메뉴 건너뛰기




Volumn 326, Issue 3, 2008, Pages 879-888

(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

Author keywords

[No Author keywords available]

Indexed keywords

(5 TERT BUTYL 2,3 DIHYDRO 1H INDEN 1 YL) 3 (1H INDAZOL 4 YL)UREA; ABT 102; ALLYL ISOTHIOCYANATE; ANANDAMIDE; CALCITONIN GENE RELATED PEPTIDE; CALCIUM ION; CAPSAICIN; CAPSAZEPINE; FREUND ADJUVANT; MENTHOL; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; INDAZOLE DERIVATIVE; TRPV1 RECEPTOR; UREA; VANILLOID RECEPTOR;

EID: 53849138741     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.108.138511     Document Type: Article
Times cited : (55)

References (42)
  • 1
    • 34447511473 scopus 로고    scopus 로고
    • Application of large-scale transiently transfected cells to functional assays of ion channels: Different targets and assay formats
    • Bianchi BR, Moreland RB, Faltynek CR, and Chen J (2007) Application of large-scale transiently transfected cells to functional assays of ion channels: different targets and assay formats. Assay Drug Dev Technol 5:417-424.
    • (2007) Assay Drug Dev Technol , vol.5 , pp. 417-424
    • Bianchi, B.R.1    Moreland, R.B.2    Faltynek, C.R.3    Chen, J.4
  • 3
    • 0141634247 scopus 로고    scopus 로고
    • Signalling pathways involved in the sensitization of mouse nociceptive neurones by nerve growth factor
    • Bonnington JK and McNaughton PA (2003) Signalling pathways involved in the sensitization of mouse nociceptive neurones by nerve growth factor. J Physiol 551:433-446.
    • (2003) J Physiol , vol.551 , pp. 433-446
    • Bonnington, J.K.1    McNaughton, P.A.2
  • 4
    • 0035823409 scopus 로고    scopus 로고
    • Peripheral capsaicin receptors increase in the inflamed rat hindpaw: A possible mechanism for peripheral sensitization
    • Carlton SM and Coggeshall RE (2001) Peripheral capsaicin receptors increase in the inflamed rat hindpaw: a possible mechanism for peripheral sensitization. Neurosci Lett 310:53-56.
    • (2001) Neurosci Lett , vol.310 , pp. 53-56
    • Carlton, S.M.1    Coggeshall, R.E.2
  • 5
    • 53849119374 scopus 로고    scopus 로고
    • Casillas LN, Jeong JU, and Marquis RW (2006, inventors; SmithKline Beecham Corp U.S, assignees. Acyclic 1,3-diamines and uses therefor. World patent WO2006029210. 2006 March 16
    • Casillas LN, Jeong JU, and Marquis RW (2006), inventors; SmithKline Beecham Corp (U.S.), assignees. Acyclic 1,3-diamines and uses therefor. World patent WO2006029210. 2006 March 16.
  • 6
    • 0034926291 scopus 로고    scopus 로고
    • The vanilloid receptor: A molecular gateway to the pain pathway
    • Caterina MJ and Julius D (2001) The vanilloid receptor: a molecular gateway to the pain pathway. Annu Rev Neurosci 24:487-517.
    • (2001) Annu Rev Neurosci , vol.24 , pp. 487-517
    • Caterina, M.J.1    Julius, D.2
  • 8
    • 2442696310 scopus 로고    scopus 로고
    • Biochemical pharmacology of the vanilloid receptor TRPV1: An update
    • Cortright DN and Szallasi A (2004) Biochemical pharmacology of the vanilloid receptor TRPV1: an update. Eur J Biochem 271:1814-1819.
    • (2004) Eur J Biochem , vol.271 , pp. 1814-1819
    • Cortright, D.N.1    Szallasi, A.2
  • 10
    • 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, Bo Y, Chen N, Dominguez C, Falsey J, Gavva NR, Katon J, Nixey T, et al. (2007) Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J Med Chem 50:3515-3527.
