메뉴 건너뛰기




Volumn 306, Issue 1, 2003, Pages 377-386

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

Author keywords

[No Author keywords available]

Indexed keywords

ANALGESIC AGENT; CALCIUM ION; CAPSAICIN; CAPSAZEPINE; ENZYME; N (4 TERT BUTYLPHENYL) 4 (3 CHLOROPYRIDIN 2 YL)TETRAHYDROPYRAZINE 1(2H) CARBOXAMIDE; PYRAZINE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; VANILLOID RECEPTOR; VANILLOID RECEPTOR 1 ANTAGONIST;

EID: 0038467306     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.045674     Document Type: Article
Times cited : (207)

References (41)
  • 1
    • 0009644628 scopus 로고
    • Some quantitative uses of drug antagonists
    • Arunlakshana O and Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol 14:48-58.
    • (1959) Br J Pharmacol , vol.14 , pp. 48-58
    • Arunlakshana, O.1    Schild, H.O.2
  • 2
    • 0001951152 scopus 로고    scopus 로고
    • Extracellullar protons both increase the activity and reduce the conductance of capsaicin-gated channels
    • Baumann TK and Martenson ME (2000) Extracellullar protons both increase the activity and reduce the conductance of capsaicin-gated channels. J Neurosci 20:RC80 (1-5).
    • (2000) J Neurosci , vol.20 , Issue.1-5
    • Baumann, T.K.1    Martenson, M.E.2
  • 3
    • 0036277884 scopus 로고    scopus 로고
    • Vanilloid and TRP channels: A family of lipid-gated cation channels
    • Benham CD, Davis JB, and Randall AD (2002) Vanilloid and TRP channels: a family of lipid-gated cation channels. Neuropharmacology 42:873-888.
    • (2002) Neuropharmacology , vol.42 , pp. 873-888
    • Benham, C.D.1    Davis, J.B.2    Randall, A.D.3
  • 4
    • 0000685271 scopus 로고
    • Capsazepine does not block the proton-induced activation of rat sensory neurons
    • Bevan S, Rang HP, and Shah K (1992) Capsazepine does not block the proton-induced activation of rat sensory neurons. Br J Pharmacol 107:235P.
    • (1992) Br J Pharmacol , vol.107
    • Bevan, S.1    Rang, H.P.2    Shah, K.3
  • 5
    • 0026100801 scopus 로고
    • Protons activate a cation conductance in a sub-population of rat dorsal root ganglion neurons
    • Bevan S and Yeats JC (1991) Protons activate a cation conductance in a sub-population of rat dorsal root ganglion neurons. J Physiol (Lond) 433:145-161.
    • (1991) J Physiol (Lond) , vol.433 , pp. 145-161
    • Bevan, S.1    Yeats, J.C.2
  • 10
    • 0029081831 scopus 로고
    • Inflammatory mediators of pain
    • Dray A (1995) Inflammatory mediators of pain. Br J Anaesth 75:125-131.
    • (1995) Br J Anaesth , vol.75 , pp. 125-131
    • Dray, A.1
  • 11
    • 0029012887 scopus 로고
    • Effects of capsazepine against capsaicin- and proton-evoked excitation of single airway C-fibers and vagus nerve from the guinea-pig
    • Fox AJ, Urban L, Barnes PJ, and Dray A (1995) Effects of capsazepine against capsaicin- and proton-evoked excitation of single airway C-fibers and vagus nerve from the guinea-pig. Neuroscience 67:741-752.
    • (1995) Neuroscience , vol.67 , pp. 741-752
    • Fox, A.J.1    Urban, L.2    Barnes, P.J.3    Dray, A.4
  • 12
    • 0033555286 scopus 로고    scopus 로고
    • Transmitters involved in antinociception in the spinal cord
    • Furst S (1999) Transmitters involved in antinociception in the spinal cord. Brain Res Bull 48:129-141.
    • (1999) Brain Res Bull , vol.48 , pp. 129-141
    • Furst, S.1
  • 13
    • 0034616036 scopus 로고    scopus 로고
