Targeting pain-evoking transient receptor potential channels for the treatment of pain

Current Neuropharmacology

Volumn 11, Issue 6, 2013, Pages 652-663

  Luo, Jialie ^a   Walters, Edgar T ^a   Carlton, Susan M ^b   Hu, Hongzhen ^a  

^a UNIVERSITY OF TEXAS MEDICAL SCHOOL   (United States)

^b University of Texas Medical Branch School of Medicine   (United States)

Author keywords

Drug target; Inflammation; Neuropathy; Pain; Pain management; Transient receptor potential channels

Indexed keywords

(5 TERT BUTYL 2,3 DIHYDRO 1H INDEN 1 YL) 3 (1H INDAZOL 4 YL)UREA; 1 (2 BROMOPHENYL) 3 [1 (5 TRIFLUOROMETHYL 2 PYRIDINYL) 3 PYRROLIDINYL]UREA; 1 (5 ISOQUINOLINYL) 3 [4 (TRIFLUOROMETHYL)BENZYL]UREA; 2 [6 (2 ACETYLAMINO 1,3 BENZOTHIAZOL 4 YLOXY) 4 PYRIMIDINYL] 5 (TRIFLUOROMETHYL)PHENYLCARBAMIC ACID TERT BUTYL ESTER; 3 [2 (1 PIPERIDINYL) 6 (TRIFLUOROMETHYL) 3 PYRIDINYL] N (5,6,7,8 TETRAHYDRO 7 HYDROXY 1 NAPHTHYL)ACRYLAMIDE; 4 CHLORO N (3 METHOXYPHENYL)CINNAMAMIDE; 4 [3 (TRIFLUOROMETHYL) 2 PYRIDINYL] N [5 (TRIFLUOROMETHYL) 2 PYRIDINYL] 1 PIPERAZINECARBOXAMIDE; A 784168; A 795614; A 967079; AP 18; AZD 1386; CALCITONIN GENE RELATED PEPTIDE; CAPSAICIN; CISPLATIN; CYCLIC AMP DEPENDENT PROTEIN KINASE ANCHORING PROTEIN; DOCOSAHEXAENOIC ACID; G PROTEIN COUPLED RECEPTOR; GRC 6211; HISTAMINE; ICOSAPENTAENOIC ACID; JTS 653; LIDOCAINE; LIDOCAINE ETHOBROMIDE; MESSENGER RNA; MK 2295; MRS 1477; N (1,4 BENZODIOXAN 6 YL) 3 (4 TERT BUTYLPHENYL)ACRYLAMIDE; N (4 ISOPROPYLPHENYL) 2 (1,2,3,6 TETRAHYDRO 1,3 DIMETHYL 2,6 DIOXO 7H PURIN 7 YL)ACETAMIDE; N [4 [6 [4 (TRIFLUOROMETHYL)PHENYL] 4 PYRIMIDINYLOXY]BENZOTHIAZOL 2 YL]ACETAMIDE; NERVE GROWTH FACTOR; NITRIC OXIDE; NONSTEROID ANTIINFLAMMATORY AGENT; OPIATE; PF 4065463; PHORBOL 13 ACETATE 12 MYRISTATE; PROSTAGLANDIN E2; RESINIFERATOXIN; SEROTONIN; SUBSTANCE P; TRANSIENT RECEPTOR POTENTIAL CHANNEL; TRANSIENT RECEPTOR POTENTIAL CHANNEL A1; TRANSIENT RECEPTOR POTENTIAL CHANNEL M3; TRANSIENT RECEPTOR POTENTIAL CHANNEL M8; TRINITROBENZENESULFONIC ACID; TUMOR NECROSIS FACTOR; UNINDEXED DRUG; VANILLOID RECEPTOR; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 1 ANTAGONIST; VANILLOID RECEPTOR 4; WN 1001;

ALLODYNIA; ANALGESIA; ARTICLE; CALCIUM CELL LEVEL; CHRONIC CONSTRICTION INJURY; CHRONIC PAIN; CLINICAL TRIAL (TOPIC); DRUG INTERACTION; HUMAN; HYPERALGESIA; HYPERTHERMIA; IC50; INFLAMMATION; INFLAMMATORY PAIN; NERVE INJURY; NEUROPATHIC PAIN; NOCICEPTIVE PAIN; NONHUMAN; OXALIPLATIN-INDUCED NEUROPATHY; PAIN RECEPTOR; PANCREATITIS; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; RECEPTOR DOWN REGULATION; RECEPTOR SENSITIVITY; REFLUX ESOPHAGITIS; SIGNAL TRANSDUCTION; TEMPERATURE SENSITIVITY; TISSUE INJURY;

EID: 84899541943     PISSN: 1570159X     EISSN: 18756190     Source Type: Journal    
DOI: 10.2174/1570159X113119990040     Document Type: Article

References (204)

1. Reichling, D. B.; Levine, J. D. Critical role of nociceptor plasticity in chronic pain. Trends Neurosci, 2009, 32(12), 611-8.
2. Costigan, M.; Scholz, J.; Woolf, C. J. Neuropathic pain: a maladaptive response of the nervous system to damage. Annu. Rev. Neurosci., 2009, 32, 1-32.
3. Dubin, A. E.; Patapoutian, A. Nociceptors: the sensors of the pain pathway. J. Clin. Invest., 2010, 120(11), 3760-72.
4. Lumpkin, E. A.; Caterina, M. J. Mechanisms of sensory transduction in the skin. Nature, 2007, 445(7130), 858-65.
5. Basbaum, A. I.; Bautista, D. M.; Scherrer, G.; Julius, D. Cellular and molecular mechanisms of pain. Cell, 2009, 139(2), 267-84.
6. Colombo, E.; Francisconi, S.; Faravelli, L.; Izzo, E.; Pevarello, P. Ion channel blockers for the treatment of neuropathic pain. Future Med. Chem., 2010, 2(5), 803-42.
7. Caterina, M. J.; Julius, D. The vanilloid receptor: a molecular gateway to the pain pathway. Annu. Rev. Neurosci., 2001, 24, 487-517.
8. Venkatachalam, K.; Montell, C. TRP channels. Annu. Rev. Biochem., 2007, 76, 387-417.
9. Nilius, B.; Owsianik, G. Transient receptor potential channelopathies. Pflugers Arch., 2010, 460(2), 437-50.
10. Dhaka, A.; Viswanath, V.; Patapoutian, A. Trp ion channels and temperature sensation. Annu. Rev. Neurosci., 2006, 29, 135-61.
11. Vriens, J.; Owsianik, G.; Hofmann, T.; Philipp, S. E.; Stab, J.; Chen, X.; Benoit, M.; Xue, F.; Janssens, A.; Kerselaers, S.; Oberwinkler, J.; Vennekens, R.; Gudermann, T.; Nilius, B.; Voets, T. TRPM3 is a nociceptor channel involved in the detection of noxious heat. Neuron, 2011, 70(3), 482-94.
12. Patapoutian, A.; Tate, S.; Woolf, C. J. Transient receptor potential channels: targeting pain at the source. Nat. Rev. Drug Discov., 2009, 8(1), 55-68.
13. Caterina, M. J.; Schumacher, M. A.; Tominaga, M.; Rosen, T. A.; Levine, J. D.; Julius, D. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature, 1997, 389(6653), 816-24.
14. Tominaga, M.; Caterina, M. J.; Malmberg, A. B.; Rosen, T. A.; Gilbert, H.; Skinner, K.; Raumann, B. E.; Basbaum, A. I.; Julius, D. The cloned capsaicin receptor integrates multiple pain-producing stimuli. Neuron, 1998, 21(3), 531-43.
15. Voets, T.; Droogmans, G.; Wissenbach, U.; Janssens, A.; Flockerzi, V.; Nilius, B. The principle of temperature-dependent gating in cold-and heat-sensitive TRP channels. Nature, 2004, 430(7001), 748-54.
16. Nilius, B.; Mahieu, F.; Karashima, Y.; Voets, T. Regulation of TRP channels: a voltage-lipid connection. Biochem. Soc. Trans, 2007, 35(Pt 1), 105-8.
17. Matta, J. A.; Ahern, G. P. Voltage is a partial activator of rat thermosensitive TRP channels. J. Physiol., 2007, 585(Pt 2), 469-82.