    • (2007) J Med Chem , vol.50 , pp. 3515-3527
    • Doherty, E.M.1    Fotsch, C.2    Bannon, A.W.3    Bo, Y.4    Chen, N.5    Dominguez, C.6    Falsey, J.7    Gavva, N.R.8    Katon, J.9    Nixey, T.10
  • 11
    • 33751000197 scopus 로고    scopus 로고
    • Differential contribution of TRPV1 to thermal responses and tissue injury-induced sensitization of dorsal horn neurons in laminae I and V in the mouse
    • Eckert WA 3rd, Julius D, and Basbaum AI (2006) Differential contribution of TRPV1 to thermal responses and tissue injury-induced sensitization of dorsal horn neurons in laminae I and V in the mouse. Pain 126:184-197.
    • (2006) Pain , vol.126 , pp. 184-197
    • Eckert 3rd, W.A.1    Julius, D.2    Basbaum, A.I.3
  • 12
    • 23044473189 scopus 로고    scopus 로고
    • A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid
    • El Kouhen R, Surowy CS, Bianchi BR, Neelands TR, McDonald HA, Niforatos W, Gomtsyan A, Lee CH, Honore P, Sullivan JP, et al. (2005) A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid. J Pharmacol Exp Ther 314:400-409.
    • (2005) J Pharmacol Exp Ther , vol.314 , pp. 400-409
    • El Kouhen, R.1    Surowy, C.S.2    Bianchi, B.R.3    Neelands, T.R.4    McDonald, H.A.5    Niforatos, W.6    Gomtsyan, A.7    Lee, C.H.8    Honore, P.9    Sullivan, J.P.10
  • 14
  • 15
    • 20144362216 scopus 로고    scopus 로고
    • Gavva NR, Tamir R, Qu Y, Klionsky L, Zhang TJ, Immke D, Wang J, Zhu D, Vanderah TW, Porreca F, et al. (2005b) 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 313:474-484.
    • Gavva NR, Tamir R, Qu Y, Klionsky L, Zhang TJ, Immke D, Wang J, Zhu D, Vanderah TW, Porreca F, et al. (2005b) 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 313:474-484.
  • 17
    • 34248525022 scopus 로고    scopus 로고
    • Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor
    • Gunthorpe MJ, Hannan SL, Smart D, Jerman JC, Arpino S, Smith GD, Brough S, Wright J, Egerton J, Lappin SC, et al. (2007) Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor. J Pharmacol Exp Ther 321:1183-1192.
    • (2007) J Pharmacol Exp Ther , vol.321 , pp. 1183-1192
    • Gunthorpe, M.J.1    Hannan, S.L.2    Smart, D.3    Jerman, J.C.4    Arpino, S.5    Smith, G.D.6    Brough, S.7    Wright, J.8    Egerton, J.9    Lappin, S.C.10
  • 18
    • 0032695819 scopus 로고    scopus 로고
    • Inhibition of spinal protein kinase c reduces nerve injury-induced tactile allodynia in neuropathic rats
    • Hua XY, Chen P, and Yaksh TL (1999) Inhibition of spinal protein kinase c reduces nerve injury-induced tactile allodynia in neuropathic rats. Neurosci Lett 276:99-102.
    • (1999) Neurosci Lett , vol.276 , pp. 99-102
    • Hua, X.Y.1    Chen, P.2    Yaksh, T.L.3
  • 20
    • 33644861384 scopus 로고    scopus 로고
    • Enhancement of spontaneous and heat-evoked activity in spinal nociceptive neurons by the endovanilloid/endocannabinoid N-arachidonoyldopamine (NADA)
    • Huang SM and Walker JM (2006) Enhancement of spontaneous and heat-evoked activity in spinal nociceptive neurons by the endovanilloid/endocannabinoid N-arachidonoyldopamine (NADA). J Neurophysiol 95:1207-1212.
    • (2006) J Neurophysiol , vol.95 , pp. 1207-1212
    • Huang, S.M.1    Walker, J.M.2
  • 22
    • 23244444988 scopus 로고    scopus 로고
    • Inhibition of peripheral vanilloid TRPV1 receptors reduces noxious heat-evoked responses of dorsal horn neurons in naive, carrageenan-inflamed and neuropathic rats
