caterina, MJ, Julius, D., 2001. The vanilloid receptor: a molecular gateway to the pain pathway. Annu. Rev. Neurosci. 24, 487-517.
27. Caterina, MJ, Schumacher, MA, Tominaga, M, Rosen, TA, Levine, JD, Julius, D., 1997. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature 389, 816-824.
28. Caterina, MJ, Leffler, A, Malmberg, AB, Martin, WJ, Trafton, J, Petersen-Zeitz, KR, Koltzenburg, M, Basbaum, AI, Julius, D., 2000. Impaired nociception and pain sensation in mice lacking the capsaicin receptor. Science 288, 306-313.
29. Chaudhari, S, Thomas, A, Kadam, A, Dhone, S, Kadam, S, Khairatkar-Joshi, N, Kattige, V., 2010a. Preparation of Fused Imidazole Carboxamides as Therapeutic TRPV3 Modulators. US 0152192.
30. Chaudhari S, Thomas A, Kadam A, Dhone S, Adik B, Khairatkar-Joshi N, Kattige V. Chromenone Derivatives as TRPV3 Antagonists and their Preparation and Use for the Treatment of Diseases. WO 055384, 2010b.
31. Chaudhari, S, Kumar, S, Thomas, A, Patil, NP, Kadam, AB, Deshmukh, VG, Dhone, SV, Chikhale, RP, Khairatkar-Joshi, N, Mukhopadhyay, I., 2010c. Fused pyrimidinedione derivatives as TRPA1 modulators and their preparation and use for the treatment and prevention of TRPA1-mediated diseases. PCT Appl., WO/2010/109287.
32. Chaudhari, SS, Kumar, S, Thomas, A, Patil, NP, Kadam, AB, Waghmare, NT, Nayan, T, Khairatkar-Joshi, N, Mukhopadhyay, I., 2011. Preparation of amides of heterocyclic compounds as TRPA1 inhibitors. PCT Appl., WO/2011/114184.
33. Chen, J, Joshi, SK, DiDomenico, S, Perner, RJ, Mikusa, JP, Gauvin, DM, Segreti, JA, Han, P, Zhang, XF, Niforatos, W, Bianchi, BR, Baker, SJ, Zhong, C, Simler, GH, McDonald, HA, Schmidt, RG, McGaraughty, SP, Chu, KL, Faltynek, CR, Kort, ME, Reilly, RM, Kym, PR., 2011. Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation. Pain 152, 1165-1172.
34. Cheng, X, Jin, J, Hu, L, Shen, D, Dong, X, Samie, MA, Knoff, J, Eisinger, B, Liu, M, Huang, SM, Caterina, MJ, Dempsey, P, Michael, LE, Dlugosz, AA, Andrews, NC, Clapham, DE, Xu, H.TRP, 2010. Channel regulates EGFR signaling in hair morphogenesis and skin barrier formation. Cell 141, 331-343.
35. Chizh, BA, O'Donnell, MB, Napolitano, A, Wang, J., 2007. The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans. Pain 132, 132-141.
36. Chong, JA, Fanger, C, Moran, MM, Underwood, DJ, Zhen, X, Ripka, A, Weigele, M, Lumma Jr, WC, Larsen, GR., 2006. Compounds for modulating TRPV3 function. PCT Appl., WO/2006/122156.
37. Chong, JA, Fanger, C, Larsen, GR, Lumma Jr, WC, Moran, MM, Ripka, A, Underwood, DJ, Weigele, M, Zhen, X, Mahadevan, A, Meltzer, P., 2007. Compounds for modulating TRPV3 function. PCT Appl., WO/2007/056124.
38. Chuang, HH, Prescott, ED, Kong, H, Shields, S, Jordt, SE, Basbaum, AI, Chao, MV, Julius, D., 2001. Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5)P2-mediated inhibition. Nature 411, 957-962.
39. Chung, MK, Lee, H, Mizuno, A, Suzuki, M, Caterina, MJ., 2004a. 2- Aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J. Neurosci. 24, 5177-5182.
40. Chung, MK, Lee, H, Mizuno, A, Suzuki, M, Caterina, MJ., 2004b. TRPV3 and TRPV4 mediate warmth evoked currents in primary mouse keratinocytes. J. Biol. Chem. 279, 21569-21575.
41. Chung, MK, Güler, AD, Caterina, MJ., 2005. Biphasic currents evoked by chemical or thermal activation of the heat-gated ion channel, TRPV3. J. Biol. Chem. 280, 15928-15941.
42. Colburn, RW, Lubin, ML, Stone Jr., DJ, Wang, Y, Lawrence, D, D'Andrea, MR, Brandt, MR, Liu, Y, Flores, CM, Qin, N., 2007. Attenuated cold sensitivity in TRPM8 null mice. Neuron 54, 379-386.
43. Colburn RW, Dax SL, Flores C, Matthews J. Cold Menthol Receptor Antagonists. US0053347; 2012.
44. Corey, DP, García-Añoveros, J, Holt, JR, Kwan, KY, Lin, SY, Vollrath, MA, Amalfitano, A, Cheung, EL, Derfler, BH, Duggan, A, Géléoc, GS, Gray, PA, Hoffman, MP, Rehm, HL, Tamasauskas, D, Zhang, DS., 2004. TRPA1 is a candidate for the mechanosensitive transduction channel of vertebrate hair cells. Nature 432, 723-730.