18. Gopinath, P.; Wan, E.; Holdcroft, A.; Facer, P.; Davis, J. B.; Smith, G. D.; Bountra, C.; Anand, P. Increased capsaicin receptor TRPV1 in skin nerve fibres and related vanilloid receptors TRPV3 and TRPV4 in keratinocytes in human breast pain. BMC Womens Health, 2005, 5(1), 2.
19. Tympanidis, P.; Casula, M. A.; Yiangou, Y.; Terenghi, G.; Dowd, P.; Anand, P. Increased vanilloid receptor VR1 innervation in vulvodynia. Eur. J. Pain, 2004, 8(2), 129-33.
20. Breese, N. M.; George, A. C.; Pauers, L. E.; Stucky, C. L. Peripheral inflammation selectively increases TRPV1 function in IB4-positive sensory neurons from adult mouse. Pain, 2005, 115(1-2), 37-49.
21. Yu, L.; Yang, F.; Luo, H.; Liu, F. Y.; Han, J. S.; Xing, G. G.; Wan, Y. The role of TRPV1 in different subtypes of dorsal root ganglion neurons in rat chronic inflammatory nociception induced by complete Freund's adjuvant. Mol. Pain, 2008, 4, 61.
22. Honore, P.; Wismer, C. T.; Mikusa, J.; Zhu, C. Z.; Zhong, C.; Gauvin, D. M.; Gomtsyan, A.; El Kouhen, R.; Lee, C. H.; Marsh, K.; Sullivan, J. P.; Faltynek, C. R.; Jarvis, M. F. A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats. J. Pharmacol. Exp. Ther., 2005, 314(1), 410-21.
23. Chizh, B. A.; O'Donnell, M. B.; Napolitano, A.; Wang, J.; Brooke, A. C.; Aylott, M. C.; Bullman, J. N.; Gray, E. J.; Lai, R. Y.; Williams, P. M.; Appleby, J. M. The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans. Pain, 2007, 132(1-2), 132-41.
24. Gavva, N. R.; Tamir, R.; Qu, Y.; Klionsky, L.; Zhang, T. J.; Immke, D.; Wang, J.; Zhu, D.; Vanderah, T. W.; Porreca, F.; Doherty, E. M.; Norman, M. H.; Wild, K. D.; Bannon, A. W.; Louis, J. C.; Treanor, J. J. AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J. Pharmacol. Exp. Ther., 2005, 313(1), 474-84.
25. Caterina, M. J.; Leffler, A.; Malmberg, A. B.; Martin, W. J.; Trafton, J.; Petersen-Zeitz, K. R.; Koltzenburg, M.; Basbaum, A. I.; Julius, D. Impaired nociception and pain sensation in mice lacking the capsaicin receptor. Science, 2000, 288(5464), 306-13.
26. Negri, L.; Lattanzi, R.; Giannini, E.; Colucci, M.; Margheriti, F.; Melchiorri, P.; Vellani, V.; Tian, H.; De Felice, M.; Porreca, F. Impaired nociception and inflammatory pain sensation in mice lacking the prokineticin receptor PKR1: focus on interaction between PKR1 and the capsaicin receptor TRPV1 in pain behavior. J. Neurosci., 2006, 26(25), 6716-27.
27. 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.; Bingham, S.; Randall, A.; Sheardown, S. A. Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia. Nature, 2000, 405(6783), 183-7.
28. Brain, S. D. TRPV1 and TRPA1 channels in inflammatory pain: elucidating mechanisms. Ann. N. Y Acad. Sci., 2011, 1245, 36-7.
29. Fernandes, E. S.; Russell, F. A.; Spina, D.; McDougall, J. J.; Graepel, R.; Gentry, C.; Staniland, A. A.; Mountford, D. M.; Keeble, J. E.; Malcangio, M.; Bevan, S.; Brain, S. D. A distinct role for transient receptor potential ankyrin 1, in addition to transient receptor potential vanilloid 1, in tumor necrosis factor alpha-induced inflammatory hyperalgesia and Freund's complete adjuvant-induced monarthritis. Arthritis Rheum., 2011, 63(3), 819-29.
30. Russell, F. A.; Schuelert, N.; Veldhoen, V. E.; Hollenberg, M. D.; McDougall, J. J. Activation of PAR(2) receptors sensitizes primary afferents and causes leukocyte rolling and adherence in the rat knee joint. Br. J. Pharmacol., 2012, 167(8), 1665-78.
31. Story, G. M.; Peier, A. M.; Reeve, A. J.; Eid, S. R.; Mosbacher, J.; Hricik, T. R.; Earley, T. J.; Hergarden, A. C.; Andersson, D. A.; Hwang, S. W.; McIntyre, P.; Jegla, T.; Bevan, S.; Patapoutian, A. ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures. Cell, 2003, 112(6), 819-29.
32. Jordt, S. E.; Bautista, D. M.; Chuang, H. H.; McKemy, D. D.; Zygmunt, P. M.; Hogestatt, E. D.; Meng, I. D.; Julius, D. Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1. Nature, 2004, 427(6971), 260-5.
33. Bautista, D. M.; Pellegrino, M.; Tsunozaki, M. TRPA1: A gatekeeper for inflammation. Annu. Rev. Physiol., 2013, 75, 181-200.
34. Nilius, B.; Appendino, G.; Owsianik, G. The transient receptor potential channel TRPA1: from gene to pathophysiology. Pflugers Arch, 2012, 464(5), 425-58.
35. Kremeyer, B.; Lopera, F.; Cox, J. J.; Momin, A.; Rugiero, F.; Marsh, S.; Woods, C. G.; Jones, N. G.; Paterson, K. J.; Fricker, F. R.; Villegas, A.; Acosta, N.; Pineda-Trujillo, N. G.; Ramirez, J. D.; Zea, J.; Burley, M. W.; Bedoya, G.; Bennett, D. L.; Wood, J. N.; Ruiz-Linares, A. A gain-of-function mutation in TRPA1 causes familial episodic pain syndrome. Neuron, 2010, 66(5), 671-80.
36. da Costa, D. S.; Meotti, F. C.; Andrade, E. L.; Leal, P. C.; Motta, E. M.; Calixto, J. B. The involvement of the transient receptor potential A1 (TRPA1) in the maintenance of mechanical and cold hyperalgesia in persistent inflammation. Pain, 2010, 148(3), 431-7.
37. Frederick, J.; Buck, M. E.; Matson, D. J.; Cortright, D. N. Increased TRPA1, TRPM8, and TRPV2 expression in dorsal root ganglia by nerve injury. Biochem. Biophys. Res. Commun., 2007, 358(4), 1058-64.
38. Obata, K.; Katsura, H.; Mizushima, T.; Yamanaka, H.; Kobayashi, K.; Dai, Y.; Fukuoka, T.; Tokunaga, A.; Tominaga, M.; Noguchi, K. TRPA1 induced in sensory neurons contributes to cold hyperalgesia after inflammation and nerve injury. J. Clin. Invest., 2005, 115(9), 2393-401.
39. Bautista, D. M.; Jordt, S. E.; Nikai, T.; Tsuruda, P. R.; Read, A. J.; Poblete, J.; Yamoah, E. N.; Basbaum, A. I.; Julius, D. TRPA1 mediates the inflammatory actions of environmental irritants and proalgesic agents. Cell, 2006, 124(6), 1269-82.
40. Petrus, M.; Peier, A. M.; Bandell, M.; Hwang, S. W.; Huynh, T.; Olney, N.; Jegla, T.; Patapoutian, A. A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition. Mol. Pain, 2007, 3, 40.
41. Eid, S. R.; Crown, E. D.; Moore, E. L.; Liang, H. A.; Choong, K. C.; Dima, S.; Henze, D. A.; Kane, S. A.; Urban, M. O. HC-030031, a TRPA1 selective antagonist, attenuates inflammatory-and neuropathy-induced mechanical hypersensitivity. Mol. Pain, 2008, 4, 48.
42. Takashima, Y.; Daniels, R. L.; Knowlton, W.; Teng, J.; Liman, E. R.; McKemy, D. D. Diversity in the neural circuitry of cold sensing revealed by genetic axonal labeling of transient receptor potential melastatin 8 neurons. J. Neurosci., 2007, 27(51), 14147-57.