    • Interactions of inflammatory mediators and low pH not influenced by capsazepine in rat cutaneous nociceptors
    • Habelt C, Kessler F, Distler C, Kress M, and Reeh PW (2000) Interactions of inflammatory mediators and low pH not influenced by capsazepine in rat cutaneous nociceptors. Neuroreport 11:973-976.
    • (2000) Neuroreport , vol.11 , pp. 973-976
    • Habelt, C.1    Kessler, F.2    Distler, C.3    Kress, M.4    Reeh, P.W.5
  • 16
    • 0036183319 scopus 로고    scopus 로고
    • Molecular basis for species-specific sensitivity to "hot" chili peppers
    • Jordt S-E and Julius D (2002) Molecular basis for species-specific sensitivity to "hot" chili peppers. Cell 108:421-430.
    • (2002) Cell , vol.108 , pp. 421-430
    • Jordt, S.-E.1    Julius, D.2
  • 17
    • 0034608878 scopus 로고    scopus 로고
    • Acid potentiation of the capsaicin receptor determined by a key extracellular site
    • Jordt S-E, Tominaga M, and Julius D (2000) Acid potentiation of the capsaicin receptor determined by a key extracellular site. Proc Natl Acad Sci USA 97:8134-8139.
    • (2000) Proc Natl Acad Sci USA , vol.97 , pp. 8134-8139
    • Jordt, S.-E.1    Tominaga, M.2    Julius, D.3
  • 19
    • 0027103748 scopus 로고
    • Inhibition of low pH evoked activation of airway sensory nerves by capsazepine, a novel capsaicin-receptor antagonist
    • Lou YP and Lundberg JM (1992) Inhibition of low pH evoked activation of airway sensory nerves by capsazepine, a novel capsaicin-receptor antagonist. Biochem Biophys Res Commun 189:537-544.
    • (1992) Biochem Biophys Res Commun , vol.189 , pp. 537-544
    • Lou, Y.P.1    Lundberg, J.M.2
  • 21
    • 0028884581 scopus 로고
    • Effects of intravenous ketamine, alfentanil or placebo on pain, pinprick hyperalgesia and allodynia produced by intradermal capsaicin in human subjects
    • Park KM, Max MM, Robinovitz E, Gracely RH, and Bennet GJ (1995) Effects of intravenous ketamine, alfentanil or placebo on pain, pinprick hyperalgesia and allodynia produced by intradermal capsaicin in human subjects. Pain 63:163-172.
    • (1995) Pain , vol.63 , pp. 163-172
    • Park, K.M.1    Max, M.M.2    Robinovitz, E.3    Gracely, R.H.4    Bennet, G.J.5
  • 22
    • 0035150677 scopus 로고    scopus 로고
    • The ligand that came from within
    • Piomelli D (2001) The ligand that came from within. Trends Pharmacol Sci 22:17-19.
    • (2001) Trends Pharmacol Sci , vol.22 , pp. 17-19
    • Piomelli, D.1
  • 23
    • 0038128285 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. II. In vivo characterization in rat models of inflammatory and neuropathic pain
    • Pomonis JD, Harrison J, Mark L, Waligora DT, Valenzano KJ, and Walker K (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. II. In vivo characterization in rat models of inflammatory and neuropathic pain. J Pharmacol Exp Ther 306:387-393.
    • (2003) J Pharmacol Exp Ther , vol.306 , pp. 387-393
    • Pomonis, J.D.1    Harrison, J.2    Mark, L.3    Waligora, D.T.4    Valenzano, K.J.5    Walker, K.6
  • 24
    • 0022903329 scopus 로고
    • Sensory receptors in mammalian skin in an in vitro preparation
    • Reeh PW (1986) Sensory receptors in mammalian skin in an in vitro preparation. Neurosci Lett 66:141-146.
    • (1986) Neurosci Lett , vol.66 , pp. 141-146
    • Reeh, P.W.1
  • 26
    • 0027174913 scopus 로고
    • Inhibitory effects of capsazepine and SR 48968 on citric acid-induced bronchoconstriction in guinea pigs
