메뉴 건너뛰기




Volumn 4, Issue 2, 2009, Pages 159-180

Screening TRPV1 antagonists for the treatment of pain: Lessons learned over a decade

Author keywords

Pain; TRPV1

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 (4 TRIFLUOROMETHYLBENZYL) 3 (ISOQUINOL 5 YL) UREA; 2 (4 PYRIDIN 2 YLPIPERAZIN 1 YL) 1H BENZO[D]IMIDAZOLE; 3 (4 TERT BUTYLPHENYL) N (2,3 DIHYDROBENZO[B][1,4] DIOXIN 6 YL)ACRYLAMIDE; 4 (3 TRIFLUOROMETHYLPYRIDIN 2 YL) 1 (5 TRIFLUOROMETHYLPYRIDIN 2 YL)PIPERAZINE 1 CARBOXAMIDE; 4 CHLORO N (3 METHOXYPHENYL)CINNAMAMIDE; A 425619; ABT 102; AMG 2674; AMG 517; AMG 628; AMG 8562; AMG 9810; AMG 986; ANTINOCICEPTIVE AGENT; AZD 1386; CANNABINOID 1 RECEPTOR; CAPSAICIN; CAPSAZEPINE; CYCLIC AMP DEPENDENT PROTEIN KINASE; GRC 6211; JNJ 17203212; JYL 1421; LJO 328; N (2 HYDROXY 2,3 DIHYDRO 1H INDEN 4 YL) 3 [2 (PIPERIDIN 1 YL) 4 (TRIFLUOROMETHYL)PHENYL]ACRYLAMIDE; N (4 TERT BUTYLBENZYL) N' [1 [3 FLUORO 4 (METHYLSULFONYLAMINO)PHENYL]ETHYL]THIOUREA; N (4 TERT BUTYLBENZYL) N' [3 FLUORO 4 (METHYLSULFONYLAMINO)BENZYL]THIOUREA; N (4 TERT BUTYLBENZYL) N' [4 (METHYLSULFONYLAMINO)BENZYL]THIOUREA; N [4 [6 (4 TRIFLUOROMETHYLPHENYL)PYRIMIDIN 4 YLOXY]BENZOTHIAZOL 2 YL]ACETAMIDE; NGD 8243; NONSTEROID ANTIINFLAMMATORY AGENT; PHOSPHOLIPASE A2; SB 452533; TRANSIENT RECEPTOR POTENTIAL CHANNEL M; UNCLASSIFIED DRUG; UNINDEXED DRUG; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 1 BLOCKING AGENT; VANILLOID RECEPTOR 4;

EID: 67649206465     PISSN: 17460441     EISSN: None     Source Type: Journal    
DOI: 10.1517/17460440802681300     Document Type: Review
Times cited : (47)

References (135)
  • 2
    • 27644561673 scopus 로고    scopus 로고
    • Available from: [Cited 2008 ]
    • Decade of Pain Control and Research Available from: http://www.ampainsoc. org/decadeofpain [Cited 2008 ]
    • Decade of Pain Control and Research
  • 4
    • 0032970173 scopus 로고    scopus 로고
    • Vanilloid (Capsaicin) receptors and mechanisms
    • Szallasi A, Blumberg PM. Vanilloid (Capsaicin) receptors and mechanisms. Pharmacol Rev 1999;51:159-212
    • (1999) Pharmacol Rev , vol.51 , pp. 159-212
    • Szallasi, A.1    Blumberg, P.M.2
  • 5
    • 38549118896 scopus 로고    scopus 로고
    • Capsaicin (TRPV1 agonist) therapy for pain relief - Farewell or revival?
    • Knotkova H, Pappagallo M, Szallasi A. Capsaicin (TRPV1 agonist) therapy for pain relief - Farewell or revival? Clin J Pain 2008;24:142-154
    • (2008) Clin J Pain , vol.24 , pp. 142-154
    • Knotkova, H.1    Pappagallo, M.2    Szallasi, A.3
  • 7
    • 34248138496 scopus 로고    scopus 로고
    • The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept
    • DOI 10.1038/nrd2280, PII NRD2280
    • 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;6:357-372 (Pubitemid 46705200)
    • (2007) Nature Reviews Drug Discovery , vol.6 , Issue.5 , pp. 357-372
    • Szallasi, A.1    Cortright, D.N.2    Blum, C.A.3    Eid, S.R.4
  • 8
    • 67649223280 scopus 로고    scopus 로고
    • Available from: [Cited 2008]
    • Migraine trials with SB-705498. Available from: http://clinicaltrials. gov/ct2/show/NCT00269022?term=SB705498&rank=1 [Cited 2008]
    • Migraine Trials with SB-705498
  • 9
    • 67649215836 scopus 로고    scopus 로고
    • Available from: [Cited 2008]
    • Merck "pipeline" Available from: http://www.merck.com/finance/ pipeline.swf [Cited 2008]
    • Merck "Pipeline"
  • 10
    • 41749117999 scopus 로고    scopus 로고
    • Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans
    • Gavva NR, Treanor JJS, Garami A, et al. Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. Pain 2008;136:202-210
    • (2008) Pain , vol.136 , pp. 202-210
    • Gavva, N.R.1    Treanor, J.J.S.2    Garami, A.3
  • 15
    • 34547953765 scopus 로고    scopus 로고
    • ThermoTRP channels as modular proteins with allosteric gating
    • DOI 10.1016/j.ceca.2007.04.004, PII S0143416007000772
    • Latorre R, Brauchi S, Orta G, et al. Thermo TRP channels as modular proteins with allosteric gating. Cell Calcium 2007;42:427-438 (Pubitemid 47264003)
    • (2007) Cell Calcium , vol.42 , Issue.4-5 , pp. 427-438
    • Latorre, R.1    Brauchi, S.2    Orta, G.3    Zaelzer, C.4    Vargas, G.5
  • 17
    • 24944546513 scopus 로고    scopus 로고
    • Gadolinium activates and sensitizes the vanilloid receptor TRPV1 through the external protonation sites
    • DOI 10.1016/j.mcn.2005.07.004, PII S1044743105001508
    • Tousova K, Vyklicky L, Susankova K, et al. Gadolinium activates and sensitizes the vanilloid receptor TRPV1 through the external protonation sites. Mol Cell Neurosci 2005;30:207-217 (Pubitemid 41319675)