43. Knowlton, W. M.; Bifolck-Fisher, A.; Bautista, D. M.; McKemy, D. D. TRPM8, but not TRPA1, is required for neural and behavioral responses to acute noxious cold temperatures and cold-mimetics in vivo. Pain, 2010, 150(2), 340-50.
44. Gentry, C.; Stoakley, N.; Andersson, D. A.; Bevan, S. The roles of iPLA2, TRPM8 and TRPA1 in chemically induced cold hypersensitivity. Mol. Pain, 2010, 6, 4.
45. Knowlton, W. M.; Daniels, R. L.; Palkar, R.; McCoy, D. D.; McKemy, D. D. Pharmacological blockade of TRPM8 ion channels alters cold and cold pain responses in mice. PLoS One, 2011, 6(9), e25894.
46. Bang, S.; Yoo, S.; Oh, U.; Hwang, S. W. Endogenous lipid-derived ligands for sensory TRP ion channels and their pain modulation. Arch. Pharm. Res., 2010, 33(10), 1509-20.
47. Bang, S.; Yoo, S.; Yang, T. J.; Cho, H.; Hwang, S. W. Isopentenyl pyrophosphate is a novel antinociceptive substance that inhibits TRPV3 and TRPA1 ion channels. Pain, 2011, 152(5), 1156-64.
48. Miyamoto, T.; Petrus, M. J.; Dubin, A. E.; Patapoutian, A. TRPV3 regulates nitric oxide synthase-independent nitric oxide synthesis in the skin. Nat. Commun., 2011, 2, 369.
49. Mandadi, S.; Sokabe, T.; Shibasaki, K.; Katanosaka, K.; Mizuno, A.; Moqrich, A.; Patapoutian, A.; Fukumi-Tominaga, T.; Mizumura, K.; Tominaga, M. TRPV3 in keratinocytes transmits temperature information to sensory neurons via ATP. Pflugers Arch., 2009, 458(6), 1093-102.
50. Huang, S. M.; Lee, H.; Chung, M. K.; Park, U.; Yu, Y. Y.; Bradshaw, H. B.; Coulombe, P. A.; Walker, J. M.; Caterina, M. J. Overexpressed transient receptor potential vanilloid 3 ion channels in skin keratinocytes modulate pain sensitivity via prostaglandin E2. J. Neurosci., 2008, 28(51), 13727-37.
51. Huang, S. M.; Li, X.; Yu, Y.; Wang, J.; Caterina, M. J. TRPV3 and TRPV4 ion channels are not major contributors to mouse heat sensation. Mol Pain, 2011, 7, 37.
52. Brederson, J. D.; Kym, P. R.; Szallasi, A. Targeting TRP channels for pain relief. Eur. J. Pharmacol, 2013 [Epub ahead of print].
53. Haanpaa, M.; Treede, R. D. Capsaicin for neuropathic pain: linking traditional medicine and molecular biology. Eur. Neurol., 2012, 68(5), 264-75.
54. Moran, M. M.; McAlexander, M. A.; Biro, T.; Szallasi, A. Transient receptor potential channels as therapeutic targets. Nat. Rev. Drug Discov., 2011, 10(8), 601-20.
55. Yamamoto, S.; Ohsawa, M.; Ono, H. Contribution of TRPV1 receptor-expressing fibers to spinal ventral root after-discharges and mechanical hyperalgesia in a spared nerve injury (SNI) rat model. J. Pharmacol. Sci., 2013, 121(1), 9-16.
56. King, T.; Qu, C.; Okun, A.; Mercado, R.; Ren, J.; Brion, T.; Lai, J.; Porreca, F. Contribution of afferent pathways to nerve injury-induced spontaneous pain and evoked hypersensitivity. Pain, 2011, 152(9), 1997-2005.
57. Vilceanu, D.; Honore, P.; Hogan, Q. H.; Stucky, C. L. Spinal nerve ligation in mouse upregulates TRPV1 heat function in injured IB4-positive nociceptors. J. Pain, 2010, 11(6), 588-99.
58. Urano, H.; Ara, T.; Fujinami, Y.; Hiraoka, B. Y. Aberrant TRPV1 expression in heat hyperalgesia associated with trigeminal neuropathic pain. Int. J. Med. Sci., 2012, 9(8), 690-7.
59. Watabiki, T.; Kiso, T.; Kuramochi, T.; Yonezawa, K.; Tsuji, N.; Kohara, A.; Kakimoto, S.; Aoki, T.; Matsuoka, N. Amelioration of neuropathic pain by novel transient receptor potential vanilloid 1 antagonist AS1928370 in rats without hyperthermic effect. J. Pharmacol. Exp. Ther., 2011, 336(3), 743-50.
60. Jhaveri, M. D.; Elmes, S. J.; Kendall, D. A.; Chapman, V. Inhibition of peripheral vanilloid TRPV1 receptors reduces noxious heat-evoked responses of dorsal horn neurons in naive, carrageenan-inflamed and neuropathic rats. Eur. J. Neurosci., 2005, 22(2), 361-70.
61. Spicarova, D.; Nerandzic, V.; Palecek, J. Modulation of spinal cord synaptic activity by tumor necrosis factor alpha in a model of peripheral neuropathy. J. Neuroinflamm., 2011, 8, 177.
62. Lee, S. E.; Kim, J. H. Involvement of substance P and calcitonin gene-related peptide in development and maintenance of neuropathic pain from spinal nerve injury model of rat. Neurosci. Res., 2007, 58(3), 245-9.
63. Kanai, Y.; Nakazato, E.; Fujiuchi, A.; Hara, T.; Imai, A. Involvement of an increased spinal TRPV1 sensitization through its up-regulation in mechanical allodynia of CCI rats. Neuropharmacology, 2005, 49(7), 977-84.
64. Lappin, S. C.; Randall, A. D.; Gunthorpe, M. J.; Morisset, V. TRPV1 antagonist, SB-366791, inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. Eur. J. Pharmacol., 2006, 540(1-3), 73-81.
65. Cavanaugh, D. J.; Chesler, A. T.; Jackson, A. C.; Sigal, Y. M.; Yamanaka, H.; Grant, R.; O'Donnell, D.; Nicoll, R. A.; Shah, N. M.; Julius, D.; Basbaum, A. I. Trpv1 reporter mice reveal highly restricted brain distribution and functional expression in arteriolar smooth muscle cells. J. Neurosci., 2011, 31(13), 5067-77.
66. Cavanaugh, D. J.; Chesler, A. T.; Braz, J. M.; Shah, N. M.; Julius, D.; Basbaum, A. I. Restriction of transient receptor potential vanilloid-1 to the peptidergic subset of primary afferent neurons follows its developmental downregulation in nonpeptidergic neurons. J. Neurosci., 2011, 31(28), 10119-27.
67. Mishra, S. K.; Tisel, S. M.; Orestes, P.; Bhangoo, S. K.; Hoon, M. A. TRPV1-lineage neurons are required for thermal sensation. EMBO J, 2011, 30(3), 582-93.
68. Kim, Y. H.; Back, S. K.; Davies, A. J.; Jeong, H.; Jo, H. J.; Chung, G.; Na, H. S.; Bae, Y. C.; Kim, S. J.; Kim, J. S.; Jung, S. J.; Oh, S. B. TRPV1 in GABAergic interneurons mediates neuropathic mechanical allodynia and disinhibition of the nociceptive circuitry in the spinal cord. Neuron, 2012, 74(4), 640-7.
69. Zhang, J.; Cavanaugh, D. J.; Nemenov, M. I.; Basbaum, A. I. The modality-specific contribution of peptidergic and non-peptidergic nociceptors is manifest at the level of dorsal horn nociresponsive neurons. J. Physiol., 2013, 591(Pt 4), 1097-110.
70. del Camino, D.; Murphy, S.; Heiry, M.; Barrett, L. B.; Earley, T. J.; Cook, C. A.; Petrus, M. J.; Zhao, M.; D'Amours, M.; Deering, N.; Brenner, G. J.; Costigan, M.; Hayward, N. J.; Chong, J. A.; Fanger, C. M.; Woolf, C. J.; Patapoutian, A.; Moran, M. M. TRPA1 contributes to cold hypersensitivity. J. Neurosci., 2010, 30(45), 15165-74.
71. Ji, G.; Zhou, S.; Carlton, S. M. Intact Adelta-fibers up-regulate transient receptor potential A1 and contribute to cold hypersensitivity in neuropathic rats. Neuroscience, 2008, 154(3), 1054-66.
