Targeting TRPV1 for pain relief: limits, losers and laurels

Bibliography

• Caterina MJ, Schumacher MA, Tominaga M, The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature 1997;389:816-24
   PubMed Web of Science ®Google Scholar
• Szallasi A, Cortright DN, Blum CA, Eid SR. The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov 2007;6:357-72
   PubMed Web of Science ®Google Scholar
• Patapoutian A, Tate S, Woolf CJ. Transient receptor potential channels: targeting pain at the source. Nat Rev Drug Discov 2009;8:55-68
   PubMed Web of Science ®Google Scholar
• Wu L-J, Sweet T-B, Clapham DE. International union of basic and clinical pharmacology. LXXVI. current progress in the mammalian TRP ion channel family. Pharmacol Rev 2010;62:381-404
   PubMed Web of Science ®Google Scholar
• Szallasi A, Blumberg PM. Molecular target size of the vanilloid (capsaicin) receptor in pig dorsal root ganglia. Life Sci 1991;48(19):1867-9
   Google Scholar
• Garcia-Sanz V, Fernandez-Carvajal A, Marenilla-Palao C, Identification of a tetramerization doamin in the C-terminus of the vanilloid receptor. J Neurosci 2004;24:5307-14
   PubMed Web of Science ®Google Scholar
• Liapi A, Wood JN. Extensive colocalization and heteromultimer formation of the vanilloid receptor-like protein TRPV2 and the capsaicin receptor TRPV1 in the adult rat cerebral cortex. Eur J Neurosci 2005;22:825-34
   PubMed Web of Science ®Google Scholar
• Szallasi A, Blumberg PM. Vanilloid (Capsaicin) receptors and mechanisms. Pharmacol Rev 1999;51:159-212
   PubMed Web of Science ®Google Scholar
• Szallasi A. editor. TRP channels in health and disease. implications for diagnosis and therapy. Nova Scientific Publishers:Hauppague, NY, USA; 2011
   Google Scholar
• Patapoutian A, Peier AM, Story GM, Viswanath V. ThermoTRP channels and beyond: mechanisms of temperature sensation. Nat Rev Neurosci 2003;4:529-39
   PubMed Web of Science ®Google Scholar
• Vlachova V, Teisinger J, Susankova K, Functional role of C-terminal cytoplasmic tail of rat vanilloid receptor 1. J Neurosci 2003;23:1340-50
   PubMed Web of Science ®Google Scholar
• Yao J, Liu B, Qin F. Modular thermal sensors in temperature-gated transient receptor potential (TRP) channels. Proc Natl Acad Sci USA 2011;108:11109-14
   PubMed Web of Science ®Google Scholar
• Nilius B, Owsianik G, Voets T, Peters JA. Transient receptor potential cation channels in disease. Physiol Rev 2007;87:165-217
   PubMed Web of Science ®Google Scholar
• Kremeyer B, Lopera F, Cox JJ, A gain-of-function mutation in TRPA1 causes episodic familial pain syndrome. Neuron 2010;66:871-80
   PubMedGoogle Scholar
• Carreno O, Corominas R, Fernandez-Morales J, SNP variant within the vanilloid TRPV1 and TRPV3 receptor genes are associated with migraine in the Spanish population. Am J Med Genet B Neurophychiatr Genet 2012;159B:94-103
   PubMed Web of Science ®Google Scholar
• Pingle SC, Matta JA, Ahern GP. Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb Exp Pharmacol 2007(179):155-71
   PubMedGoogle Scholar
• Caterina MJ, Julius D. The vanilloid receptor: a molecular gateway to the pain pathway. Annu Rev Neurosci 2001;24:487-517
   PubMed Web of Science ®Google Scholar
• Caterina MJ, Leffler A, Malmberg AB, Impaired nociception and pain sensation in mice lacking the capsaicin receptor. Science 2000;288:306-13
   PubMed Web of Science ®Google Scholar
• Davis JB, Gray J, Gunthorpe MJ, Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia. Nature 2000;405:183-7
   PubMed Web of Science ®Google Scholar
• Kasama S, Kawakubo M, Suzuki T, RNA interference-mediated knock-down of transient receptor potential vanilloid 1 prevents forepaw inflammatory hyperalgesia in rat. Eur J Neurosci 2007;25:2956-63