    • (2005) Molecular and Cellular Neuroscience , vol.30 , Issue.2 , pp. 207-217
    • Tousova, K.1    Vyklicky, L.2    Susankova, K.3    Benedikt, J.4    Vlachova, V.5
  • 18
    • 33646899582 scopus 로고    scopus 로고
    • A hot-sensing cold receptor: C-terminal domain determines thermosensation in transient receptor potential channels
    • DOI 10.1523/JNEUROSCI.5080-05.2006
    • Brauchi S, Orta G, Salazar M, et al. A hot-sensing cold receptor: C-terminal domain determines thermosensation in transient receptor potential channels. J Neurosci 2006;26:4835-4840 (Pubitemid 44315324)
    • (2006) Journal of Neuroscience , vol.26 , Issue.18 , pp. 4835-4840
    • Brauchi, S.1    Orta, G.2    Salazar, M.3    Rosenmann, E.4    Latorre, R.5
  • 19
    • 25644433563 scopus 로고    scopus 로고
    • Camphor activates and strongly desensitizes the transient receptor potential vanilloid subtype 1 channel in a vanilloid-independent mechanism
    • DOI 10.1523/JNEUROSCI.2574-05.2005
    • Xu HX, Blair NT, Clapham DE. Camphor activates and strongly desensitizes the transient receptor potential vanilloid subtype 1 channel in a vanilloid-independent mechanism. J Neurosci 2005;25:8924-8937 (Pubitemid 41384461)
    • (2005) Journal of Neuroscience , vol.25 , Issue.39 , pp. 8924-8937
    • Xu, H.1    Blair, N.T.2    Clapham, D.E.3
  • 21
    • 33947697100 scopus 로고    scopus 로고
    • Biochemistry and pharmacology of endovanilloids
    • Starowicz K, Nigam S, Di Marzo V. Biochemistry and pharmacology of endovanilloids. Pharmacol Ther 2007;114:13-33
    • (2007) Pharmacol Ther , vol.114 , pp. 13-33
    • Starowicz, K.1    Nigam, S.2    Di Marzo, V.3
  • 23
    • 44049107494 scopus 로고    scopus 로고
    • Novel gating and sensitizing mechanism of capsaicin receptor (TRPV1) - Tonic inhibitory regulation of extracellular sodium through the external protonation sites on TRPV1
    • Ohta T, Imagawa T, Ito S. Novel gating and sensitizing mechanism of capsaicin receptor (TRPV1) - Tonic inhibitory regulation of extracellular sodium through the external protonation sites on TRPV1. J Biol Chem 2008;283:9377-9387
    • (2008) J Biol Chem , vol.283 , pp. 9377-9387
    • Ohta, T.1    Imagawa, T.2    Ito, S.3
  • 24
    • 0032967640 scopus 로고    scopus 로고
    • Immunocytochemical localization of the vanilloid receptor 1 (VR1): Relationship to neuropeptides, the P2X(3) purinoceptor and IB4 binding sites
    • Guo A, Vulchanova L, Wang J, et al. Immunocytochemical localization of the vanilloid receptor 1 (VR1): relationship to neuropeptides, the P2X(3) purinoceptor and IB4 binding sites. Eur J Neurosci 1999;11:946-958
    • (1999) Eur J Neurosci , vol.11 , pp. 946-958
    • Guo, A.1    Vulchanova, L.2    Wang, J.3
  • 25
    • 2442696310 scopus 로고    scopus 로고
    • Biochemical pharmacology of the vanilloid receptor TRPV1: An update
    • DOI 10.1111/j.1432-1033.2004.04082.x
    • Cortright DN, Szallasi A. Biochemical pharmacology of the vanilloid receptor TRPV1. An update. Eur J Biochem 2004;271:1814-1819 (Pubitemid 38657335)
    • (2004) European Journal of Biochemistry , vol.271 , Issue.10 , pp. 1814-1819
    • Cortright, D.W.1    Szallasi, A.2
  • 26
    • 33750524257 scopus 로고    scopus 로고
    • Phosphoinositide 3-kinase binds to TRPV1 and mediates NGF-stimulated TRPV1 trafficking to the plasma membrane
    • DOI 10.1085/jgp.200609576
    • Stein AT, Ufret-Vincenty CA, Hua L, et al. Phosphoinositide 3-kinase binds to TRPV1 and mediates NGF-stimulated TRPV1 trafficking to the plasma membrane. J Gen Physiol 2006;128:509-522 (Pubitemid 44664629)
    • (2006) Journal of General Physiology , vol.128 , Issue.5 , pp. 509-522
    • Stein, A.T.1    Ufret-Vincenty, C.A.2    Hua, L.3    Santana, L.F.4    Gordon, S.E.5
  • 27
    • 29244484493 scopus 로고    scopus 로고
    • NGF rapidly increases membrane expression of TRPV1 heat-gated ion channels
    • DOI 10.1038/sj.emboj.7600893
    • Zhang XM, Huang JH, McNaughton PA. NGF rapidly increases membrane expression of TRPV1 heat-gated ion channels. EMBO J 2005;24:4211-4223 (Pubitemid 41828897)
    • (2005) EMBO Journal , vol.24 , Issue.24 , pp. 4211-4223
    • Zhang, X.1    Huang, J.2    McNaughton, P.A.3
  • 28
    • 0036605663 scopus 로고    scopus 로고
    • Hot channels in airways: Pharmacology of the vanilloid receptor
    • DOI 10.1016/S1471-4892(02)00149-2
    • Hwang SW, Oh U. Hot channels in airways: pharmacology of the vanilloid receptor. Curr Opin Pharmacol 2002;2:235-242 (Pubitemid 34594361)
    • (2002) Current Opinion in Pharmacology , vol.2 , Issue.3 , pp. 235-242