72. Chen, J.; Joshi, S. K.; DiDomenico, S.; Perner, R. J.; Mikusa, J. P.; Gauvin, D. M.; Segreti, J. A.; Han, P.; Zhang, X. F.; Niforatos, W.; Bianchi, B. R.; Baker, S. J.; Zhong, C.; Simler, G. H.; McDonald, H. A.; Schmidt, R. G.; McGaraughty, S. P.; Chu, K. L.; Faltynek, C. R.; Kort, M. E.; Reilly, R. M.; Kym, P. R. Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation. Pain, 2011, 152(5), 1165-72.
73. Katsura, H.; Obata, K.; Mizushima, T.; Yamanaka, H.; Kobayashi, K.; Dai, Y.; Fukuoka, T.; Tokunaga, A.; Sakagami, M.; Noguchi, K. Antisense knock down of TRPA1, but not TRPM8, alleviates cold hyperalgesia after spinal nerve ligation in rats. Exp Neurol, 2006, 200(1), 112-23.
74. Caspani, O.; Zurborg, S.; Labuz, D.; Heppenstall, P. A. The contribution of TRPM8 and TRPA1 channels to cold allodynia and neuropathic pain. PLoS One, 2009, 4(10), e7383.
75. Su, L.; Wang, C.; Yu, Y. H.; Ren, Y. Y.; Xie, K. L.; Wang, G. L. Role of TRPM8 in dorsal root ganglion in nerve injury-induced chronic pain. BMC Neurosci., 2011, 12, 120.
76. Serra, J.; Sola, R.; Quiles, C.; Casanova-Molla, J.; Pascual, V.; Bostock, H.; Valls-Sole, J. C-nociceptors sensitized to cold in a patient with small-fiber neuropathy and cold allodynia. Pain, 2009, 147(1-3), 46-53.
77. Proudfoot, C. J.; Garry, E. M.; Cottrell, D. F.; Rosie, R.; Anderson, H.; Robertson, D. C.; Fleetwood-Walker, S. M.; Mitchell, R. Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr. Biol., 2006, 16(16), 1591-605.
78. Baron, R. Neuropathic pain: a clinical perspective. Handb. Exp. Pharmacol., 2009, (194), 3-30.
79. Zhao, M.; Isami, K.; Nakamura, S.; Shirakawa, H.; Nakagawa, T.; Kaneko, S. Acute cold hypersensitivity characteristically induced by oxaliplatin is caused by the enhanced responsiveness of TRPA1 in mice. Mol. Pain, 2012, 8, 55.
80. 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. Oxaliplatin elicits mechanical and cold allodynia in rodents via TRPA1 receptor stimulation. Pain, 2011, 152(7), 1621-31.
81. Barriere, D. A.; Rieusset, J.; Chanteranne, D.; Busserolles, J.; Chauvin, M. A.; Chapuis, L.; Salles, J.; Dubray, C.; Morio, B. Paclitaxel therapy potentiates cold hyperalgesia in streptozotocin-induced diabetic rats through enhanced mitochondrial reactive oxygen species production and TRPA1 sensitization. Pain, 2012, 153(3), 553-61.
82. Anand, U.; Otto, W. R.; Anand, P. Sensitization of capsaicin and icilin responses in oxaliplatin treated adult rat DRG neurons. Mol. Pain, 2010, 6, 82.
83. Chen, Y.; Yang, C.; Wang, Z. J. Proteinase-activated receptor 2 sensitizes transient receptor potential vanilloid 1, transient receptor potential vanilloid 4, and transient receptor potential ankyrin 1 in paclitaxel-induced neuropathic pain. Neuroscience, 2011, 193, 440-51.
84. Hara, T.; Chiba, T.; Abe, K.; Makabe, A.; Ikeno, S.; Kawakami, K.; Utsunomiya, I.; Hama, T.; Taguchi, K. Effect of paclitaxel on transient receptor potential vanilloid 1 in rat dorsal root ganglion. Pain, 2013, 154(6),882-9.
85. Yiangou, Y.; Facer, P.; Dyer, N. H.; Chan, C. L.; Knowles, C.; Williams, N. S.; Anand, P. Vanilloid receptor 1 immunoreactivity in inflamed human bowel. Lancet, 2001, 357(9265), 1338-9.
86. Chan, C. L.; Facer, P.; Davis, J. B.; Smith, G. D.; Egerton, J.; Bountra, C.; Williams, N. S.; Anand, P. Sensory fibres expressing capsaicin receptor TRPV1 in patients with rectal hypersensitivity and faecal urgency. Lancet, 2003, 361(9355), 385-91.
87. Matthews, P. J.; Aziz, Q.; Facer, P.; Davis, J. B.; Thompson, D. G.; Anand, P. Increased capsaicin receptor TRPV1 nerve fibres in the inflamed human oesophagus. Eur. J. Gastroenterol. Hepatol., 2004, 16(9), 897-902.
88. Fujino, K.; de la Fuente, S. G.; Takami, Y.; Takahashi, T.; Mantyh, C. R. Attenuation of acid induced oesophagitis in VR-1 deficient mice. Gut, 2006, 55(1), 34-40.
89. Fasanella, K. E.; Christianson, J. A.; Chanthaphavong, R. S.; Davis, B. M. Distribution and neurochemical identification of pancreatic afferents in the mouse. J. Comp. Neurol., 2008, 509(1), 42-52.
90. Hutter, M. M.; Wick, E. C.; Day, A. L.; Maa, J.; Zerega, E. C.; Richmond, A. C.; Jordan, T. H.; Grady, E. F.; Mulvihill, S. J.; Bunnett, N. W.; Kirkwood, K. S. Transient receptor potential vanilloid (TRPV-1) promotes neurogenic inflammation in the pancreas via activation of the neurokinin-1 receptor (NK-1R). Pancreas, 2005, 30(3), 260-5.
91. Wick, E. C.; Hoge, S. G.; Grahn, S. W.; Kim, E.; Divino, L. A.; Grady, E. F.; Bunnett, N. W.; Kirkwood, K. S. Transient receptor potential vanilloid 1, calcitonin gene-related peptide, and substance P mediate nociception in acute pancreatitis. Am. J. Physiol. Gastrointest. Liver Physiol., 2006, 290(5), G959-69.
92. Xu, G. Y.; Winston, J. H.; Shenoy, M.; Yin, H.; Pendyala, S.; Pasricha, P. J. Transient receptor potential vanilloid 1 mediates hyperalgesia and is up-regulated in rats with chronic pancreatitis. Gastroenterology, 2007, 133(4), 1282-92.
93. Christoph, T.; Grunweller, A.; Mika, J.; Schafer, M. K.; Wade, E. J.; Weihe, E.; Erdmann, V. A.; Frank, R.; Gillen, C.; Kurreck, J. Silencing of vanilloid receptor TRPV1 by RNAi reduces neuropathic and visceral pain in vivo. Biochem. Biophys. Res. Commun., 2006, 350(1), 238-43.
94. Zhu, Y.; Colak, T.; Shenoy, M.; Liu, L.; Pai, R.; Li, C.; Mehta, K.; Pasricha, P. J. Nerve growth factor modulates TRPV1 expression and function and mediates pain in chronic pancreatitis. Gastroenterology, 2011, 141(1), 370-7.
95. Andrade, E. L.; Forner, S.; Bento, A. F.; Leite, D. F.; Dias, M. A.; Leal, P. C.; Koepp, J.; Calixto, J. B. TRPA1 receptor modulation attenuates bladder overactivity induced by spinal cord injury. Am. J. Physiol. Renal Physiol.,2011, 300(5), F1223-34.
96. Du, S.; Araki, I.; Yoshiyama, M.; Nomura, T.; Takeda, M. Transient receptor potential channel A1 involved in sensory transduction of rat urinary bladder through C-fiber pathway. Urology, 2007, 70(4), 826-31.
97. Lapointe, T. K.; Altier, C. The role of TRPA1 in visceral inflammation and pain. Channels (Austin), 2011, 5(6), 525-9.
98. Rogler, G.; Andus, T. Cytokines in inflammatory bowel disease. World J. Surg., 1998, 22(4), 382-9.
99. Kawada, M.; Arihiro, A.; Mizoguchi, E. Insights from advances in research of chemically induced experimental models of human inflammatory bowel disease. World J. Gastroenterol., 2007, 13(42), 5581-93.