   PubMed Web of Science ®Google Scholar
• Christoph T, Gillen C, Mika J, Antinociceptive effect of antisense oligonucleotides against the vanilloid receptor VR1/TRPV1. Neurochem Int 2007;50:281-90
   PubMed Web of Science ®Google Scholar
• Knotkova H, Pappagallo M, Szallasi A. Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival? Clin J Pain 2008;24:142-54
   PubMed Web of Science ®Google Scholar
• Iadarola MJ, Mannes AJ. The vanilloid agonist resiniferatoxin for interventional-based pain control. Curr Top Med Chem 2011;11:2171-9
   PubMed Web of Science ®Google Scholar
• Faltynek C, Gomtsyan A. editors. Vanilloid receptor TRPV1 in drug discovery: targeting pain and other pathological disorders. John Wiley & Sons: Hoboken, NJ, USA; 2009
   Google Scholar
• Gunthorpe MJ, Szallasi A. Peripheral TRPV1 receptors as targets for drug development: new molecules and mechanisms. Curr Pharm Des 2008;14:32-41
   PubMed Web of Science ®Google Scholar
• Moran MM, McAlexander MA, Biro T, Szallasi A. Transient receptor potential channels as therapeutic targets. Nat Rev Drug Discov 2011;10:601-20
   PubMed Web of Science ®Google Scholar
• Preti D, Szallasi A, Patacchini R. TRP channels as therapeutic targets in airway disorders: a patent review. Exp Opin Ther Pat 2012;22:663-695. [in press]
   PubMed Web of Science ®Google Scholar
• Available from: http://www.xention.com/overactive-bladder
   Google Scholar
• Jancso N, Jancso A. Desensitization of sensory nerve endings. Kiserletes Orvostudomany 1949;2(2 Suppl):15
   Google Scholar
• Jancso N, Jancso-Gabor A, Szolcsanyi J. Direct evidence for neurogenic inflammation and its prevention by denervation and by pretreatment with capsaicin. Br J Pharmacol Chemother 1967;31:138-51
   PubMed Web of Science ®Google Scholar
• Jancso G, Kiraly E, Jancso-Gabor A. Pharmacologically induced selective degeneration of chemosensitive primary sensory neurones. Nature 1977;270:741-3
   PubMed Web of Science ®Google Scholar
• Szolcsanyi J. In: Malmberg AB, Bley KR, editors. Turning up the heat on pain: TRPV1 receptors in pain and inflammation. Birkhauser: Basel, Switzerland; 2005. p. 3-22
   Google Scholar
• Szallasi A. Vanilloid-sensitive neurons: a fundamental subdivision of the peripheral nervous system. J Peripher Nerv Syst 1996;1:6-18
   PubMedGoogle Scholar
• Levy DM, Abraham RR, Tomlinson DR. Topical capsaicin in the treatment of painful diabetic neuropathy. N Engl J Med 1991;324:776-7
   PubMed Web of Science ®Google Scholar
• Noto C, Pappagallo M, Szallasi A. NGX-4010, a high-concentration capsaicin dermal patch for lasting relief of peripheral neuropathic pain. Curr Opin Investig Drugs 2009;10:702-10
   PubMed Web of Science ®Google Scholar
• Kennedy WR, Vanhove GF, Lu SP, 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 2010;11:579-87
   PubMed Web of Science ®Google Scholar
• Simpson DM, Gazda S, Brown S, Long-term safety of NGX-4010, a high-concentration capsaicin patch, in patients with peripheral neuropathic pain. J Pain Symptom Manage 2010;39:1053-64
   PubMed Web of Science ®Google Scholar
• Jones VM, Moore KA, Peterson DM. Capsaicin 8% patch (Qutenza) – a review of the evidence. J Pain Palliat Care Pharmacother 2011;25:32-41
   PubMedGoogle Scholar
• Neurogesx company website. Clinical trial Number (NCT01228838). Available from: http://www.neurogesx.com/c204_clinical_trial. http://www.clinicaltrial.gov/ct2/show/NCT01228838?term=NCT01228838&rank=1
   Google Scholar
• Webster LR, Peppin JF, Murphy FT, Efficacy, safety, and tolerability of NGX-4010, capsaicin 8% patch, in an open-label study of patients with peripheral neuropathic pain. Diabetes Res Clin Pract 2011;93:187-97
   PubMed Web of Science ®Google Scholar