45. Cui, M, Honore, P, Zhong, C, Gauvin, D, Mikusa, J, Hernandez, G, Chandran, P, Gomtsyan, A, Brown, B, Bayburt, EK, Marsh, K, Bianchi, B, McDonald, H, Niforatos, W, Neelands, R, Moreland, BB, Decker, MW, Lee, CH, Sullivan, JP, Feltynek, CR., 2006. TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J. Neurosci. 26, 9385-9393.
46. Cuypers, E, Yanagihara, A, Karlsson, E, Tytgat, J., 2006. Jellyfish and other cnidarian envenomations cause pain by affecting TRPV1 channels. FEBS Lett. 580, 5728-5732.
47. Davis, JB, Gray, J, Gunthorpe, MJ, Hatcher, JP, Davey, PT, Overend, P, Harries, MH, Latcham, J, Clapham, C, Atkinson, K, Hughes, SA, Rance, K, Grau, F, Harper, AJ, Pugh, PL, Rogers, DC, Bingham, S, Randall, A, Sheardown, SA., 2000. Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia. Nature 405, 183-187.
48. DeFalco, J, Duncton, MAJ, Emerling, D., 2011. TRPM8 biology and medicinal chemistry. Curr. Top. Med. Chem. 11, 2237-2252.
49. Dhaka, A, Murray, AN, Mathur, J, Earley, TJ, Petrus, MJ, Patapoutian, A., 2007. TRPM8 is required for cold sensation in mice. Neuron 54, 371-378.
50. Dhaka, A, Earley, TJ, Watson, J, Patapoutian, A, 2008. Visualizing cold spots: TRPM8-expressing sensory neurons and their projections. J. Neurosci. 28, 566-575.
51. Eid, SR., 2011. Therapeutic targeting of TRP channels: the TR(i)P to pain relief. Curr. Top. Med. Chem. 11, 2118-2130.
52. Facer, P, Casula, MA, Smith, GD, Benham, CD, Chessell, IP, Bountra, C, Sinisi, M, Birch, R, Anand, P., 2007. Differential expression of the capsaicin receptor TRPV1 and related novel receptors TRPV3, TRPV4 and TRPM8 in normal human tissues and changes in traumatic and diabetic neuropathy. BMC Neurol. 7, 11-22.
53. Fernández-Peña, C, Viana, F., 2012. Targeting TRPM8 for pain relief. Open Pain J., Epub ahead of print.
54. Frederick, J, Buck, ME, Matson, DJ, Cortright, DN., 2007. Increased TRPA1, TRPM8, and TRPV2 expression in dorsal root ganglia by nerve injury. Biochem. Biophys. Res. Commun. 358, 1058-1064.
55. Frank R, Bahrenberg G, Christoph T, Schiene K, DeVry J, Damann N, Frormann S, Lesch B, Lee J, Kim Y-S, Kim M-S. PCT Int. Appl. WO 2010/127855.
56. Fuller, RW, Dixon, CM, Barnes, PJ., 1985. Bronchoconstrictor response to inhaled capsaicin in humans. J. Appl. Physiol. 58, 1080-1084.
57. Garrison, SR, Stucky, CL., 2011. The dynamic TRPA1 channel: a suitable pharmacological pain target? Curr. Pharm. Biotechnol. 12, 1689-1697.
58. Gavva, NR, Bannon, AW, Hovland Jr., DN, Lehto, SG, Klionsky, L, Surapaneni, S, Immke, DC, Henley, C, Arik, L, Bak, A, Davis, J, Ernst, N, Haver, G, Kuang, R, Shi, L, Tamir, R, Wang, J, Wang, W, Zajic, G, Zhu, D, Norman, MH, Louis, JC, Magal, E, Treanor, JJ., 2007a. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J. Pharmacol. Exp. Ther. 323, 128-137.
59. Gavva, NR, Bannon, AW, Surapaneni, S, Teanor, JJ., 2007b. The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J. Neurosci. 27, 3366-3374.
60. Gavva, NR, Treanor, JJ, Garami, A, Fang, L, Surapaneni, S, Akrami, A, Alvarez, F, Bak, A, Darling, M, Gore, A, Jang, GR, Kesslak, JP, Ni, L, Norman, MH, Palluconi, G, Rose, MJ, Salfi, M, Tan, E, Romanovsky, AA, Banfield, C, Davar, G., 2008. Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. Pain 136, 202-210.
61. Gavva, NR, Davis, C, Lehto, SG, Rao, S, Wang, W, Zhu, DX., 2012. Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Mol. Pain 8, 36-41.
62. Gharat, L, Szallasi, A., 2008. Advances in the design and therapeutic use of capsaicin receptor TRPV1 agonists and antagonists. Exp. Opin. Ther. Patents 18, 159-209.
63. Gentry, C, Stoakley, N, Andersson, DA, Bevan, S., 2010. The roles of iPLA2, TRPM8 and TRPA1 in chemically-induced cold hypersensitivity. Mol. Pain 6, 4-11.
64. Gijsen, H, Berthelot, D, De Cleyn, M., 2009. 3,4-Dihydropyrimidine derivatives as TRPA1 antagonists and their preparation, pharmaceutical compositions and use in the treatment of disease. WO 147079.
65. Gopinath, P, Wan, E, Holdcroft, A, Facer, P, Davis, JB, Smith, GD, Bountra, C, Anand, P., 2005. Increased capsaicin receptor TRPV1 in skin nerve fibres and related vanilloid receptors TRPV3 and TRPV4 in keratinocytes in human breast pain. BMC Womens Health 5, 2-10.
66. Guatteo, E, Chung, KK, Bowala, TK, Bernardi, G, Mercuri, NB, Lipski, J., 2005. Temperature sensitivity of dopaminergic neurons of the substantia nigra pars compacta: involvement of transient receptor potential channels. J. Neurophysiol. 94, 3069-3080.