100. Engel, M. A.; Becker, C.; Reeh, P. W.; Neurath, M. F. Role of sensory neurons in colitis: increasing evidence for a neuroimmune link in the gut. Inflamm. Bowel Dis., 2011, 17(4), 1030-3.
101. Engel, M. A.; Leffler, A.; Niedermirtl, F.; Babes, A.; Zimmermann, K.; Filipovic, M. R.; Izydorczyk, I.; Eberhardt, M.; Kichko, T. I.; Mueller-Tribbensee, S. M.; Khalil, M.; Siklosi, N.; Nau, C.; Ivanovic-Burmazovic, I.; Neuhuber, W. L.; Becker, C.; Neurath, M. F.; Reeh, P. W. TRPA1 and substance P mediate colitis in mice. Gastroenterology, 2011, 141(4), 1346-58.
102. Macpherson, L. J.; Dubin, A. E.; Evans, M. J.; Marr, F.; Schultz, P. G.; Cravatt, B. F.; Patapoutian, A. Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines. Nature, 2007, 445(7127), 541-5.
103. Hinman, A.; Chuang, H. H.; Bautista, D. M.; Julius, D. TRP channel activation by reversible covalent modification. Proc. Natl. Acad. Sci. U. S. A., 2006, 103(51), 19564-8.
104. Boesmans, W.; Owsianik, G.; Tack, J.; Voets, T.; Vanden Berghe, P. TRP channels in neurogastroenterology: opportunities for therapeutic intervention. Br. J. Pharmacol., 2011, 162(1), 18-37.
105. Brierley, S. M.; Hughes, P. A.; Page, A. J.; Kwan, K. Y.; Martin, C. M.; O'Donnell, T. A.; Cooper, N. J.; Harrington, A. M.; Adam, B.; Liebregts, T.; Holtmann, G.; Corey, D. P.; Rychkov, G. Y.; Blackshaw, L. A. The ion channel TRPA1 is required for normal mechanosensation and is modulated by algesic stimuli. Gastroenterology, 2009, 137(6), 2084-2095 e3.
106. Yang, J.; Li, Y.; Zuo, X.; Zhen, Y.; Yu, Y.; Gao, L. Transient receptor potential ankyrin-1 participates in visceral hyperalgesia following experimental colitis. Neurosci. Lett., 2008, 440(3), 237-41.
107. Vermeulen, W.; De Man, J. G.; De Schepper, H. U.; Bult, H.; Moreels, T. G.; Pelckmans, P. A.; De Winter, B. Y. Role of TRPV1 and TRPA1 in visceral hypersensitivity to colorectal distension during experimental colitis in rats. Eur. J. Pharmacol., 2013, 698(1-3), 404-12.
108. Li, C.; Zhu, Y.; Shenoy, M.; Pai, R.; Liu, L.; Pasricha, P. J. Anatomical and functional characterization of a duodeno-pancreatic neural reflex that can induce acute pancreatitis. Am. J. Physiol. Gastrointest. Liver Physiol., 2013, 304(5), G490-500.
109. Ceppa, E.; Cattaruzza, F.; Lyo, V.; Amadesi, S.; Pelayo, J. C.; Poole, D. P.; Vaksman, N.; Liedtke, W.; Cohen, D. M.; Grady, E. F.; Bunnett, N. W.; Kirkwood, K. S. Transient receptor potential ion channels V4 and A1 contribute to pancreatitis pain in mice. Am. J. Physiol. Gastrointest. Liver Physiol., 2010, 299(3), G556-71.
110. Cattaruzza, F.; Johnson, C.; Leggit, A.; Grady, E. F.; Schenk, A. K.; Cevikbas, F.; Cedron, W. J.; Bondada, S.; Kirkwood, R.; Malone, B. J.; Steinhoff, M.; Bunnett, N. W.; Kirkwood, K. S. Transient Receptor Potential Ankyrin 1 (TRPA1) Mediates Chronic Pancreatitis Pain In Mice. Am. J. Physiol. Gastrointest. Liver Physiol., 2013, 304(11),G 1002-12.
111. Schwartz, E. S.; Christianson, J. A.; Chen, X.; La, J. H.; Davis, B. M.; Albers, K. M.; Gebhart, G. F. Synergistic role of TRPV1 and TRPA1 in pancreatic pain and inflammation. Gastroenterology, 2011, 140(4), 1283-1291 e1-2.
112. Schwartz, E. S.; La, J. H.; Scheff, N. N.; Davis, B. M.; Albers, K. M.; Gebhart, G. F. TRPV1 and TRPA1 Antagonists Prevent the Transition of Acute to Chronic Inflammation and Pain in Chronic Pancreatitis. J. Neurosci., 2013, 33(13), 5603-11.
113. Akopian, A. N.; Ruparel, N. B.; Jeske, N. A.; Hargreaves, K. M. Transient receptor potential TRPA1 channel desensitization in sensory neurons is agonist dependent and regulated by TRPV1-directed internalization. J. Physiol., 2007, 583(Pt 1), 175-93.
114. Ruparel, N. B.; Patwardhan, A. M.; Akopian, A. N.; Hargreaves, K. M. Homologous and heterologous desensitization of capsaicin and mustard oil responses utilize different cellular pathways in nociceptors. Pain, 2008, 135(3), 271-9.
115. Akopian, A. N. Regulation of nociceptive transmission at the periphery via TRPA1-TRPV1 interactions. Curr. Pharm. Biotechnol., 2011, 12(1), 89-94.
116. Cenac, N.; Altier, C.; Chapman, K.; Liedtke, W.; Zamponi, G.; Vergnolle, N. Transient receptor potential vanilloid-4 has a major role in visceral hypersensitivity symptoms. Gastroenterology, 2008, 135(3), 937-46, 946 e1-2.
117. Brierley, S. M.; Page, A. J.; Hughes, P. A.; Adam, B.; Liebregts, T.; Cooper, N. J.; Holtmann, G.; Liedtke, W.; Blackshaw, L. A. Selective role for TRPV4 ion channels in visceral sensory pathways. Gastroenterology, 2008, 134(7), 2059-69.
118. Sipe, W. E.; Brierley, S. M.; Martin, C. M.; Phillis, B. D.; Cruz, F. B.; Grady, E. F.; Liedtke, W.; Cohen, D. M.; Vanner, S.; Blackshaw, L. A.; Bunnett, N. W. Transient receptor potential vanilloid 4 mediates protease activated receptor 2-induced sensitization of colonic afferent nerves and visceral hyperalgesia. Am. J. Physiol. Gastrointest. Liver Physiol., 2008, 294(5), G1288-98.
119. Cenac, N.; Altier, C.; Motta, J. P.; d'Aldebert, E.; Galeano, S.; Zamponi, G. W.; Vergnolle, N. Potentiation of TRPV4 signalling by histamine and serotonin: an important mechanism for visceral hypersensitivity. Gut, 2010, 59(4), 481-8.
120. Yamada, T.; Ugawa, S.; Ueda, T.; Ishida, Y.; Kajita, K.; Shimada, S. Differential localizations of the transient receptor potential channels TRPV4 and TRPV1 in the mouse urinary bladder. J. Histochem. Cytochem., 2009, 57(3), 277-87.
121. Everaerts, W.; Zhen, X.; Ghosh, D.; Vriens, J.; Gevaert, T.; Gilbert, J. P.; Hayward, N. J.; McNamara, C. R.; Xue, F.; Moran, M. M.; Strassmaier, T.; Uykal, E.; Owsianik, G.; Vennekens, R.; De Ridder, D.; Nilius, B.; Fanger, C. M.; Voets, T. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis. Proc. Natl. Acad. Sci. U. S. A., 2010, 107(44), 19084-9.
122. Harrington, A. M.; Hughes, P. A.; Martin, C. M.; Yang, J.; Castro, J.; Isaacs, N. J.; Blackshaw, L. A.; Brierley, S. M. A novel role for TRPM8 in visceral afferent function. Pain, 2011, 152(7), 1459-68.
123. Ramachandran, R.; Hyun, E.; Zhao, L.; Lapointe, T. K.; Chapman, K.; Hirota, C. L.; Ghosh, S.; McKemy, D. D.; Vergnolle, N.; Beck, P. L.; Altier, C.; Hollenberg, M. D. TRPM8 activation attenuates inflammatory responses in mouse models of colitis. Proc. Natl. Acad. Sci. U. S. A., 2013, 110(18), 7476-81.