• Szallasi A, Blumberg PM. Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper. Neuroscience 1989;30:515-20
   PubMed Web of Science ®Google Scholar
• Szolcsanyi J, Szallasi A, Szallasi Z, Resiniferatoxin, an ultrapotent selective modulator of capsaicin-sensitive primary sensory neurons. J Pharmacol Exp Ther 1990;255:923-8
   PubMed Web of Science ®Google Scholar
• Kissin I, Szallasi A. Therapeutic targeting of TRPV1 by resiniferatoxin, from preclinical studies to clinical trials. Curr Top Med Chem 2011;11:2159-70
   PubMed Web of Science ®Google Scholar
• Kissin I. Vanilloid-induced conduction analgesia, selective, long-lasting, dose-dependent, with a low level of potential neurotoxicity. Anesth Analg 2008;107:261-71
   Google Scholar
• Jeffrey JA, Yu SQ, Sikard P, Selective targeting of TRPV1 expressing sensory nerve terminals in the spinal cord for long lasting analgesia. PLoS ONE 2009;4:7021-5
   Google Scholar
• Liu L, Oortgiesen AM, Simon SA. Capsaicin inhibits activation of voltage-gated sodium currents in capsaicin-sensitive trigeminal ganglion neurons. J Neurophysiol 2001;85:745-58
   PubMed Web of Science ®Google Scholar
• Kissin I, Davison N, Bradley EL Jr. Perineural resiniferatoxin prevents hyperalgesia in a model of postoperative pain. Anesth Analg 2005;10:774-80
   Google Scholar
• Kissin I, Bright CA, Bradley EL Jr. Selective and long-lasting blockade with resiniferatoxin prevents inflammatory pain hypersensitivity. Anesth Analg 2002;94:1253-8
   PubMed Web of Science ®Google Scholar
• Neubert JK, Laszlo K, Jun J, Peripherally induced resiniferatoxin analgesia. Pain 2003;104:219-28
   PubMed Web of Science ®Google Scholar
• Neubert JK, Mannes AJ, Laszlo K, Perineural resiniferatoxin selectively inhibits inflammatory hyperalgesia. Mol Pain 2008;4:1-10
   PubMedGoogle Scholar
• Kissin I, Freitas CF, Bradley EL Jr. Preineural resiniferatoxin prevents the development of hyperalgesia produced by loose ligation of the sciatic nerve in rats. Anesth Analg 2007;104:1210-16
   PubMed Web of Science ®Google Scholar
• Kissin EY, Freitas CF, Kissin I. The effects of intraarticular resiniferatoxin in experimental knee-joint arthritis. Anesth Analg 2005;101:1433-9
   PubMed Web of Science ®Google Scholar
• Karai L, Brown DC, Mannes AJ, Deletion of the vanilloid receptor 1-expressing primary afferent neurons for pain control. J Clin Invest 2004;113:1344-52
   PubMed Web of Science ®Google Scholar
• Neubert JK, Mannes AJ, Keller J, Peripheral targeting of the trigeminal ganglia via the infraorbital foramen as a therapeutic strategy. Brain Res Brain Res Protoc 2005;15:119-25
   PubMedGoogle Scholar
• Brown DC, Iadarola MJ, Perkowski SZ, Physiologic and antinociceptive effects of intrathecal resiniferatoxin in a canine bone cancer model. Anesthesiology 2005;103:1052-9
   PubMed Web of Science ®Google Scholar
• Bates BD, Michell K, Keller JM, Prolonged analgesic response of cornea to topical resiniferatoxin, a potent TRPV1 agonist. Pain 2010;49:522-8
   Google Scholar
• Gharat L, Szallasi A. Advances in the design and therapeutic use of capsaicin receptor TRPV1 agonists and antagonists. Exp Opin Ther Patents 2008;18:159-209
   Web of Science ®Google Scholar
• Appendino G., Szallasi A. Progress in medicinal chemistry. Elsevier: Amsterdam, Netherlands; Vol. 44 2006. p. 145-80
   Google Scholar
• Chizh BA, O'Donnell MB, Napolitano A, The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans. Pain 2007;132:132-41
   PubMed Web of Science ®Google Scholar
• Rami HK, Thompson M, Stemp G, Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonists suitable for clinical development. Bioorg Med Chem Lett 2006;16:3287-91
   PubMed Web of Science ®Google Scholar