67. Gullapali, S, Thomas, A, Chaudhari, SS, Lingam, VSRL, Kattige, V, Gudi, GS, Godsafe, Z, Maharaj, N, Ward, P, Khairatkar-Joshi, N., 2010. GRC 15300 - A Novel, Selective, Orally Active TRPV3 Antagonist in Clinical Trial for Potential Treatment of Chronic Inflammatory and Neuropathic Pain. World Pharmaceutical Congress. Cambridge Healthtech Institute, Philadephia, PA.
68. Haeseler, G, Maue, D, Grosskreutz, J, Bufler, J, Nentwig, B, Piepenbrock, S, Dengler, R, Leuwer, M., 2002. Voltage-dependent block of neuronal and skeletal muscle sodium channels by thymol and menthol. Eur. J. Anaesthesiol. 19, 571-579.
69. Hamamoto, T, Takumida, M, Hirakawa, K, Tatsukawa, T, Ishibashi, T., 2009. Localization of transient receptor potential vanilloid (TRPV) in the human larynx. Acta Otolaryngol. 129, 560-568.
70. Hamamoto, T, Takumida, M, Hirakawa, K, Takeno, S, Tatsukawa, T., 2008. Localization of transient receptor potential channel vanilloid subfamilies in the mouse larynx. Acta Otolaryngol. 128, 685-693.
71. Hu, HZ, Gu, Q, Wang, C, Colton, CK, Tang, J, Kinoshita-Kawada, M, Lee, LY, Wood, J.D, Zhu, MX., 2004. 2-Aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3. J. Biol. Chem. 279, 35741-35748.
72. Hu, HZ, Xiao, R, Wang, C, Gao, N, Colton, CK, Wood, JD, Zhu, MX., 2006. Potentiation of TRPV3 channel function by unsaturated fatty acids. J. Cell. Physiol. 208, 201-212.
73. Huang, SM, Lee, H, Chung, MK, Park, U, Yu, YY, Bradshaw, HB, Coulombe, PA, Walker, JM, Caterina, MJ., 2008. Overexpressed transient receptor potential vanilloid 3 ion channels in skin keratinocytes modulate pain sensitivity via prostaglandin E2. J. Neurosci. 28, 13727-13737.
74. Huang, SM, Li, X, Yu, Y, Wang, J, Caterina, MJ., 2011. TRPV3 and TRPV4 ion channels are not major contributors to mouse heat sensation. Mol. Pain 17 (7), 37.
75. Iadarola, MJ, Mannes, AJ., 2011. The vanilloid agonist resiniferatoxin for interventional-based pain control. Curr. Top. Med. Chem. 11, 2171-2179.
76. Iadarola, MJ, Gonnella, GL., 2012. Resiniferatoxin for pain treatment: an interventional approach to personalized pain medicine. Open Pain J., Epub ahead of print.
77. Immke, DC, Gavva, NR., 2006. The TRPV1 receptor and nociception. Semin. Cell Dev. Biol. 17, 582-591.
78. Imura, K, Yoshioka, T, Hikita, I, Tsukahara, K, Hirasawa, T, Higashino, K, Gahara, Y, Arimura, A, Sakata, T., 2007. Influence of TRPV3 mutation on hair growth cycle in mice. Biochem. Biophys. Res. Commun. 363, 479-483.
79. Imura, K, Yoshioka, T, Hirasawa, T, Sakata, T., 2009. Role of TRPV3 in immune response to development of dermatitis. J. Inflamm. (Lond) 25, 6-17.
80. Irlapati, NR, Thomas, A, Kurhe, DK, Shelke, SY, Khairatkar-Joshi, N, Viswanadha, S, Mukhopadhyay, I., 2010. Preparation of fused oxazole and thiazole derivatives as TRPM8 modulators. Chem. Abstr. 152, 192106.
81. Ji, G, Zhou, S, Carlton, SM., 2008. Intact a delta-fibers up-regulate transient receptor potential A1 and contribute to cold hypersensitivity in neuropathic rats. Neuroscience 154, 1054-1066.
82. Jones, VM, Moore, KA., Peterson, DM., 2011. Capsaicin 8% patch (Qutenza) - a review of the evidence. J. Pain Palliat Care Pharmacother 25, 32-41.
83. 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.
84. 2+/calmodulin- dependent kinase II regulates its vanilloid binding. J. Biol. Chem. 279, 7048-7054.
85. Karai L, Brown DC, Mannes AJ, Conelly ST, Brown J, Gandal M, Wellisch OM, Neubert JK, Olah Z, Iadarola MJ. Deletion of vanilloid receptor 1-expressing primary afferent neurons for pain control. J. Clin. Invest. 113:1344-1352.
86. Karashima, Y, Talavera, K, Everaerts, W, Janssens, A, Kwan, KY, Vennekens, R, Nilius, B, Voets, T., 2009. TRPA1 acts as a cold sensor in vitro and in vivo. Proc. Nat. Acad. Sci. U.S.A. 106, 1273-1278.
87. Kasama, S, Kawakubo, M, Suzuki, T, Nishizawa, T, Ishia, A, Nakayama, J., 2007. RNA interference-mediated knock-down of transient receptor potential vanilloid 1 prevents forepaw inflammatory hyperalgesia in rat. Eur. J. Neurosci. 25, 2956-2963.
88. Kennedy, WR, Vanhove, GF, Lu, SP, Tobias, J, Bley, KR, Walk, D, Wendelschafer-Crabb, G, Simone, DA, Selim, MM., 2010. A randomized, controlled, open-label study of the long-term effects of NGX-4010, a high-concentration capsaicin patch, on epidermal nerve fiber density and sensory function in healthy volunteers. J. Pain 11, 579-587.