124. Wong, G. Y.; Gavva, N. R. Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks. Brain Res. Rev., 2009, 60(1), 267-77.
125. Szallasi, A.; Sheta, M. Targeting TRPV1 for pain relief: limits, losers and laurels. Expert Opin. Investig. Drugs, 2012, 21(9), 1351-69.
126. Blumberg, P. M.; Pearce, L. V.; Lee, J. TRPV1 activation is not an all-or-none event: TRPV1 partial agonism/antagonism and its regulatory modulation. Curr. Top. Med. Chem., 2011, 11(17), 2151-8.
127. Steiner, A. A.; Turek, V. F.; Almeida, M. C.; Burmeister, J. J.; Oliveira, D. L.; Roberts, J. L.; Bannon, A. W.; Norman, M. H.; Louis, J. C.; Treanor, J. J.; Gavva, N. R.; Romanovsky, A. A. Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors. J. Neurosci., 2007, 27(28), 7459-68.
128. Gavva, N. R.; Bannon, A. W.; Hovland, D. N., Jr.; Lehto, S. G.; Klionsky, L.; Surapaneni, S.; Immke, D. C.; Henley, C.; Arik, L.; Bak, A.; Davis, J.; Ernst, N.; Hever, G.; Kuang, R.; Shi, L.; Tamir, R.; Wang, J.; Wang, W.; Zajic, G.; Zhu, D.; Norman, M. H.; Louis, J. C.; Magal, E.; Treanor, J. J. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J. Pharmacol. Exp. Ther., 2007, 323(1), 128-37.
129. Doherty, E. M.; Fotsch, C.; Bannon, A. W.; Bo, Y.; Chen, N.; Dominguez, C.; Falsey, J.; Gavva, N. R.; Katon, J.; Nixey, T.; Ognyanov, V. I.; Pettus, L.; Rzasa, R. M.; Stec, M.; Surapaneni, S.; Tamir, R.; Zhu, J.; Treanor, J. J.; Norman, M. H. Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J. Med. Chem., 2007, 50(15), 3515-27.
130. Gunthorpe, M. J.; Rami, H. K.; Jerman, J. C.; Smart, D.; Gill, C. H.; Soffin, E. M.; Luis Hannan, S.; Lappin, S. C.; Egerton, J.; Smith, G. D.; Worby, A.; Howett, L.; Owen, D.; Nasir, S.; Davies, C. H.; Thompson, M.; Wyman, P. A.; Randall, A. D.; Davis, J. B. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology, 2004, 46(1), 133-49.
131. Cui, M.; Honore, P.; Zhong, C.; Gauvin, D.; Mikusa, J.; Hernandez, G.; Chandran, P.; Gomtsyan, A.; Brown, B.; Bayburt, E. K.; Marsh, K.; Bianchi, B.; McDonald, H.; Niforatos, W.; Neelands, T. R.; Moreland, R. B.; Decker, M. W.; Lee, C. H.; Sullivan, J. P.; Faltynek, C. R. TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J. Neurosci., 2006, 26(37), 9385-93.
132. Swanson, D. M.; Dubin, A. E.; Shah, C.; Nasser, N.; Chang, L.; Dax, S. L.; Jetter, M.; Breitenbucher, J. G.; Liu, C.; Mazur, C.; Lord, B.; Gonzales, L.; Hoey, K.; Rizzolio, M.; Bogenstaetter, M.; Codd, E. E.; Lee, D. H.; Zhang, S. P.; Chaplan, S. R.; Carruthers, N. I. Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J. Med. Chem., 2005, 48(6), 1857-72.
133. Pomonis, J. D.; Harrison, J. E.; Mark, L.; Bristol, D. R.; Valenzano, K. J.; Walker, K. N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine-1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflammatory and neuropathic pain. J. Pharmacol. Exp. Ther., 2003, 306(1), 387-93.
134. Khairatkar-Joshi, N.; Szallasi, A. TRPV1 antagonists: the challenges for therapeutic targeting. Trends Mol. Med., 2009, 15(1), 14-22.
135. Gavva, N. R.; Treanor, J. J.; Garami, A.; Fang, L.; Surapaneni, S.; Akrami, A.; Alvarez, F.; Bak, A.; Darling, M.; Gore, A.; Jang, G. R.; Kesslak, J. P.; Ni, L.; Norman, M. H.; Palluconi, G.; Rose, M. J.; Salfi, M.; Tan, E.; Romanovsky, A. A.; Banfield, C.; Davar, G. Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. Pain, 2008, 136(1-2), 202-10.
136. Rowbotham, M. C.; Nothaft, W.; Duan, W. R.; Wang, Y.; Faltynek, C.; McGaraughty, S.; Chu, K. L.; Svensson, P. Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial. Pain, 2011, 152(5), 1192-200.
137. Krarup, A. L.; Ny, L.; Astrand, M.; Bajor, A.; Hvid-Jensen, F.; Hansen, M. B.; Simren, M.; Funch-Jensen, P.; Drewes, A. M. Randomised clinical trial: the efficacy of a transient receptor potential vanilloid 1 antagonist AZD1386 in human oesophageal pain. Aliment Pharmacol. Ther., 2011, 33(10), 1113-22.
138. Lehto, S. G.; Tamir, R.; Deng, H.; Klionsky, L.; Kuang, R.; Le, A.; Lee, D.; Louis, J. C.; Magal, E.; Manning, B. H.; Rubino, J.; Surapaneni, S.; Tamayo, N.; Wang, T.; Wang, J.; Wang, W.; Youngblood, B.; Zhang, M.; Zhu, D.; Norman, M. H.; Gavva, N. R. 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., 2008, 326(1), 218-29.
139. Garami, A.; Shimansky, Y. P.; Pakai, E.; Oliveira, D. L.; Gavva, N. R.; Romanovsky, A. A. Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia. J. Neurosci., 2010, 30(4), 1435-40.
140. Reilly, R. M.; McDonald, H. A.; Puttfarcken, P. S.; Joshi, S. K.; Lewis, L.; Pai, M.; Franklin, P. H.; Segreti, J. A.; Neelands, T. R.; Han, P.; Chen, J.; Mantyh, P. W.; Ghilardi, J. R.; Turner, T. M.; Voight, E. A.; Daanen, J. F.; Schmidt, R. G.; Gomtsyan, A.; Kort, M. E.; Faltynek, C. R.; Kym, P. R. Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature. J. Pharmacol. Exp. Ther., 2012, 342(2), 416-28.
141. Ro, J. Y.; Lee, J. S.; Zhang, Y. Activation of TRPV1 and TRPA1 leads to muscle nociception and mechanical hyperalgesia. Pain, 2009, 144(3), 270-7.
142. McNamara, C. R.; Mandel-Brehm, J.; Bautista, D. M.; Siemens, J.; Deranian, K. L.; Zhao, M.; Hayward, N. J.; Chong, J. A.; Julius, D.; Moran, M. M.; Fanger, C. M. TRPA1 mediates formalin-induced pain. Proc. Natl. Acad. Sci. U. S.A., 2007, 104(33), 13525-30.
143. McGaraughty, S.; Chu, K. L.; Perner, R. J.; Didomenico, S.; Kort, M. E.; Kym, P. R. TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats. Mol. Pain, 2010, 6, 14.
144. Mukhopadhyay, I.; Gomes, P.; Aranake, S.; Shetty, M.; Karnik, P.; Damle, M.; Kuruganti, S.; Thorat, S.; Khairatkar-Joshi, N. Expression of functional TRPA1 receptor on human lung fibroblast and epithelial cells. J. Recept Signal Transduct. Res., 2011, 31(5), 350-8.
145. Gijsen, H. J.; Berthelot, D.; De Cleyn, M. A.; Geuens, I.; Brone, B.; Mercken, M. Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists. Bioorg. Med. Chem. Lett., 2012, 22(2), 797-800.
146. Lashinger, E. S.; Steiginga, M. S.; Hieble, J. P.; Leon, L. A.; Gardner, S. D.; Nagilla, R.; Davenport, E. A.; Hoffman, B. E.; Laping, N. J.; Su, X. AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome. Am. J. Physiol. Renal Physiol., 2008, 295(3), F803-10.