• Tekus V, Bolcskei K, Kiss-Varga A, Effect of the transient receptor potential vanilloid 1 (TRPV1) antagonist compounds SB-705498, BCTC and AMG9810 in rat models of thermal hyperalgesia measured with an increasing temperature water bath. Eur J Pharmacol 2010;641:135-41
   PubMed Web of Science ®Google Scholar
• Krarup AL, Ny L, Astrand M, Randomized clinical trial: the efficacy of the transient receptor potential vanilloid 1 antagonist AZD1386 in human oesophageal pain. Aliment Pharmacol Ther 2011;33:1113-22
   PubMed Web of Science ®Google Scholar
• Eid SR. Therapeutic targeting of TRP channels: the TR(i)P to pain relief. Curr Top Med Chem 2011;11:2118-30
   PubMed Web of Science ®Google Scholar
• Eid SR. In: 2009. Available from: http://www.arrowheadpublishers.com/conferences/pain-therapeutics-2009/agenda/Summit
   Google Scholar
• Available from: http://www.pharmeste.com/include/PHE377.pdf
   Google Scholar
• Trevisani M. TRPV1 antagonists for pain relief, cough and urinary incontinence. Available from: http://www.worldpharma2010/pp/W03.1.pdf
   Google Scholar
• Jancso-Gabor A, Szolcsanyi J, Jancso N. Irreversible impairment of thermoregulation induced by capsaicin and similar pungent substances in the rats and guinea pigs. J Physiol 1970;206:495-507
   PubMed Web of Science ®Google Scholar
• Hori T. Capsaicin and central control of thermoregulation. Pharmacol Ther 1984;26:389-416
   PubMed Web of Science ®Google Scholar
• Szolcsanyi J, Joo F, Jancso-Gabor A. Mitochondrial changes in preoptic neurons after capsaicin desensitization of the hypothalamic thermodetectors in the rat. Nature 1971;229:116-17
   PubMed Web of Science ®Google Scholar
• Gavva NR, Bannon AW, Surapaneni S, The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J Neurosci 2007;27:3366-74
   PubMed Web of Science ®Google Scholar
• Gavva NR, Treanor JJ, Garami A, Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. Pain 2008;136:202-10
   PubMed Web of Science ®Google Scholar
• Gavva NR, Bannon AW, Hovland DN Jr, Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther 2007;323:128-37
   PubMed Web of Science ®Google Scholar
• Iida T, Shimizu I, Nealen ML, Attenuated fever response in mice lacking TRPV1. Neurosci Lett 2005;378:28-33
   PubMed Web of Science ®Google Scholar
• Romanovsky AA, Almeida MC, Garami A, The transient receptor potential vanilloid-1 channel in thermoregulation: a thermosensor it is not. Pharmacol Rev 2009;61:228-61
   PubMed Web of Science ®Google Scholar
• Gavva NR. Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1. Trends Pharmacol Sci 2008;19:19-23
   Google Scholar
• Hajos M, Obal F Jr, Jancso G, Obal F. Capsaicin impairs preoptic serotonin-sensitive structures mediating hypothermia in rats. Neurosci Lett 1985;54:97-102
   PubMed Web of Science ®Google Scholar
• Cui M, Honore P, Zhong C, TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J Neurosci 2006;26:9385-93
   PubMed Web of Science ®Google Scholar
• Lehto SG, Tamir R, Deng H, 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;326:218-29
   PubMed Web of Science ®Google Scholar
• Kaszas K, Keller JM, Coddou C, Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. J Pharmacol Exp Ther 2012;340:152-60
   PubMed Web of Science ®Google Scholar
• Jancso G. editor. Neuroimmune biology. neurogenic inflammation in health and disease. Elsevier: Amsterdam, Netherlands; 2009
   Google Scholar
• Alawi K, Keeble J. The paradoxical role of the transient receptor potential vanilloid 1 receptor in inflammation. Pharmacol Ther 2010;125:181-91
   PubMed Web of Science ®Google Scholar
• Wanner SP, Garami A, Pakai E, Aging reverses the role of the transient receptor potential vanilloid 1 channel in systemic inflammation from antiinflammatory to pro-inflammatory. Cell Cycle 2012;11:343-9