89. Kim, YS, Son, JY, Kim, TH, Paik, SK, Dai, Y, Noguchi, K, Ahn, DK, Bae, YC., 2010. Expression of transient receptor potential ankyrin 1 (TRPA1) in the rat trigeminal sensory afferents and spinal dorsal horn. J. Comp. Neurol. 518, 687-698.
90. Kissin, I., 2008. Vanilloid-induced conduction analgesia, selective, long-lasting, dose-dependent, with a low level of potential neurotoxicity. Anesth. Analg. 107, 261-271.
91. Kissin, I, Szallasi, A., 2011. Therapeutic targeting of TRPV1 by resiniferatoxin, from preclinical studies to clinical trials. Curr. Top. Med. Chem. 11, 2159-2170.
92. Kissin, Bright CA, Bradley Jr., EL, 2002. Selective and long-lasting blockade with resiniferatoxin prevents inflammatory pain hypersensitivity. Anesth. Analg. 94, 1253-1258.
93. Kissin, EY, Freitas, CF, Kissin, I., 2005b. The effects of intraarticular resiniferatoxin in experimental knee-joint arthritis. Anesth. Analg. 101, 1433-1439.
94. Kissin, I, Davison, N, Bradley Jr., EL, 2005a. Perineural resiniferatoxin prevents hyperalgesia in a model of postoperative pain. Anesth. Analg. 10, 774-780.
95. Klein, AH, Sawyer, CM, Carstens, MI, Tsagareli, MG, Tsiklauri, N, Carstens, E., 2010. Topical application of L-menthol induces heat analgesia, mechanical allodynia, and a biphasic effect on cold sensitivity in rats. Behav. Brain Res. 212, 179-186.
96. Knowlton, WM, Bifolck-Fisher, A, Bautista, DM, McKemy, DD., 2010. TRPM8, but not TRPA1, is required for neural and behavioral responses to acute noxious cold temperatures and cold-mimetics in vivo. Pain 150, 340-350.
97. Knowlton, WM, Daniels, RL, Palkar, R, McCoy, DD, McKemy, DD., 2011. Pharmacological blockade of TRPM8 ion channels alters cold and cold pain responses in mice. PLoS, e25894.
98. Kobayashi, K, Fukuoka, T, Obata, K, Yamanaka, H, Dai, Y, Tokunaga, A, Noguchi, K., 2005. Distinct expression of TRPM8, TRPA1, and TRPV1 mRNAs in rat primary afferent neurons with adelta/c-fibers and colocalization with trk receptors. J. Comp. Neurol. 26, 596-606.
99. Koivisto, A, Hukkanen, M, Saarnilehto, M, Chapman, H, Kuokkanen, K, Wei, H, Viisanen, H, Akerman, KE, Lindstedt, K, Pertovaara, A., 2012. Inhibiting TRPA1 ion channel reduces loss of cutaneous nerve fiber function in diabetic animals: sustained activation of the TRPA1 channel contributes to the pathogenesis of peripheral diabetic neuropathy. Pharmacol. Res. 65, 149-158.
100. Kort, ME, Kym, PR., 2012. TRPV1 antagonists: clinical setbacks and prospects for future development. Prog. Med. Chem. 51, 57-70.
101. Krarup, AL, Ny, L, Astrand, M, Bajor, A, Hvid-Jensen, F, Hansen, MB, Simren, M, Funch-Jensen, P, Drewes, AM., 2011. Randomized clinical trial: the efficacy of the transient receptor potential vanilloid 1 antagonist AZD1386 in human oesophageal pain. Aliment. Pharmacol. Ther. 33, 1113-1122.
102. Kremeyer, B, Lopera, F, Cox, JJ, Momin, A, Rugiero, F, Marsh, S, Woods, CG, Jones, NG, Paterson, KJ, Fricker, FR, Villegas, A, Acosta, N, Pineda-Trujillo, NG, Ramírez, JD, Zea, J, Burley, MW, Bedoya, G, Bennett, DL, Wood, JN, Ruiz-Linares, A., 2010. A gain-of-function mutation in TRPA1 causes familial episodic pain syndrome. Neuron 66, 671-680.
103. Kumar, S, Thomas, A, Margal, S, Khairatkar-Joshi, N, Mukhopadhyay, I., 2010a. Preparation of isothiazolo-pyrimidinedione derivatives as TRPA1 modulators. PCT Appl., WO/2010/109328.
104. Kumar, S, Thomas, A, Waghmare, NT, Margal, S, Khairatkar-Joshi, N, Mukhopadhyay, I., 2010b. Preparation of thieno-pyrimidinedione derivatives as TRPA1 modulators. PCT Appl., WO/2010/109334.
105. Lai-Cheong, JE, Sethuraman, G, Ramam, M, Stone, K, Simpson, MA, McGrath, JA., 2012. Recurrent heterozygous missense mutation, p.Gly573Ser, in the TRPV3 gene in an Indian boy with sporadic Olmsted syndrome. Br. J. Dermatol. 167, 440-442.
106. Lam, PM, McDonald, J., Lambert, DG., 2005. Characterization and comparison of recombinant human and rat TRPV1 receptors: effects of exo- and endocannabinoids. Br. J. Anaesth. 94, 649-656.
107. Lashinger, ES, Steiginga, MS, Hieble, JP, Leon, LA, Gardner, SD, Nagilla, R, Davenport, EA, Hoffman, BE, Laping, NJ, Su, X.AMTB, 2008. A TRMP8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome. Am. J. Physiol. Ren. Physiol. 295, F803-F810.