    • Hwang, S.W.1    Oh, U.2
  • 29
    • 0033166535 scopus 로고    scopus 로고
    • Specific involvement of PKC-epsilon in sensitization of the neuronal response to painful heat
    • DOI 10.1016/S0896-6273(00)80813-2
    • Cesare P, Dekker LV, Sardini A, et al. Specific involvement of PKC-epsilon in sensitization of the neuronal response to painful heat. Neuron 1999;23:617-624 (Pubitemid 29359931)
    • (1999) Neuron , vol.23 , Issue.3 , pp. 617-624
    • Cesare, P.1    Dekker, L.V.2    Sardini, A.3    Parker, P.J.4    McNaughton, P.A.5
  • 30
    • 44949131718 scopus 로고    scopus 로고
    • Protein kinase A anchoring via AKAP150 is essential for TRPV1 modulation by forskolin and prostaglandin E2 in mouse sensory neurons
    • Schnizler K, Shutov LP, Van Kanegan MJ, et al. Protein kinase A anchoring via AKAP150 is essential for TRPV1 modulation by forskolin and prostaglandin E2 in mouse sensory neurons. J Neurosci 2008;28:4904-4917
    • (2008) J Neurosci , vol.28 , pp. 4904-4917
    • Schnizler, K.1    Shutov, L.P.2    Van Kanegan, M.J.3
  • 31
    • 48749115596 scopus 로고    scopus 로고
    • Proinflammatory mediators modulate the heat-activated ion channel TRPV1 via the scaffolding protein AKAP79/150
    • Zhang X, Li L, McNaughton PA. Proinflammatory mediators modulate the heat-activated ion channel TRPV1 via the scaffolding protein AKAP79/150. Neuron 2008;59:450-461
    • (2008) Neuron , vol.59 , pp. 450-461
    • Zhang, X.1    Li, L.2    McNaughton, P.A.3
  • 32
    • 50249119619 scopus 로고    scopus 로고
    • A-kinase anchoring protein mediates TRPV1 thermal hyperalgesia through PKA phosphorylation of TRPV1
    • [Epub ahead of print]
    • Jeske NA, Diogenes A, Ruparel NB, et al. A-kinase anchoring protein mediates TRPV1 thermal hyperalgesia through PKA phosphorylation of TRPV1. Pain 2008 [Epub ahead of print]
    • (2008) Pain
    • Jeske, N.A.1    Diogenes, A.2    Ruparel, N.B.3
  • 33
    • 0028943777 scopus 로고
    • Association of protein-kinase-a and protein-phosphatase-2b with a common anchoring rotein
    • Coghlan VM, Perrino BA, Howard M, et al. Association of protein-kinase-a and protein-phosphatase-2b with a common anchoring rotein. Science 1995;267:108-111
    • (1995) Science , vol.267 , pp. 108-111
    • Coghlan, V.M.1    Perrino, B.A.2    Howard, M.3
  • 34
    • 0029887701 scopus 로고    scopus 로고
    • Coordination of three signaling enzymes by AKAP79, a mammalian scaffold protein
    • Klauck TM, Faux MC, Labudda K, et al. Coordination of three signaling enzymes by AKAP79, a mammalian scaffold protein. Science 1996;271:1589-1592 (Pubitemid 26097218)
    • (1996) Science , vol.271 , Issue.5255 , pp. 1589-1592
    • Klauck, T.M.1    Faux, M.C.2    Labudda, K.3    Langeberg, L.K.4    Jaken, S.5    Scott, J.D.6
  • 36
    • 33750399000 scopus 로고    scopus 로고
    • Potentiation of transient receptor potential V1 functions by the activation of metabotropic 5-HT receptors in rat primary sensory neurons
    • DOI 10.1113/jphysiol.2006.112250
    • Ohta T, Ikemi Y, Murakami M, et al. Potentiation of transient receptor potential V1 functions by the activation of metabotropic 5-HT receptors in rat primary sensory neurons. J Physiol 2006;576:809-822 (Pubitemid 44637885)
    • (2006) Journal of Physiology , vol.576 , Issue.3 , pp. 809-822
    • Ohta, T.1    Ikemi, Y.2    Murakami, M.3    Imagawa, T.4    Otsuguro, K.-I.5    Ito, S.6
  • 37
    • 2342466078 scopus 로고    scopus 로고
    • Histamine-induced Ca2+ influx via the PLA(2)/lipoxygenase/TRPV1 pathway in rat sensory neurons
    • Kim BM, Lee SH, Shim WS, Oh U. Histamine-induced Ca2+ influx via the PLA(2)/lipoxygenase/TRPV1 pathway in rat sensory neurons. Neurosci Lett 2004;361:159-162
    • (2004) Neurosci Lett , vol.361 , pp. 159-162
    • Kim, B.M.1    Lee, S.H.2    Shim, W.S.3    Oh, U.4
  • 38
    • 0035927651 scopus 로고    scopus 로고
    • Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5) P2-mediated inhibition
    • Chuang HH, Prescott ED, Kong H, et al. Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5) P2-mediated inhibition. Nature 2001;411:957-962
    • (2001) Nature , vol.411 , pp. 957-962
    • Chuang, H.H.1    Prescott, E.D.2    Kong, H.3
  • 39
    • 0037799198 scopus 로고    scopus 로고
    • 2 binding site as a determinant of capsaicin receptor sensitivity
    • DOI 10.1126/science.1083646
    • Prescott ED, Julius D. A modular PIP2 binding site as a determinant of capsaicin receptor sensitivity. Science 2003;300:1284-1288 (Pubitemid 36618238)
    • (2003) Science , vol.300 , Issue.5623 , pp. 1284-1288