   PubMed Web of Science ®Google Scholar
• Guptill V, Cui X, Khaibullina A, Disruption of the transient receptor potential vanilloid 1 can affect survival, bacterial clearance, and cytokine gene expression during murine sepsis. Anesthesiology 2011;114:1190-9
   PubMed Web of Science ®Google Scholar
• Clark N, Keeble J, Fernandes ES, The transient receptor potential vanilloid 1 (TRPV1) protects against the onset of sepsis after endotoxin. FASEB J 2007;21:3747-55
   PubMed Web of Science ®Google Scholar
• Quezado ZM, Szallasi A. TRPV1 antagonists may exacerbate sepsis in aged mice: should we be nervous? Cell Cycle 2012;11:647-8
   PubMed Web of Science ®Google Scholar
• Available from: http://www.qutenza.com
   Google Scholar
• Remadevi R, Szallasi A. Adlea (ALGRX-4975), an injectable capsaicin (TRPV1 receptor agonist) formulation for long lasting pain relief. IDrugs 2008;11:120-32
   PubMed Web of Science ®Google Scholar
• Available from: http://www.bizjournals.com/sanfrancisco/stories/2010/01/11/story4.html
   Google Scholar
• Bloomberg. NeurogesX fails to win US approval to sell patch for HIV-related pain. Available from: http://www.bloomberg.com/neurogesx-fails-to-win-u-s-approval-to-sell-patch-for-hiv-related-pain.html
   Google Scholar
• Cruz F, Dinis P. Resiniferatoxin and botulinum toxin type A for the treatment of lower urinary tract syndromes. Neurourol Urodyn 2007;26:920-7
   PubMed Web of Science ®Google Scholar
• Menendez L, Juarez L, Garcia E, Analgesic effects of capsazepine and resiniferatoxin on bone cancer pain in mice. Neurosci Lett 2006;393:70-3
   PubMed Web of Science ®Google Scholar
• Motter AL, Ahern GP. TRPV1 null mice are protected from diet-induced obesity. FASEB J 2008;582:2257-62
   Google Scholar
• Wanner SP, Garami A, Romanovsky AA. Hyperactive when young, hypoactive and overweight when aged: connecting the dots in the story about locomotor activity, body mass, and aging in trpv1 knockout mice. Aging 2011;3:450-4
   PubMedGoogle Scholar
• Available from: http://www.podiatry-arena.com/podiatry-forum/showthread.php?t.9707
   Google Scholar
• Malmberg AB, Mizisin AP, Calcutt NA, Reduced heat sensitivity and epidermal nerve fiber immunostaining following single applications of a high-concentration capsaicin patch. Pain 2004;111:360-7
   PubMed Web of Science ®Google Scholar
• Significant pain reduction for post-shingles patients. NeurogesX, Inc Press Release 2003 April 01 (neurogesx.com)
   Google Scholar
• Simpson DM, Estanislaso L, Brwn SJ, Sampson J. An open-label pilot study of high-concentration capsaicin patch in painful HIV neuropathy. J Pain Symptom Manage 2008;12:1106-12
   Google Scholar
• NeurogesX, Inc. Form 10-K. NeurogesX, Inc. Form 10-K 2008 March 26 (neurogesx.com)
   Google Scholar
• Webster LR, Tark M, Rauck R, Effect of duration of postherpetic neuralgia on efficacy analyses in a multicenter, randomized, controlled study of NGX-4010, an 8% capsaicin patch evaluated for the treatment of postherpetic neuralgia. BMC Neurol 2010;10:92
   PubMed Web of Science ®Google Scholar
• Backonfa M, Wallace MS, Blonsky ER, NGX-4010, a high-concentration capsaicin patch, for the treatment of postherpetic neuralgia: a randomized, double-blind study. Lancet Neurol 2008;12:1106-12
   Google Scholar
• Irving GA, Backonja MM, Dunteman E, A multicenter, randomized, double-blind, controlled study of NGX-4010, a high-concentration capsaicin patch, for the treatment of postherpetic neuralgia. Pain Med 2011;1:99-109
   Google Scholar
• Simpson DM, Browen S, Tobias J. Controlled trial of high-concentration capsaicin patch for treatment of painful HIV neuropathy. Neurology 2008;28:2305-13
   Google Scholar