108. Lauria, G, Morbin, M, Lombardi, R, Capobianco, R, Camozzi, F, Pareyson, D, Manconi, M, Geppetti, P., 2006. Expression of capsaicin receptor immunoreactivity in human peripheral nervous system and in painful neuropathies. J. Peripher. Nerv. Syst. 11, 262-271.
109. Lehto, SG, Tamir, R, Deng, H, Klionsky, L, Kuang, R, Le, A, Lee, D, Louis, JC, Magal, E, Manning, BH, Rubino, J, Surapaneni, S, Tamayo, N, Wang, T, Wang, J, Youngblood, B, Zhang, M, Zhu, D, Norman, MH, Gavva, N., 2008. Antihyperalgesic effects of (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2- (piperidin-1- yl)-4-(trifluorom ethyl)phenyl)-acrylamide (AMG8562), a novel transient receptor potential vanilloid type 1 modulator that does not cause hyperthermia in rats. J. Pharmacol. Exp. Ther. 326, 218-229.
110. Liang, J, Ji, Q, Ji, W., 2011. Role of transient receptor potential ankyrin subfamily member 1 in pruritus induced by endothelin-1. Neurosci. Lett. 492, 175-178.
111. Lin, Z, Chen, Q, Lee, M, Cao, X, Zhang, J, Ma, D, Chen, L, Hu, X, Wang, H, Wang, X, Zhang, P, Liu, X, Guan, L, Tang, Y, Yang, H, Tu, P, Bu, D, Zhu, X, Wang, K, Li, R, Yang, Y., 2012. Exome sequencing reveals mutations in TRPV3 as a cause of Olmsted syndrome. Am. J. Hum. Genet. 90, 558-564.
112. Lindemann, J, Tsakiropoulou, E, Scheithauer, MO, Konstantinidis, I, Wiesmiller, KM., 2008. Impact of menthol on nasal mucosal temperature and nasal patency. Am. J. Rhinol. 22, 402-405.
113. Lingam, VSP, Abraham, T, More, DA, Khatik, JY, Khairatkar-Joshi, N, Kattige, VG., 2009A. Fused pyrimidine derivatives as TRPV3 modulators. PCT Appl., WO/2009/109987.
114. Lingam, VSP, Thomas, A, More, D, Khatik, J, Khairatkar, J, Kattige, V., 2009B. Preparation of fused pyrimidine derivatives as TRPV3 modulators. WO 109987.
115. Lingam, VSP, Thomas, A, Phatangare, S, Mindhe, A, Khatik, J, Khairatkar-Joshi, N, Kattige, V., 2010. Preparation of fused imidazole derivatives as TRPV3 antagonists useful in treatment and prevention of TRPV3 receptor-mediated diseases. WO 073128.
116. 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 μ- opioid receptors in the descending antinociceptive pathway activates glutamate transmission and induces analgesia. J. Neurophysiol. 101, 2411-2422.
117. Malmberg, AB, Mizisin, AP, Calcutt, NA, von Stein, T, Robbins, WR, Bley, KR., 2004. Reduced heat sensitivity and epidermal nerve fiber immunostaining following single applications of a high-concentration capsaicin patch. Pain 111, 360-367.
118. Mandadi, S, Roufogalis, BD., 2008. ThermoTRP channels in nociceptors: taking a lead from the capsaicin receptor TRPV1. Curr. Neuropharmacol. 6, 21-38.
119. Mandadi, S, Sokabe, T, Shibasaki, K, Katanosaka, K, Mizuno, A, Moqrich, A, Patapoutian, A, Fukumi-Tominaga, T, Mizumura, K, Tominaga, M., 2009. TRPV3 in keratinocytes transmits temperature information to sensory neurons via ATP. Pfluger's Arch. 458, 1093-1102.
120. Materazzi, S, Fusi, C, Benemei, S, Pedretti, P, Patacchini, R, Nilius, B, Prenen, J, Creminon, C, Geppetti, P, Nassini, R., 2012. TRPA1 and TRPV4 mediate paclitaxel-induced peripheral neuropathy in mice via a glutathione-sensitive mechanism. Pfluger's Arch. 463, 561-569.
121. Matthews, JM, Qin, N, Colburn, RW., 2012. The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists. Bioorg. Med. Chem. Lett. 22, 2922-2926.
122. May, D, Baastrup, J, Nientit, MR, Binder, A, Schünke, M, Baron, R, Cascorbi, I., 2012. Differential expression and functionality of TRPA1 protein genetic variants in conditions of thermal stimulation. J. Biol. Chem. 287 (32), 27087-27094.
123. McCoy, DD, Knowlton, WM, McKemy, DD., 2011. Scraping through the ice: uncovering the role of TRPM8 in cold transduction. Am. J. Physiol. Regul. Integr. Comp. Physiol. 300, R1278-R1287.
124. McGaraughty, S, Segreti, JA, Fryer, RM, Brown, BS, Faltynek, CR, Kym, PR., 2009. Antagonism of TRPV1 receptors indirectly modulates activity of thermoregulatory neurons in the medial preoptic area of rats. Brain Res. 1268, 58-67.
125. McGaraughty, S, Chu, KL, Perner, RJ, Didomenico, S, Kort, ME, Kym, PR., 2010. TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats. Mol. Pain 6, 14.
126. McKemy, DD, Neuhausser, WM, Julius, D., 2002. Identification of a cold receptor reveals a general role for TRP channels in thermosensation. Nature 416, 52-58.