    • Prescott, E.D.1    Julius, D.2
  • 41
    • 42949125051 scopus 로고    scopus 로고
    • Pirt, a Phosphoinositide-Binding Protein, Functions as a Regulatory Subunit of TRPV1
    • DOI 10.1016/j.cell.2008.02.053, PII S0092867408005060
    • Kim AY, Tang ZX, Liu Q, et al. Pirt, a phosphoinositide-binding protein, functions as a regulatory subunit of TRPV1. Cell 2008;133:475-485 (Pubitemid 351608697)
    • (2008) Cell , vol.133 , Issue.3 , pp. 475-485
    • Kim, A.Y.1    Tang, Z.2    Liu, Q.3    Patel, K.N.4    Maag, D.5    Geng, Y.6    Dong, X.7
  • 42
    • 0034700494 scopus 로고    scopus 로고
    • Induction of vanilloid receptor channel activity by protein kinase C
    • DOI 10.1038/35050121
    • Premkumar LS, Ahern GP. Induction of vanilloid receptor channel activity by protein kinase C. Nature 2000;408:985-990 (Pubitemid 32101646)
    • (2000) Nature , vol.408 , Issue.6815 , pp. 985-990
    • Premkumar, L.S.1    Ahern, G.P.2
  • 43
    • 0035425705 scopus 로고    scopus 로고
    • Protein kinase C activation potentiates gating of the vanilloid receptor VR1 by capsaicin, protons, heat and anandamide
    • DOI 10.1111/j.1469-7793.2001.00813.x
    • Vellani V, Mapplebeck S, Moriondo A, et al. Protein kinase C activation potentiates gating of the vanilloid receptor VR1 by capsaicin, protons, heat and anandamide. J Physiol 2001;534:813-825 (Pubitemid 32700878)
    • (2001) Journal of Physiology , vol.534 , Issue.3 , pp. 813-825
    • Vellani, V.1    Mapplebeck, S.2    Moriondo, A.3    Davis, J.B.4    McNaughton, P.A.5
  • 45
    • 0037134417 scopus 로고    scopus 로고
    • Direct phosphorylation of capsaicin receptor VR1 by protein kinase Cepsilon and identification of two target serine residues
    • DOI 10.1074/jbc.C200104200
    • Numazaki M, Tominaga T, Toyooka H, Tominaga M. Direct phosphorylation of capsaicin receptor VR1 by protein kinase Cepsilon and identification of two target serine residues. J Biol Chem 2002;277:13375-13378 (Pubitemid 34967929)
    • (2002) Journal of Biological Chemistry , vol.277 , Issue.16 , pp. 13375-13378
    • Numazaki, M.1    Tominaga, T.2    Toyooka, H.3    Tominaga, M.4
  • 46
    • 2942614748 scopus 로고    scopus 로고
    • Regulated exocytosis contributes to protein kinase C potentiation of vanilloid receptor activity
    • DOI 10.1074/jbc.M311515200
    • Morenilla-Palao C, Planells-Cases R, Garcia-Sanz N, Ferrer-Montiel A. Regulated exocytosis contributes to protein kinase C potentiation of vanilloid receptor activity. J Biol Chem 2004;279:25665-25672 (Pubitemid 38756829)
    • (2004) Journal of Biological Chemistry , vol.279 , Issue.24 , pp. 25665-25672
    • Morenilla-Palao, C.1    Planells-Cases, R.2    Garcia-Sanz, N.3    Ferrer-Montiel, A.4
  • 47
    • 44949251781 scopus 로고    scopus 로고
    • Endogenous tumor necrosis factor alpha (TNFalpha) requires TNF receptor type 2 to generate heat hyperalgesia in a mouse cancer model
    • Constantin CE, Mair N, Sailer CA, et al. Endogenous tumor necrosis factor alpha (TNFalpha) requires TNF receptor type 2 to generate heat hyperalgesia in a mouse cancer model. J Neurosci 2008;28:5072-5081
    • (2008) J Neurosci , vol.28 , pp. 5072-5081
    • Constantin, C.E.1    Mair, N.2    Sailer, C.A.3
  • 48
    • 45749148702 scopus 로고    scopus 로고
    • Neurokinin 2 receptor-mediated activation of protein kinase C modulates capsaicin responses in DRG neurons from adult rats
    • DOI 10.1111/j.1460-9568.2008.06267.x
    • Sculptoreanu A, Aura Kullmann F, de Groat WC. Neurokinin 2 receptor-mediated activation of protein kinase C modulates capsaicin responses in DRG neurons from adult rats. Eur J Neurosci 2008;27:3171-3181 (Pubitemid 351863592)
    • (2008) European Journal of Neuroscience , vol.27 , Issue.12 , pp. 3171-3181
    • Sculptoreanu, A.1    Aura Kullmann, F.2    De Groat, W.C.3
  • 50
    • 33748180653 scopus 로고    scopus 로고
    • The mu opioid agonist morphine modulates potentiation of capsaicin-evoked TRPV1 responses through a cyclic AMP-dependent protein kinase a pathway
    • DOI 10.1186/1744-8069-2-22
    • Vetter I, Wyse BD, Monteith GR, et al. The mu opioid agonist morphine modulates potentiation of capsaicin-evoked TRPV1 responses through a cyclic AMP-dependent protein kinase A pathway. Mol Pain 2006;2:22-29 (Pubitemid 44308920)
    • (2006) Molecular Pain , vol.2 , pp. 22
    • Vetter, I.1    Wyse, B.D.2    Monteith, G.R.3    Roberts-Thomson, S.J.4    Cabot, P.J.5
  • 52
    • 17144397173 scopus 로고    scopus 로고
    • 2+-dependent desensitization in the vanilloid receptor TRPV1 by calcineurin and cAMP-dependent protein kinase