    • Jhaveri MD, Elmes SJ, Kendall DA, and Chapman V (2005) 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 22:361-370.
    • (2005) Eur J Neurosci , vol.22 , pp. 361-370
    • Jhaveri, M.D.1    Elmes, S.J.2    Kendall, D.A.3    Chapman, V.4
  • 23
    • 0034608878 scopus 로고    scopus 로고
    • Acid potentiation of the capsaicin receptor determined by a key extracellular site
    • Jordt SE, Tominaga M, and Julius D (2000) Acid potentiation of the capsaicin receptor determined by a key extracellular site. Proc Natl Acad Sci U S A 97: 8134-8139.
    • (2000) Proc Natl Acad Sci U S A , vol.97 , pp. 8134-8139
    • Jordt, S.E.1    Tominaga, M.2    Julius, D.3
  • 24
    • 0030727883 scopus 로고    scopus 로고
    • Peripheral CGRP release as a marker for neurogenic inflammation: A model system for the study of neuropeptide secretion in rat paw skin
    • Kilo S, Harding-Rose C, Hargreaves KM, and Flores CM (1997) Peripheral CGRP release as a marker for neurogenic inflammation: a model system for the study of neuropeptide secretion in rat paw skin. Pain 73:201-207.
    • (1997) Pain , vol.73 , pp. 201-207
    • Kilo, S.1    Harding-Rose, C.2    Hargreaves, K.M.3    Flores, C.M.4
  • 25
    • 33645894707 scopus 로고    scopus 로고
    • The role of the capsaicin receptor TRPV1 and acid-sensing ion channels (ASICS) in proton sensitivity of subpopulations of primary nociceptive neurons in rats and mice
    • Leffler A, Monter B, and Koltzenburg M (2006) The role of the capsaicin receptor TRPV1 and acid-sensing ion channels (ASICS) in proton sensitivity of subpopulations of primary nociceptive neurons in rats and mice. Neuroscience 139:699-709.
    • (2006) Neuroscience , vol.139 , pp. 699-709
    • Leffler, A.1    Monter, B.2    Koltzenburg, M.3
  • 27
    • 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
    • McGaraughty S, Chu KL, Faltynek CR, and Jarvis MF (2006) 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 95:18-25.
    • (2006) J Neurophysiol , vol.95 , pp. 18-25
    • McGaraughty, S.1    Chu, K.L.2    Faltynek, C.R.3    Jarvis, M.F.4
  • 29
    • 1342344077 scopus 로고    scopus 로고
    • Enhancement of potency and efficacy of NADA by PKC-mediated phosphorylation of vanilloid receptor
    • Premkumar LS, Qi ZH, Van Buren J, and Raisinghani M (2004) Enhancement of potency and efficacy of NADA by PKC-mediated phosphorylation of vanilloid receptor. J Neurophysiol 91:1442-1449.
    • (2004) J Neurophysiol , vol.91 , pp. 1442-1449
    • Premkumar, L.S.1    Qi, Z.H.2    Van Buren, J.3    Raisinghani, M.4
  • 30
    • 33847628339 scopus 로고    scopus 로고
    • Critical evaluation of the colocalization between calcitonin gene-related peptide, substance P, transient receptor potential vanilloid subfamily type 1 immunoreactivities, and isolectin B4 binding in primary afferent neurons of the rat and mouse
    • Price TJ and Flores CM (2007) Critical evaluation of the colocalization between calcitonin gene-related peptide, substance P, transient receptor potential vanilloid subfamily type 1 immunoreactivities, and isolectin B4 binding in primary afferent neurons of the rat and mouse. J Pain 8:263-272.
    • (2007) J Pain , vol.8 , pp. 263-272
    • Price, T.J.1    Flores, C.M.2
  • 33
    • 34249717691 scopus 로고    scopus 로고