127. Montell, C., 2010. Preventing a perm with TRPV3. Cell 141, 218-220.
128. Moqrich, A, Hwang, SW, Earley, TJ, Petrus, MJ, Murray, AN, Spencer, KS, Andahazy, M, Story, GM, Patapoutian, A., 2005. Impaired thermosensation in mice lacking TRPV3, a heat and camphor sensor in the skin. Science 307, 1468-1472.
129. Moran, MM, McAlexander, MA, Biro, T, Szallasi, A., 2011. Transient receptor potential channels as therapeutic targets. Nat. Rev. Drug Discovery 10, 601-620.
130. Moriyama, T, Higashi, T, Togashi, K, Iida, T, Segi, E, Sugimoto, Y, Tominaga, T, Narumiya, S, Tominaga, M., 2005. Sensitization of TRPV1 by EP1 and IP reveals peripheral nociceptive mechanism of prostaglandins. Mol. Pain 1, 3-9.
131. Moussaieff, A, Rimmerman, N, Bregman, T, Straiker, A, Felder, CC, Shoham, S, Kashman, Y, Huang, SM, Lee, H, Shohami, E, Mackie, K, Caterina, MJ, Walker, JM, Fride, E, Mechoulam, R., 2008. Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain. FASEB J.
132. Nassini, R, Gees, M, Harrison, S, De Siena, G, Materazzi, S, Moretto, N, Failli, P, Preti, D, Marchetti, N, Cavazzini, A, Mancini, F, Pedretti, P, Nilius, B, Patacchini, R, Geppetti, P., 2011. Oxaliplatin elicits mechanical and cold allodynia in rodents via TRPA1 receptor stimulation. Pain 152, 1621-1631.
133. Muthuppalniappan, M, Thomas, A, Kumar, S, Margal, S, Khairatkar-Joshi, N, Mukhopadhyay, I., Gullapalli, S., 2010. Preparation of quinazolinedione derivatives as TRPA1 modulators. PCT Appl., WO/2010/004390.
134. Neubert, JK, Mannes, AJ, Keller, J, Wexel, M, Iadarola, MJ, Caudle, RM., 2005. Peripheral targeting of the trigeminal ganglia via the infraorbital foramen as a therapeutic strategy. Brain Res. Brain Res. Protocol. 15, 119-125.
135. Neubert, JK, Mannes, AJ, Karai, LJ, Jenkins, AC, Zawatski, L, Abu-Asab, M, Iadarola, MJ., 2008. Perineural resiniferatoxin selectively inhibits inflammatory hyperalgesia. Mol. Pain 4, 1-10.
136. Ng, H, Hang, J., 2010. Compositions useful for treating disorders related to TRPA1. PCT Appl., WO/2010/075353.
137. Nilius, B, Owsianik, G, Voets, T, Peters, JA., 2007. Transient receptor potential cation channels in disease. Physiol. Rev. 87, 165-217.
138. Norman, MH, Bo, YY, Gore, VK, Horne, D, Kaller, M, Ma, VV, Monenschein, H, Nguyen, T, Nishimura, N, Tamayo, N., 2009. Preparation of substituted dihydroisoquinoline derivatives for use as TRP-M8 receptor ligands. Chem. Abstr. 151, 33430.
139. Noto, C, Pappagallo, M, Szallasi, A., 2009. NGX-4010, a high-concentration capsaicin dermal patch for lasting relief of peripheral neuropathic pain. Curr. Opin. Invest. Drugs 10, 702-710.
140. Numazaki, M, Tominaga, M., 2004. Nociception and TRP channels. Curr Drug Targets CNS Neurol. Disord. 3, 479-485.
141. Obata, K, Katsura, H, Mizushima, T, Yamanaka, H, Kobayashi, K, Dai, Y, Fukuoka, T, Tokunaga, A, Tominaga, M, Noguchi, K., 2005. TRPA1 induced in sensory neurons contributes to cold hyperalgesia after inflammation and nerve injury. J. Clin. Invest..
142. Parks, DJ, Parsons, WH, Colburn, RW., 2011. Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists. J. Med. Chem. 54, 233-247.
143. Patapoutian, A, Peier, AM, Story, GM, Viswanath, V., 2003. ThermoTRP channels and beyond: mechanisms of temperature sensation. Nat. Rev. Neurosci. 4, 529-539.
144. Patapoutian, A, Tate, S, Woolf, CJ., 2009. Transient receptor potential channels: targeting pain at the source. Nat. Rev. Drug Discovery 8, 55-68.
145. Pecze, L, Pelsoczi, P, Kecskés, M, Winter, Z, Papp, A, Kaszás, K, Letoha, T, Vizler, C, Oláh, Z., 2009. Resiniferatoxin mediated ablation of TRPV1+ neurons removes TRPA1 as well. Can. J. Neurol. Sci. 36 234-141.
146. Peier, AM, Reeve, AJ, Andersson, DA, Moqrich, A, Earley, TJ, Hergarden, AC, Story, GM, Colley, S, Hogenesch, JB, McIntyre, P, Bevan, S, Patapoutian, A., 2002a. A heat-sensitive TRP channel expressed in keratinocytes. Science 296 2046-2204.
147. Peier, AM, Moqrich, A, Hergarden, AC, Reeve, AJ, Andersson, DA, Story,
148. Peppin, JF, Majors, K, Webster, LR, Simpson, DM, Tobias, JK, Vanhove, GF., 2011. Tolerability of NGX-4010, a capsaicin 8% patch for peripheral neuropathic pain. J. Pain Res. 4, 385-392.
149. Pingle, SC, Matta, JA, Ahern, GP., 2007. Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb. Exp. Pharmacol. 179, 155-171.