    • DOI 10.1074/jbc.M410917200
    • Mohapatra DP, Nau C. Regulation of Ca2+-dependent desensitization in the vanilloid receptor TRPV1 by calcineurin and cAMP-dependent protein kinase. J Biol Chem 2005;280:13424-13432 (Pubitemid 40517230)
    • (2005) Journal of Biological Chemistry , vol.280 , Issue.14 , pp. 13424-13432
    • Mohapatra, D.P.1    Nau, C.2
  • 54
    • 0036183319 scopus 로고    scopus 로고
    • Molecular basis for species-specific sensitivity to "hot" chili peppers
    • Jordt SE, Julius D. Molecular basis for species-specific sensitivity to "hot" chili peppers. Cell 2002;108:421-430
    • (2002) Cell , vol.108 , pp. 421-430
    • Jordt, S.E.1    Julius, D.2
  • 58
    • 0025224503 scopus 로고
    • Resiniferatoxin - An ultrapotent selective modulator of capsaicin-sensitive primary afferent neurons
    • Szolcsanyi J, Szallasi A, Szallasi Z, et al. Resiniferatoxin - an ultrapotent selective modulator of capsaicin-sensitive primary afferent neurons. J Pharmacol Exp Ther 1990;255:923-928
    • (1990) J Pharmacol Exp Ther , vol.255 , pp. 923-928
    • Szolcsanyi, J.1    Szallasi, A.2    Szallasi, Z.3
  • 59
    • 0028868678 scopus 로고
    • Vanilloid (capsaicin) receptors in the rat: Distribution in the brain, regional differences in the spinal cord, axonal transport to the periphery, and depletion by systemic vanilloid treatment
    • Szallasi A, Nilsson S, Farkas-Szallasi T, et al. Vanilloid (capsaicin) receptors in the rat: distribution in the brain, regional differences in the spinal cord, axonal transport to the periphery, and depletion by systemic vanilloid treatment. Brain Res 1995;703:175-183
    • (1995) Brain Res , vol.703 , pp. 175-183
    • Szallasi, A.1    Nilsson, S.2    Farkas-Szallasi, T.3
  • 61
    • 29144457594 scopus 로고    scopus 로고
    • Pain research update from a genetic point of view
    • DOI 10.1111/j.1533-2500.2005.00036.x
    • Sery O, Hrazdilova O, Matalova E, Sevcik P. Pain research update from a genetic point of view. Pain Pract 2005;5:341-348 (Pubitemid 41807083)
    • (2005) Pain Practice , vol.5 , Issue.4 , pp. 341-348
    • Sery, O.1    Hrazdilova, O.2    Matalova, E.3    Sevcik, P.4
  • 62
    • 13244298667 scopus 로고    scopus 로고
    • Are mu-opioid receptor polymorphisms important for clinical opioid therapy?
    • Lotsch J, Geisslinger G. Are mu-opioid receptor polymorphisms important for clinical opioid therapy? Trends Mol Med 2005;11:82-89
    • (2005) Trends Mol Med , vol.11 , pp. 82-89
    • Lotsch, J.1    Geisslinger, G.2
  • 64
    • 33846269106 scopus 로고    scopus 로고
    • Genetic predictors for acute experimental cold and heat pain sensitivity in humans
    • Kim H, Mittal DP, Iadarola MJ, Dionne RA. Genetic predictors for acute experimental cold and heat pain sensitivity in humans. J Med Genet 2006;43:e40
    • (2006) J Med Genet , vol.43
    • Kim, H.1    Mittal, D.P.2    Iadarola, M.J.3    Dionne, R.A.4
  • 65
    • 34247874778 scopus 로고    scopus 로고
    • Loss-of-function mutations in the Na(v)1.7 gene underlie congenital indifference to pain in multiple human populations
    • Goldberg YP, MacFarlane J, MacDonald ML, et al. Loss-of-function mutations in the Na(v)1.7 gene underlie congenital indifference to pain in multiple human populations. Clin Genet 2007;71:311-319
    • (2007) Clin Genet , vol.71 , pp. 311-319
    • Goldberg, Y.P.1    MacFarlane, J.2    MacDonald, M.L.3
  • 66
    • 42449107733 scopus 로고    scopus 로고
    • Genetic mutations that prevent pain: Implications for future pain medication
    • DOI 10.2217/14622416.9.2.179
    • Oertel B, Lotsch J. Genetic mutations that prevent pain: implications for future pain medication. Pharmacogenomics 2008;9:179-194 (Pubitemid 351566942)
    • (2008) Pharmacogenomics , vol.9 , Issue.2 , pp. 179-194
    • Oertel, B.1    Lotsch, J.2
  • 68
    • 2442420245 scopus 로고    scopus 로고
    • Genetic influence on variability in human acute experimental pain sensitivity associated with gender, ethnicity and psychological temperament
    • DOI 10.1016/j.pain.2004.02.027, PII S0304395904001198
    • Kim H, Neubert JK, San Miguel A, et al. Genetic influence on variability in human acute experimental pain sensitivity associated with gender, ethnicity and psychological temperament. Pain 2004;109:488-496 (Pubitemid 38638726)
    • (2004) Pain , vol.109 , Issue.3 , pp. 488-496
    • Kim, H.1    Neubert, J.K.2    San Miguel, A.3    Xu, K.4    Krishnaraju, R.K.5    Iadarola, M.J.6    Goldman, D.7    Dionne, R.A.8
  • 70
    • 40749097682 scopus 로고    scopus 로고