147. Calvo, R. R.; Meegalla, S. K.; Parks, D. J.; Parsons, W. H.; Ballentine, S. K.; Lubin, M. L.; Schneider, C.; Colburn, R. W.; Flores, C. M.; Player, M. R. Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia. Bioorg. Med. Chem. Lett., 2012, 22(5), 1903-7.
148. Zhu, B.; Xia, M.; Xu, X.; Ludovici, D. W.; Tennakoon, M.; Youngman, M. A.; Matthews, J. M.; Dax, S. L.; Colburn, R. W.; Qin, N.; Hutchinson, T. L.; Lubin, M. L.; Brandt, M. R.; Stone, D. J.; Flores, C. M.; Macielag, M. J. Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists. Bioorg. Med. Chem. Lett., 2013, 23(7), 2234-7.
149. Beech, D. J.; Bahnasi, Y. M.; Dedman, A. M.; Al-Shawaf, E. TRPC channel lipid specificity and mechanisms of lipid regulation. Cell Calcium, 2009, 45(6), 583-8.
150. Rohacs, T.; Nilius, B. Regulation of transient receptor potential (TRP) channels by phosphoinositides. Pflugers Arch., 2007, 455(1), 157-68.
151. Zhang, M. J.; Spite, M. Resolvins: anti-inflammatory and proresolving mediators derived from omega-3 polyunsaturated fatty acids. Annu Rev Nutr, 2012, 32, 203-27.
152. Ji, R. R.; Xu, Z. Z.; Strichartz, G.; Serhan, C. N. Emerging roles of resolvins in the resolution of inflammation and pain. Trends Neurosci., 2011, 34(11), 599-609.
153. Xu, Z. Z.; Zhang, L.; Liu, T.; Park, J. Y.; Berta, T.; Yang, R.; Serhan, C. N.; Ji, R. R. Resolvins RvE1 and RvD1 attenuate inflammatory pain via central and peripheral actions. Nat. Med., 2010, 16(5), 592-7, 1p following 597.
154. Park, C. K.; Xu, Z. Z.; Liu, T.; Lu, N.; Serhan, C. N.; Ji, R. R. Resolvin D2 is a potent endogenous inhibitor for transient receptor potential subtype V1/A1, inflammatory pain, and spinal cord synaptic plasticity in mice: distinct roles of resolvin D1, D2, and E1. J. Neurosci., 2011, 31(50), 18433-8.
155. Lima-Garcia, J. F.; Dutra, R. C.; da Silva, K.; Motta, E. M.; Campos, M. M.; Calixto, J. B. The precursor of resolvin D series and aspirin-triggered resolvin D1 display anti-hyperalgesic properties in adjuvant-induced arthritis in rats. Br. J. Pharmacol., 2011, 164(2), 278-93.
156. Kida, N.; Sokabe, T.; Kashio, M.; Haruna, K.; Mizuno, Y.; Suga, Y.; Nishikawa, K.; Kanamaru, A.; Hongo, M.; Oba, A.; Tominaga, M. Importance of transient receptor potential vanilloid 4 (TRPV4) in epidermal barrier function in human skin keratinocytes. Pflugers Arch., 2012, 463(5), 715-25.
157. Sulk, M.; Seeliger, S.; Aubert, J.; Schwab, V. D.; Cevikbas, F.; Rivier, M.; Nowak, P.; Voegel, J. J.; Buddenkotte, J.; Steinhoff, M. Distribution and expression of non-neuronal transient receptor potential (TRPV) ion channels in rosacea. J. Invest. Dermatol., 2012, 132(4), 1253-62.
158. Cheng, X.; Jin, J.; Hu, L.; Shen, D.; Dong, X. P.; Samie, M. A.; Knoff, J.; Eisinger, B.; Liu, M. L.; Huang, S. M.; Caterina, M. J.; Dempsey, P.; Michael, L. E.; Dlugosz, A. A.; Andrews, N. C.; Clapham, D. E.; Xu, H. TRP channel regulates EGFR signaling in hair morphogenesis and skin barrier formation. Cell, 2010, 141(2), 331-43.
159. 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. Exome sequencing reveals mutations in TRPV3 as a cause of Olmsted syndrome. Am. J. Hum. Genet., 2012, 90(3), 558-64.
160. O'Neill, J.; Brock, C.; Olesen, A. E.; Andresen, T.; Nilsson, M.; Dickenson, A. H. Unravelling the mystery of capsaicin: a tool to understand and treat pain. Pharmacol. Rev., 2012, 64(4), 939-71.
161. Backonja, M.; Wallace, M. S.; Blonsky, E. R.; Cutler, B. J.; Malan, P., Jr.; Rauck, R.; Tobias, J. NGX-4010, a high-concentration capsaicin patch, for the treatment of postherpetic neuralgia: a randomised, double-blind study. Lancet Neurol., 2008, 7(12), 1106-12.
162. Zhang, Y. H.; Chen, Y.; Zhao, Z. Q. Resiniferatoxin reversibly blocks adjuvant-induced thermal hyperalgesia in the rat. Eur. J. Pharmacol., 2003, 481(2-3), 301-4.
163. Iadarola, M. J.; Mannes, A. J. The vanilloid agonist resiniferatoxin for interventional-based pain control. Curr. Top. Med. Chem., 2011, 11(17), 2171-9.
164. Karai, L.; Brown, D. C.; Mannes, A. J.; Connelly, S. T.; Brown, J.; Gandal, M.; Wellisch, O. M.; Neubert, J. K.; Olah, Z.; Iadarola, M. J. Deletion of vanilloid receptor 1-expressing primary afferent neurons for pain control. J. Clin. Invest., 2004, 113(9), 1344-52.
165. Kissin, I.; Szallasi, A. Therapeutic targeting of TRPV1 by resiniferatoxin, from preclinical studies to clinical trials. Curr. Top. Med. Chem., 2011, 11(17), 2159-70.
166. Lebovitz, E. E.; Keller, J. M.; Kominsky, H.; Kaszas, K.; Maric, D.; Iadarola, M. J. Positive allosteric modulation of TRPV1 as a novel analgesic mechanism. Mol. Pain, 2012, 8, 70.
167. Amaya, F.; Decosterd, I.; Samad, T. A.; Plumpton, C.; Tate, S.; Mannion, R. J.; Costigan, M.; Woolf, C. J. Diversity of expression of the sensory neuron-specific TTX-resistant voltage-gated sodium ion channels SNS and SNS2. Mol. Cell Neurosci., 2000, 15(4), 331-42.
168. Jaggi, A. S.; Singh, N. Therapeutic targets for the management of peripheral nerve injury-induced neuropathic pain. CNS Neurol. Disord. Drug Targets, 2011, 10(5), 589-609.
169. Andersson, D. A.; Gentry, C.; Moss, S.; Bevan, S. Transient receptor potential A1 is a sensory receptor for multiple products of oxidative stress. J. Neurosci., 2008, 28(10), 2485-94.
170. Cruz-Orengo, L.; Dhaka, A.; Heuermann, R. J.; Young, T. J.; Montana, M. C.; Cavanaugh, E. J.; Kim, D.; Story, G. M. Cutaneous nociception evoked by 15-delta PGJ2 via activation of ion channel TRPA1. Mol. Pain, 2008, 4, 30.
171. Taylor-Clark, T. E.; Undem, B. J.; Macglashan, D. W., Jr.; Ghatta, S.; Carr, M. J.; McAlexander, M. A. Prostaglandin-induced activation of nociceptive neurons via direct interaction with transient receptor potential A1 (TRPA1). Mol. Pharmacol., 2008, 73(2), 274-81.
172. Kawabata, A. Prostaglandin E2 and pain--an update. Biol. Pharm. Bull, 2011, 34(8), 1170-3.
173. Weng, Y.; Batista-Schepman, P. A.; Barabas, M. E.; Harris, E. Q.; Dinsmore, T. B.; Kossyreva, E. A.; Foshage, A. M.; Wang, M. H.; Schwab, M. J.; Wang, V. M.; Stucky, C. L.; Story, G. M. Prostaglandin metabolite induces inhibition of TRPA1 and channel-dependent nociception. Mol. Pain, 2012, 8, 75.