150. Player, MR, Parks, DJ, Parsons, W, Meegalla, SK, Illig, CR, Ballentine, SK., 2010. Heterocyclic benzimidazoles as TRPM8 modulators. Chem. Abstr. 152, 470455.
151. Premkumar, LS, Ahern, G., 2000. Induction of vanilloid receptor channel activity by protein kinase C. Nature 408, 985-990.
152. Preti, D, Szallasi, A, Patacchini, R.TRP, 2012. channels as therapeutic targets in airway disorders: a patent review. Exp. Opin. Ther. Pat. 22, 663-695.
153. Proudfoot, CJ, Garry, EM, Cottrell, DF, Rosie, R, Anderson, H, Robertson, DC, Fleetwood-Walker, SM, Mitchell, R., 2006. Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr. Biol. 16, 1591-1605.
154. Rami, HK, Thompson, M, Stemp, G, Fell, S, Jermann, JC, Stevens, AJ, Smart, D, Sargent, B, Sanderson, D, Randall, AD, Gunthorpe, MJ, Davis, JB., 2006. Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonists suitable for clinical development. Bioorg. Med. Chem. Lett. 16, 3287-3291.
155. Reilly, RM, McDonald, HA, Puttfarcken, PS, Joshi, SK, Lewis, L, Pai, M, Franklin, PH, Segreti, JM, Neelands, TR, Han, P, Chen, J, Mantyh, PW, Ghilardi, JR, Turner, TM, Voight, EA, Daanen, JF, Schmidt, RS, Gomtsyan, A, Kort, ME, Faltynek, CR, Kym, PR., 2012. J. Pharmacol. Exp. Ther. 342, 416-428.
156. Remadevi, R, Szallasi, A., 2008. Adlea (ALGRX-4975), an injectable capsaicin (TRPV1 receptor agonist) formulation for long lasting pain relief. IDrugs 11, 120-132.
157. Rossi, HL, Jenkins, AC, Kaufman, J, Bhattacharyya, I, Caudle, RM, Neubert, JK., 2012. Characterization of bilateral trigeminal constriction injury using an operant facial pain assay. Neuroscience, Epub ahead of print.
158. Rowbotham, MC, Nothaft, W, Duan, WR, Wang, Y, Faltynek, C, McGaraughty, S, Chu, KL, Svensson, P., 2011. Pain 152, 1192-1200.
159. Salazar, M, Moldenhauer, H, Baez-Nieto, D., 2011. Could an allosteric gating model explain the role of TRPA1 in cold hypersensitivity? J. Neurosci. 31, 5554-5556.
160. Sherkheli, MA, Vogt-Eisele, AK, Bura, D, Beltran Marques, LR, Gisselmann, G, Hatt, H., 2010. Characterization of selective TRPM8 ligands and their structure-activity response (SAR) relationship. J. Pharm. Pharm. Sci. 13, 242-253.
161. Siemens, J, et al., 2006. Spider toxins activate the capsaicin receptor to produce inflammatory pain. Nature 444, 208-212.
162. Simpson, DM, Gazda, S, Brown, S, et al., 2010. Long-term safety of NGX-4010, a high-concentration capsaicin patch, in patients with peripheral neuropathic pain. J. Pain Symptom Manage. 39, 1053-1064.
163. Smith, GD, Gunthorpe, MJ, Kelsell, RE, Hayes, PD, Reilly, P, Facer, P, Wright, JE, Jerman, JC, Walhin, JP, Ooi, L, Egerton, J, Charles, KJ, Smart, D, Randall, AD, Anand, P, Davis, JB., 2002. TRPV3 is atemperature-sensitive vanilloid receptor-like protein. Nature 418, 186-190.
164. Story, GM, Peier, AM, Reeve, AJ, Eid, SR, Mosbacher, J, Hricik, TR, Earley, TJ, Hergarden, AC, Andersson, DA, Hwang, SW, McIntyre, P, Jegla, T, Bevan, S, Patapoutian, A., 2003. ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures. Cell 112 (6), 819-829.
165. Su, L, Wang, C, Yu, YH, Ren, YY, Xie, KL, Wang, GL., 2011. Role of TRPM8 in dorsal root ganglion in nerve injury-induced chronic pain. BMC Neurosci. 12, 120-128.
166. Sulk, M, Seeliger, S, Aubert, J, Schwab, VD, Cevikbas, F, Rivier, M, Nowak, P, Voegel, JJ, Buddenkotte, J, Steinhoff, M., 2012. Distribution and expression of non-neuronal transient receptor potential (TRPV) ion channels in rosacea. J. Invest. Dermatol. 132, 1253-1262.
167. Swandulla, D, Carbone, E, Schafer, K, Lux, HD., 1987. Effect of menthol on two types of Ca currents in cultured sensory neurons of vertebrates. Pfluger's Arch. 409, 52-59.
168. Szallasi, A, Blumberg, PM., 1989. Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper. Neuroscience 30, 515-520.
169. Szallasi, A, Blumberg, PM., 1999. Vanilloid (Capsaicin) receptors and mechanisms. Pharmacol. Rev. 51, 159-212.
170. Szallasi, A, Cortright, DN, Blum, CA, Eid, SR., 2007. The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat. Rev. Drug Discovery 6, 357-372.
171. Ta, LE, Bieber, AJ, Carlton, SM, Loprinzi, CL, Low, PA, Windebank, AJ., 2010. Transient receptor potential vanilloid 1 is essential for cisplatin-induced heat hyperalgesia in mice. Mol. Pain 6, 15.