    • Advances in the design and therapeutic use of capsaicin receptor TRPV1 agonists and antagonists
    • Gharat LA, Szallasi A. Advances in the design and therapeutic use of capsaicin receptor TRPV1 agonists and antagonists. Exp Opin Ther Patents 2008;18:159-209
    • (2008) Exp Opin Ther Patents , vol.18 , pp. 159-209
    • Gharat, L.A.1    Szallasi, A.2
  • 71
    • 0028021842 scopus 로고
    • The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin
    • DOI 10.1021/jm00039a006
    • Walpole CSJ, Bevan S, Bovermann G, et al. The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin. J Med Chem 1994;37:1942-1954 (Pubitemid 24233606)
    • (1994) Journal of Medicinal Chemistry , vol.37 , Issue.13 , pp. 1942-1954
    • Walpole, C.S.J.1    Bevan, S.2
  • 72
    • 0026767602 scopus 로고
    • Capsazepine - A competitive antagonist of the sensory neuron excitant capsaicin
    • Bevan S, Hothi S, Hughes G, et al. Capsazepine - a competitive antagonist of the sensory neuron excitant capsaicin. Br J Pharmacol 1992;107:544-552
    • (1992) Br J Pharmacol , vol.107 , pp. 544-552
    • Bevan, S.1    Hothi, S.2    Hughes, G.3
  • 73
    • 0027452376 scopus 로고
    • 3H]resiniferatoxin binding to central (spinal cord and dorsal root ganglia) and peripheral (urinary bladder and airways) vanilloid (capsaicin) receptors in the rat
    • Szallasi A, Goso C, Blumberg PM, Manzini S. Competitive-inhibition by capsazepine of [H-3] resiniferatoxin binding to central (spinal-cord and dorsal-root ganglia) and peripheral (urinary-bladder and airways) vanilloid (capsaicin) receptors in the rat. J Pharmacol Exp Ther 1993;267:728-733 (Pubitemid 23352531)
    • (1993) Journal of Pharmacology and Experimental Therapeutics , vol.267 , Issue.2 , pp. 728-733
    • Szallasi, A.1    Goso, C.2    Blumberg, P.M.3    Manzini, S.4
  • 74
  • 76
    • 1842453817 scopus 로고    scopus 로고
    • Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay
    • DOI 10.1038/sj.bjp.0705652
    • Behrendt HJ, Germann T, Gillen C, et al. Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay. Br J Pharmacol 2004;141:737-745 (Pubitemid 38453266)
    • (2004) British Journal of Pharmacology , vol.141 , Issue.4 , pp. 737-745
    • Behrendt, H.-J.1    Germann, T.2    Gillen, C.3    Hatt, H.4    Jostock, R.5
  • 78
    • 23944483778 scopus 로고    scopus 로고
    • 5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro
    • DOI 10.1124/jpet.105.084277
    • Shimizu I, Iida T, Horiuchi N, Caterina MJ. 5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro. J Pharmacol Exp Ther 2005;314:1378-1385 (Pubitemid 41206005)
    • (2005) Journal of Pharmacology and Experimental Therapeutics , vol.314 , Issue.3 , pp. 1378-1385
    • Shimizu, I.1    Iida, T.2    Horiuchi, N.3    Caterina, M.J.4
  • 79
    • 0035173995 scopus 로고    scopus 로고
    • Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist
    • Wahl P, Foged C, Tullin S, Thomsen C. Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist. Mol Pharmacol 2001;59:9-15
    • (2001) Mol Pharmacol , vol.59 , pp. 9-15
    • Wahl, P.1    Foged, C.2    Tullin, S.3    Thomsen, C.4
  • 80
    • 33645103126 scopus 로고    scopus 로고
    • Kinetics of penetration influence the apparent potency of vanilloids on TRPV1
    • Lazar J, Braun DC, Toth A, et al. Kinetics of penetration influence the apparent potency of vanilloids on TRPV1. Mol Pharmacol 2006;69:1166-1173
    • (2006) Mol Pharmacol , vol.69 , pp. 1166-1173
    • Lazar, J.1    Braun, D.C.2    Toth, A.3
  • 81
    • 33645572464 scopus 로고    scopus 로고
    • Participation of the spinal TRPV1 receptors in formalin-evoked pain transduction: A study using a selective TRPV1 antagonist, iodo-resiniferatoxin
    • Kanai Y, Hara T, Imai A. Participation of the spinal TRPV1 receptors in formalin-evoked pain transduction: a study using a selective TRPV1 antagonist, iodo-resiniferatoxin. J Pharm Pharmacol 2006;58:489-493
    • (2006) J Pharm Pharmacol , vol.58 , pp. 489-493
    • Kanai, Y.1    Hara, T.2    Imai, A.3
  • 84
    • 0036783709 scopus 로고    scopus 로고
    • High affinity antagonists of the vanilloid receptor
    • Wang Y, Szabo T, Welter JD, et al. High affinity antagonists of the vanilloid receptor. Mol Pharmacol 2002;62:947-956
    • (2002) Mol Pharmacol , vol.62 , pp. 947-956
    • Wang, Y.1    Szabo, T.2    Welter, J.D.3
  • 86
    • 34548670044 scopus 로고    scopus 로고
    • The role of transient receptor potential vanilloid 1 in mechanical and chemical visceral hyperalgesia following experimental colitis