    • Potentiation of glutamatergic synaptic transmission by protein kinase C-mediated sensitization of TRPV1 at the first sensory synapse
    • Sikand P and Premkumar LS (2007) Potentiation of glutamatergic synaptic transmission by protein kinase C-mediated sensitization of TRPV1 at the first sensory synapse. J Physiol 581:631-647.
    • (2007) J Physiol , vol.581 , pp. 631-647
    • Sikand, P.1    Premkumar, L.S.2
  • 34
    • 27744472280 scopus 로고    scopus 로고
    • Inflammatory mediators convert anandamide into a potent activator of the vanilloid type 1 transient receptor potential receptor in nociceptive primary sensory neurons
    • Singh Tahim A, Sántha P, and Nagy I (2005) Inflammatory mediators convert anandamide into a potent activator of the vanilloid type 1 transient receptor potential receptor in nociceptive primary sensory neurons. Neuroscience 136:539-548.
    • (2005) Neuroscience , vol.136 , pp. 539-548
    • Singh Tahim, A.1    Sántha, P.2    Nagy, I.3
  • 36
    • 0026581550 scopus 로고
    • Protons selectively induce lasting excitation and sensitization to mechanical stimulation of nociceptors in rat skin, in vitro
    • Steen KH, Reeh PW, Anton F, and Handwerker HO (1992) Protons selectively induce lasting excitation and sensitization to mechanical stimulation of nociceptors in rat skin, in vitro. J Neurosci 12:86-95.
    • (1992) J Neurosci , vol.12 , pp. 86-95
    • Steen, K.H.1    Reeh, P.W.2    Anton, F.3    Handwerker, H.O.4
  • 37
    • 34248138496 scopus 로고    scopus 로고
    • The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept
    • Szallasi A, Cortright DN, Blum CA, and Eid SR (2007) The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov 6:357-372.
    • (2007) Nat Rev Drug Discov , vol.6 , pp. 357-372
    • Szallasi, A.1    Cortright, D.N.2    Blum, C.A.3    Eid, S.R.4
  • 39
    • 0035109136 scopus 로고    scopus 로고
    • Axonal transport of VR1 capsaicin receptor mRNA in primary afferents and its participation in inflammation-induced increase in capsaicin sensitivity
    • Tohda C, Sasaki M, Konemura T, Sasamura T, Itoh M, and Kuraishi Y (2001) Axonal transport of VR1 capsaicin receptor mRNA in primary afferents and its participation in inflammation-induced increase in capsaicin sensitivity. J Neurochem 76:1628-1635.
    • (2001) J Neurochem , vol.76 , pp. 1628-1635
    • Tohda, C.1    Sasaki, M.2    Konemura, T.3    Sasamura, T.4    Itoh, M.5    Kuraishi, Y.6
  • 41
    • 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, Hachicha M, Schmid L, Tafesse L, Sun Q, Rotshteyn Y, Francis J, Limberis J, et al. (2003) 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 306:377-386.
    • (2003) J Pharmacol Exp Ther , vol.306 , pp. 377-386
    • Valenzano, K.J.1    Grant, E.R.2    Wu, G.3    Hachicha, M.4    Schmid, L.5    Tafesse, L.6    Sun, Q.7    Rotshteyn, Y.8    Francis, J.9    Limberis, J.10
  • 42
    • 0035939450 scopus 로고    scopus 로고
    • Vanilloid receptor VR1 is both presynaptic and postsynaptic in the superficial laminae of the rat dorsal horn
    • Valtschanoff JG, Rustioni A, Guo A, and Hwang SJ (2001) Vanilloid receptor VR1 is both presynaptic and postsynaptic in the superficial laminae of the rat dorsal horn. J Comp Neurol 436:225-235.
    • (2001) J Comp Neurol , vol.436 , pp. 225-235
    • Valtschanoff, J.G.1    Rustioni, A.2    Guo, A.3    Hwang, S.J.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.