174. Dai, Y.; Wang, S.; Tominaga, M.; Yamamoto, S.; Fukuoka, T.; Higashi, T.; Kobayashi, K.; Obata, K.; Yamanaka, H.; Noguchi, K. Sensitization of TRPA1 by PAR2 contributes to the sensation of inflammatory pain. J Clin Invest, 2007, 117(7), 1979-87.
175. Mandadi, S.; Armati, P. J.; Roufogalis, B. D. Protein kinase C modulation of thermo-sensitive transient receptor potential channels: Implications for pain signaling. J. Nat. Sci. Biol. Med., 2011, 2(1), 13-25.
176. Vay, L.; Gu, C.; McNaughton, P. A. Current perspectives on the modulation of thermo-TRP channels: new advances and therapeutic implications. Expert Rev. Clin. Pharmacol., 2010, 3(5), 687-704.
177. Wang, S.; Elitt, C. M.; Malin, S. A.; Albers, K. M. Effects of the neurotrophic factor artemin on sensory afferent development and sensitivity. Sheng Li Xue Bao, 2008, 60(5), 565-70.
178. Jeske, N. A.; Patwardhan, A. M.; Henry, M. A.; Milam, S. B. Fibronectin stimulates TRPV1 translocation in primary sensory neurons. J Neurochem, 2009, 108(3), 591-600.
179. Zhang, X.; Li, L.; McNaughton, P. A. Proinflammatory mediators modulate the heat-activated ion channel TRPV1 via the scaffolding protein AKAP79/150. Neuron, 2008, 59(3), 450-61.
180. Schnizler, K.; Shutov, L. P.; Van Kanegan, M. J.; Merrill, M. A.; Nichols, B.; McKnight, G. S.; Strack, S.; Hell, J. W.; Usachev, Y. M. Protein kinase A anchoring via AKAP150 is essential for TRPV1 modulation by forskolin and prostaglandin E2 in mouse sensory neurons. J. Neurosci., 2008, 28(19), 4904-17.
181. Schmidt, M.; Dubin, A. E.; Petrus, M. J.; Earley, T. J.; Patapoutian, A. Nociceptive signals induce trafficking of TRPA1 to the plasma membrane. Neuron, 2009, 64(4), 498-509.
182. Dray, A. Neuropathic pain: emerging treatments. Br. J. Anaesth., 2008, 101(1), 48-58.
183. Btesh, J.; Fischer, M. J.; Stott, K.; McNaughton, P. A. Mapping the Binding Site of TRPV1 on AKAP79: Implications for Inflammatory Hyperalgesia. J. Neurosci., 2013, 33(21), 9184-93.
184. Fischer, M. J.; Btesh, J.; McNaughton, P. A. Disrupting sensitization of transient receptor potential vanilloid subtype 1 inhibits inflammatory hyperalgesia. J. Neurosci., 2013, 33(17), 7407-14.
185. Mike, A.; Lukacs, P. The enigmatic drug binding site for sodium channel inhibitors. Curr. Mol. Pharmacol., 2010, 3(3), 129-44.
186. Heavner, J. E. Local anesthetics. Curr. Opin. Anaesthesiol., 2007, 20(4), 336-42.
187. Leffler, A.; Fischer, M. J.; Rehner, D.; Kienel, S.; Kistner, K.; Sauer, S. K.; Gavva, N. R.; Reeh, P. W.; Nau, C. The vanilloid receptor TRPV1 is activated and sensitized by local anesthetics in rodent sensory neurons. J. Clin. Invest., 2008, 118(2), 763-76.
188. Leffler, A.; Lattrell, A.; Kronewald, S.; Niedermirtl, F.; Nau, C. Activation of TRPA1 by membrane permeable local anesthetics. Mol. Pain, 2011, 7, 62.
189. Zhang, H.; Wickley, P. J.; Sinha, S.; Bratz, I. N.; Damron, D. S. Propofol restores transient receptor potential vanilloid receptor subtype-1 sensitivity via activation of transient receptor potential ankyrin receptor subtype-1 in sensory neurons. Anesthesiology, 2011, 114(5), 1169-79.
190. Matta, J. A.; Cornett, P. M.; Miyares, R. L.; Abe, K.; Sahibzada, N.; Ahern, G. P. General anesthetics activate a nociceptive ion channel to enhance pain and inflammation. Proc. Natl. Acad. Sci. U. S. A., 2008, 105(25), 8784-9.
191. Cornett, P. M.; Matta, J. A.; Ahern, G. P. General anesthetics sensitize the capsaicin receptor transient receptor potential V1. Mol. Pharmacol., 2008, 74(5), 1261-8.
192. Piao, L. H.; Fujita, T.; Jiang, C. Y.; Liu, T.; Yue, H. Y.; Nakatsuka, T.; Kumamoto, E. TRPA1 activation by lidocaine in nerve terminals results in glutamate release increase. Biochem. Biophys. Res. Commun., 2009, 379(4), 980-4.
193. Fischer, M. J.; Leffler, A.; Niedermirtl, F.; Kistner, K.; Eberhardt, M.; Reeh, P. W.; Nau, C. The general anesthetic propofol excites nociceptors by activating TRPV1 and TRPA1 rather than GABAA receptors. J. Biol. Chem., 2010, 285(45), 34781-92.
194. Eilers, H.; Cattaruzza, F.; Nassini, R.; Materazzi, S.; Andre, E.; Chu, C.; Cottrell, G. S.; Schumacher, M.; Geppetti, P.; Bunnett, N. W. Pungent general anesthetics activate transient receptor potential-A1 to produce hyperalgesia and neurogenic bronchoconstriction. Anesthesiology, 2010, 112(6), 1452-63.
195. Xiao, B.; Dubin, A. E.; Bursulaya, B.; Viswanath, V.; Jegla, T. J.; Patapoutian, A. Identification of transmembrane domain 5 as a critical molecular determinant of menthol sensitivity in mammalian TRPA1 channels. J. Neurosci., 2008, 28(39), 9640-51.
196. Binshtok, A. M.; Bean, B. P.; Woolf, C. J. Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers. Nature, 2007, 449(7162), 607-10.
197. Binshtok, A. M.; Gerner, P.; Oh, S. B.; Puopolo, M.; Suzuki, S.; Roberson, D. P.; Herbert, T.; Wang, C. F.; Kim, D.; Chung, G.; Mitani, A. A.; Wang, G. K.; Bean, B. P.; Woolf, C. J. Coapplication of lidocaine and the permanently charged sodium channel blocker QX-314 produces a long-lasting nociceptive blockade in rodents. Anesthesiology, 2009, 111(1), 127-37.
198. Liu, H.; Zhang, H. X.; Hou, H. Y.; Lu, X. F.; Wei, J. Q.; Wang, C. G.; Zhang, L. C.; Zeng, Y. M.; Wu, Y. P.; Cao, J. L. Acid solution is a suitable medium for introducing QX-314 into nociceptors through TRPV1 channels to produce sensory-specific analgesic effects. PLoS One, 2011, 6(12), e29395.
199. Rivera-Acevedo, R. E.; Pless, S. A.; Ahern, C. A.; Schwarz, S. K. The quaternary lidocaine derivative, QX-314, exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels in vitro. Anesthesiology, 2011, 114(6), 1425-34.
200. Chen, J.; Kim, D.; Bianchi, B. R.; Cavanaugh, E. J.; Faltynek, C. R.; Kym, P. R.; Reilly, R. M. Pore dilation occurs in TRPA1 but not in TRPM8 channels. Mol. Pain, 2009, 5, 3.
201. Banke, T. G.; Chaplan, S. R.; Wickenden, A. D. Dynamic changes in the TRPA1 selectivity filter lead to progressive but reversible pore dilation. Am. J. Physiol. Cell Physiol., 2010, 298(6), C1457-68.
202. Chung, M. K.; Guler, A. D.; Caterina, M. J. TRPV1 shows dynamic ionic selectivity during agonist stimulation. Nat. Neurosci., 2008, 11(5), 555-64.
203. Puopolo, M.; Binshtok, A. M.; Yao, G. L.; Oh, S. B.; Woolf, C. J.; Bean, B. P. Permeation and block of TRPV1 channels by the cationic lidocaine derivative QX-314. J. Neurophysiol., 2013, 109(7), 1704-12.
204. Nakagawa, H.; Hiura, A. Comparison of the transport of QX-314 through TRPA1, TRPM8, and TRPV1 channels. J. Pain Res., 2013, 6, 223-30.