    • DOI 10.1016/j.neuroscience.2007.05.034, PII S030645220700646X
    • Miranda A, Nordstrom E, Mannem A, et al. The role of transient receptor potential vanilloid 1 in mechanical and chemical visceral hyperalgesia following experimental colitis. Neuroscience 2007;148:1021-1032 (Pubitemid 47419190)
    • (2007) Neuroscience , vol.148 , Issue.4 , pp. 1021-1032
    • Miranda, A.1    Nordstrom, E.2    Mannem, A.3    Smith, C.4    Banerjee, B.5    Sengupta, J.N.6
  • 88
    • 1642498152 scopus 로고    scopus 로고
    • Design of a High-Affinity Competitive Antagonist of the Vanilloid Receptor Selective for the Calcium Entry-Linked Receptor Population
    • DOI 10.1124/mol.65.2.282
    • Toth A, Blumberg PM, Chen Z, Kozikowski AP. Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population. Mol Pharmacol 2004;65:282-291 (Pubitemid 38134255)
    • (2004) Molecular Pharmacology , vol.65 , Issue.2 , pp. 282-291
    • Toth, A.1    Blumberg, P.M.2    Chen, Z.3    Kozikowski, A.P.4
  • 89
    • 34247281575 scopus 로고    scopus 로고
    • Antinociceptive pharmacology of N-(4-chlorobenzyl)-N′-(4-hydroxy-3- Iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor
    • DOI 10.1124/jpet.106.117572
    • Tang L, Chen Y, Chen ZL, et al. Antinociceptive pharmacology of N-(4-chlorobenzyl)-N′-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor. J Pharmacol Exp Ther 2007;321:791-798 (Pubitemid 46624524)
    • (2007) Journal of Pharmacology and Experimental Therapeutics , vol.321 , Issue.2 , pp. 791-798
    • Tang, L.1    Chen, Y.2    Chen, Z.3    Blumberg, P.M.4    Kozikowski, A.P.5    Wang, Z.J.6
  • 91
    • 20144362216 scopus 로고    scopus 로고
    • 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
    • Gavva NR, Tamir R, Qu YS, et al. 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;313:474-484
    • (2005) J Pharmacol Exp Ther , vol.313 , pp. 474-484
    • Gavva, N.R.1    Tamir, R.2    Qu, Y.S.3
  • 92
    • 67649240813 scopus 로고    scopus 로고
    • Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1
    • Gavva NR. Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1. Trends Pharmacol Sci 2008;19:19-23
    • (2008) Trends Pharmacol Sci , vol.19 , pp. 19-23
    • Gavva, N.R.1
  • 94
    • 0038128285 scopus 로고    scopus 로고
    • 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
    • Pomonis JD, Harrison JE, Mark L, et al. 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;306:387-393
    • (2003) J Pharmacol Exp Ther , vol.306 , pp. 387-393
    • Pomonis, J.D.1    Harrison, J.E.2    Mark, L.3
  • 101
    • 48649096712 scopus 로고    scopus 로고
    • Aminoquinazolines as TRPV1 antagonists: Modulation of drug-like properties through the exploration of 2-position substitution
    • Blum CA, Zheng X, Brielmann H, et al. Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution. Bioorg Med Chem Lett 2008;18:4573-4577
    • (2008) Bioorg Med Chem Lett , vol.18 , pp. 4573-4577
    • Blum, C.A.1    Zheng, X.2    Brielmann, H.3
  • 109
    • 53849138741 scopus 로고    scopus 로고
    • (R)-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) blocks polymodal activation of transient receptor potential vanilloid 1 receptors in vitro and heat-evoked firing of spinal dorsal horn neurons in vivo
    • Surowy CS, Neelands TR, Bianchi BR, et al. (R)-(5-tert-butyl-2,3-dihydro- 1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) blocks polymodal activation of transient receptor potential vanilloid 1 receptors in vitro and heat-evoked firing of spinal dorsal horn neurons in vivo. J Pharmacol Exp Ther 2008;326:879-888
    • (2008) J Pharmacol Exp Ther , vol.326 , pp. 879-888
    • Surowy, C.S.1    Neelands, T.R.2    Bianchi, B.R.3
  • 111
    • 34547573343 scopus 로고    scopus 로고
    • Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides
    • Norman MH, Zhu JW, Fotsch C, et al. Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides. J Med Chem 2007;50:3497-3514
    • (2007) J Med Chem , vol.50 , pp. 3497-3514
    • Norman, M.H.1    Zhu, J.W.2    Fotsch, C.3
  • 116
    • 33646043767 scopus 로고    scopus 로고
    • Increasingly irritable and close to tears: TRPA1 in inflammatory pain
    • McMahon SB, Wood JN. Increasingly irritable and close to tears: TRPA1 in inflammatory pain. Cell 2006;124:1123-1125
    • (2006) Cell , vol.124 , pp. 1123-1125
    • McMahon, S.B.1    Wood, J.N.2
  • 117
    • 54949145332 scopus 로고    scopus 로고
    • Spinal interleukin-1beta in a mouse model of arthritis and joint pain
    • Fiorentino PM, Tallents RH, Miller JN, et al. Spinal interleukin-1beta in a mouse model of arthritis and joint pain. Arthritis Rheum 2008;58:3100-3109