172. Takashima, Y, Daniels, RL, Knowlton, W, Teng, J, Liman, ER, McKemy, DD., 2007. Diversity in the neural circuitry of cold sensing revealed by genetic axonal labeling of transient receptor potential melastatin 8 neurons. J. Neurosci. 27, 14147-14157.
173. Trevisani M. TRPV1 antagonists for pain relief, cough and urinary incontinence. 〈http://www.worldpharma2010/pp/W03.1.pdf〉.
174. Trevisani, M, Smart, D, Gunthorpe, MJ, Tognetto, M, Barbieri, M, Campi, B, Amadesi, S, Gray, J, Jerman, JC, Brough, SJ, Owen, D, Smith, GD, Randall, AS, Harrison, S, Bianchi, A, Davis, JB, Geppetti, P., 2002. Ethanol elicits and potentiates nociceptor responses via the vanilloid receptor-1. Nat. Neurosci. 5, 546-551.
175. Uchida, H., Ogawa, S., Makabe, M., Maeda, Y., 2008. PCT Int. Appl., WO2008/091021.
176. Ueda, T, Yamada, T, Ugawa, S, Ishida, Y, Shimada, S., 2009. TRPV3, a thermosensitive channel is expressed in mouse distal colon epithelium. Biochem. Biophys. Res. Commun. 383 (1), 130-134.
177. Voets, T, Owsianik, G, Nilius, B., 2007. TRPM8. Handb. Exp. Pharmacol., 329-344.
178. Wang, Z, Miyares, RL, Ahern, GP., 2005. Oleoylethanolamide excites vagal sensory neurones, induces visceral pain and reduces short-term food intake in mice via capsaicin receptor TRPV1. J. Physiol. 564, 541-547.
179. Watabiki, T, Kiso, T, Kuramochi, T, Yonezawa, K, Tsuji, N, Kohara, A, Kakimoto, S, Aoki, T, Matsuoka, N., 2011. Amelioration of neuropathic pain by novel transient receptor potential vanilloid 1 antagonists AS1928370 in rats without hyperthermic effect. J. Pharmacol. Exp. Ther. 336, 743-750.
180. Wei, H, Hämäläinen, MM, Saarnilehto, M, Koivisto, A, Pertovaara, A., 2009. Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals. Anesthesiology 111 (1), 147-154.
181. Wei, H, Chapman, H, Saarnilehto, M, Kuokkanen, K, Koivisto, A, Pertovaara, A., 2010. Roles of cutaneous versus spinal TRPA1 channels in mechanical hypersensitivity in the diabetic or mustard oil-treated non-diabetic rat. Neuropharmacology 58 (3), 578-584.
182. Wilson, SR, Gerhold, KA, Bifolck-Fisher, A, Liu, Q, Patel, KN, Dong, X, Bautista, DM., 2011. TRPA1 is required for histamine-independent, mas-related G protein-coupled receptor-mediated itch. Nat. Neurosci. 14, 595-602.
183. Wu, L-J, Sweet, T-B, Clapham, DE., 2010. International union of basic and clinical pharmacology. LXXVI. Current progress in the mammalian TRP ion channel family. Pharmacol. Rev. 62, 381-404.
184. Xiao, R, Tian, J, Tang, J, Zhu, MX., 2008. The TRPV3 mutation associated with the hairless phenotype in rodents is constitutively active. Cell Calcium 43, 334-343.
185. Xing, H, Chen, M, Ling, J, Tan, W, Gu, JG, 2007. TRPM8 mechanism of cold allodynia after chronic nerve injury. J. Neurosci. 27, 13680-13690.
186. Xu, H, Ramsey, IS, Kotecha, SA, Moran, MM, Chong, JA, Lawson, D, Ge, P, Lilly, J, Silos-Santiago, I, Xie, Y, DiStefano, PS, Curtis, R, Clapham, DE., 2002. TRPV3 is a calcium-permeable temperature-sensitive cation channel. Nature 418, 181-186.
187. Xu, H, Delling, M, Jun, JC, Clapham, DE., 2006. Oregano, thyme and clove-derived flavors and skin sensitizers activate specific TRP channels. Nat. Neurosci. 9, 628-635.
188. Yamada, T, Ueda, T, Ugawa, S, Ishida, Y, Imayasu, M, Koyama, S, Shimada, S., 2010. Functional expression of transient receptor potential vanilloid 3 (TRPV3) in corneal epithelial cells: involvement in thermosensation and wound healing. Exp. Eye Res. 90 (1), 121-129.
189. Yoshioka, T., Imura, K., Asakawa, M., Suzuki, M., Oshima, I., Hirasawa, T., Sakata, T., Horikawa, T., Arimura, A., 2009. Impact of the Gly573Ser substitution in TRPV3 on the development of allergic and pruritic dermatitis in mice. J. Invest. Dermatol. 129, 714-722.
190. Zayats, V, Samad, A, Minofar, B, Roelofs, KE, Stockner, T, Ettrich, R., 2012. Regulation of the transient receptor potential channel TRPA1 by its N-terminal ankyrin repeat domain. J. Mol. Model., 3. [Epub ahead of print].
191. Zhang, XF, Chen, J, Faltynek, CR, Moreland, RB, Neelands, TR., 2008. Transient receptor potential A1 mediates an osmotically activated ion channel. Eur. J. Neurosci. 27 (3), 605-611.
192. Zhao, M, Isami, K, Nakamura, S, Shirakawa, H, Nakagawa, T, Kaneko, S., 2010. Acute cold hypersensitivity characteristically induced by oxaliplatin is caused by the enhanced responsiveness of TRPA1 in mice. Mol. Pain 8 (1), 55.