    • (2008) Arthritis Rheum , vol.58 , pp. 3100-3109
    • Fiorentino, P.M.1    Tallents, R.H.2    Miller, J.N.3
  • 118
    • 33645969571 scopus 로고    scopus 로고
    • Chronic IL-1beta signaling potentiates voltage-dependent sodium currents in trigeminal nociceptive neurons
    • Liu L, Yang TM, Liedtke W, Simon SA. Chronic IL-1beta signaling potentiates voltage-dependent sodium currents in trigeminal nociceptive neurons. J Neurophysiol 2006;95:1478-1490
    • (2006) J Neurophysiol , vol.95 , pp. 1478-1490
    • Liu, L.1    Yang, T.M.2    Liedtke, W.3    Simon, S.A.4
  • 119
    • 0029001071 scopus 로고
    • Sensory denervation with capsaicin attenuates inflammation and nocicpetion in arthritic rats
    • Cruwys SC, Garrett NE, Kidd BC. Sensory denervation with capsaicin attenuates inflammation and nocicpetion in arthritic rats. Neurosci Lett 1995;193:205-207
    • (1995) Neurosci Lett , vol.193 , pp. 205-207
    • Cruwys, S.C.1    Garrett, N.E.2    Kidd, B.C.3
  • 121
    • 0142062922 scopus 로고    scopus 로고
    • Mechanism of action of analgesics used to treat osteoarthritis pain
    • DOI 10.1016/S0889-857X(03)00058-9
    • Raffa RB. Mechanism of action of analgesics used to treat osteoarthritis pain. Rheum Dis Clin North Am 2003;29:733-745 (Pubitemid 37296768)
    • (2003) Rheumatic Disease Clinics of North America , vol.29 , Issue.4 , pp. 733-745
    • Raffa, R.B.1
  • 127
    • 0038467306 scopus 로고    scopus 로고
    • N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl) tetrahydropyrazine- 1(2H)-carbox-amide(BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. In vitro characterization and pharmacokinetic properties
    • Valenzano KJ, Grant ER, Wu G, et al. N-(4-tertiarybutylphenyl)-4-(3- chloropyridin-2-yl) tetrahydropyrazine- 1(2H)-carbox-amide(BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. In vitro characterization and pharmacokinetic properties. J Pharmacol Exp Ther 2003;306:377-386
    • (2003) J Pharmacol Exp Ther , vol.306 , pp. 377-386
    • Valenzano, K.J.1    Grant, E.R.2    Wu, G.3
  • 128
    • 53049105094 scopus 로고    scopus 로고
    • Characterization of A-425619 at native TRPV1 receptors: A comparison between dorsal root ganglia and trigeminal ganglia
    • McDonald HA, Neelands TR, Kort M, et al. Characterization of A-425619 at native TRPV1 receptors: A comparison between dorsal root ganglia and trigeminal ganglia. Eur J Pharmacol 2008
    • (2008) Eur J Pharmacol
    • McDonald, H.A.1    Neelands, T.R.2    Kort, M.3
  • 129
    • 34547560453 scopus 로고    scopus 로고
    • Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate
    • Doherty EM, Fotsch C, Bannon AW, et al. Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J Med Chem 2007;50:3515-3527
    • (2007) J Med Chem , vol.50 , pp. 3515-3527
    • Doherty, E.M.1    Fotsch, C.2    Bannon, A.W.3
  • 130
    • 34547556499 scopus 로고    scopus 로고
    • Novel vanilloid receptor-1 antagonists:3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties
    • Wang HL, Katon J, Balan C, et al. Novel vanilloid receptor-1 antagonists:3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. J Med Chem 2007;50:3528-3539
    • (2007) J Med Chem , vol.50 , pp. 3528-3539
    • Wang, H.L.1    Katon, J.2    Balan, C.3
  • 133
    • 27144440511 scopus 로고    scopus 로고
    • Involvement of an increased spinal TRPV1 sensitization through its up-regulation in mechanical allodynia of CCI rats
    • DOI 10.1016/j.neuropharm.2005.05.003, PII S0028390805001863
    • Kanai Y, Nakazato E, Fujiuchi A, et al. Involvement of an increased spinal TRPV1 sensitization through its up-regulation in mechanical allodynia of CCI rats. Neuropharmacology 2005;49:977-984 (Pubitemid 41503297)
    • (2005) Neuropharmacology , vol.49 , Issue.7 , pp. 977-984
    • Kanai, Y.1    Nakazato, E.2    Fujiuchi, A.3    Hara, T.4    Imai, A.5
  • 134
    • 33644805715 scopus 로고    scopus 로고
    • Systemic and site-specific effects of A-425619, a selective TRPV1 receptor antagonist, on wide dynamic range neurons in CFA-treated and uninjured rats
    • DOI 10.1152/jn.00560.2005
    • McGaraughty S, Chu KL, Faltynek CR, Jarvis MF. Systemic and site-specific effects of A-425619, a selective TRPV1 receptor antagonist, on wide dynamic range neurons in CFA-treated and uninjured rats. J Neurophysiol 2006;95:18-25 (Pubitemid 44698913)
    • (2006) Journal of Neurophysiology , vol.95 , Issue.1 , pp. 18-25
    • McGaraughty, S.1    Chu, K.L.2    Faltynek, C.R.3    Jarvis, M.F.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.