    • Satoh H, Lou YP, and Lundberg JM (1993) Inhibitory effects of capsazepine and SR 48968 on citric acid-induced bronchoconstriction in guinea pigs. Eur J Pharmacol 236:367-372.
    • (1993) Eur J Pharmacol , vol.236 , pp. 367-372
    • Satoh, H.1    Lou, Y.P.2    Lundberg, J.M.3
  • 28
    • 0036894895 scopus 로고    scopus 로고
    • Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenyla-cetate ester) iodo-resiniferatoxin
    • Seabrook GR, Sutton KG, Jarolimek W, Hollingworth GJ, Teague S, Webb J, Clark N, Boyce S, Kerby J, Ali Z, et al. (2002) Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenyla-cetate ester) iodo-resiniferatoxin. J Pharmacol Exp Ther 303:1052-1060.
    • (2002) J Pharmacol Exp Ther , vol.303 , pp. 1052-1060
    • Seabrook, G.R.1    Sutton, K.G.2    Jarolimek, W.3    Hollingworth, G.J.4    Teague, S.5    Webb, J.6    Clark, N.7    Boyce, S.8    Kerby, J.9    Ali, Z.10
  • 29
    • 0027171235 scopus 로고
    • Capsaicin-induced activation of fine afferent fibers from rat skin in vitro
    • Seno N and Dray A (1993) Capsaicin-induced activation of fine afferent fibers from rat skin in vitro. Neuroscience 55:563-569.
    • (1993) Neuroscience , vol.55 , pp. 563-569
    • Seno, N.1    Dray, A.2
  • 30
    • 0023203334 scopus 로고
    • Hyperalgesia to heat after intradermal injection of capsaicin
    • Simone DA, Ngeow JYF, Putterman GJ, and Lamotte RH (1987) Hyperalgesia to heat after intradermal injection of capsaicin. Brain Res 418:201-203.
    • (1987) Brain Res , vol.418 , pp. 201-203
    • Simone, D.A.1    Ngeow, J.Y.F.2    Putterman, G.J.3    Lamotte, R.H.4
  • 32
    • 0026581550 scopus 로고
    • Protons selectively induce lasting excitation and sensitization to mechanical stimulation of nociceptors in rat skin in vitro
    • Steen KH, Reeh OW, 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, O.W.2    Anton, F.3    Handwerker, H.O.4
  • 33
    • 0032876069 scopus 로고    scopus 로고
    • The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons
    • Szallasi A, Blumberg PM, Annicelli LL, Krause JE, and Cortright DN (1999) The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons. Mol Pharmacol 56:581-587.
    • (1999) Mol Pharmacol , vol.56 , pp. 581-587
    • Szallasi, A.1    Blumberg, P.M.2    Annicelli, L.L.3    Krause, J.E.4    Cortright, D.N.5
  • 35
    • 2642623583 scopus 로고    scopus 로고
    • Inflammatory mediators at acidic pH activate capsaicin receptors in cultured sensory neurons from newborn rats
    • Vyklicky L, Knotkova-Urbancova H, Vitaskova Z, Vlachova V, Kress M, and Reeh PW (1998) Inflammatory mediators at acidic pH activate capsaicin receptors in cultured sensory neurons from newborn rats. J Neurophysiol 79:670-676.
    • (1998) J Neurophysiol , vol.79 , pp. 670-676
    • Vyklicky, L.1    Knotkova-Urbancova, H.2    Vitaskova, Z.3    Vlachova, V.4    Kress, M.5    Reeh, P.W.6
  • 37
    • 0037215646 scopus 로고    scopus 로고
    • The VR1 antagonist, capsazepine, reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain
    • Walker K, Urban L, Medhurst SJ, Patel S, Panesar M, Fox AJ, and McIntyre P (2003) The VR1 antagonist, capsazepine, reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain. J Pharmacol Exp Ther 304:56-62.
    • (2003) J Pharmacol Exp Ther , vol.304 , pp. 56-62
    • Walker, K.1    Urban, L.2    Medhurst, S.J.3    Patel, S.4    Panesar, M.5    Fox, A.J.6    McIntyre, P.7
  • 40
    • 0034610391 scopus 로고    scopus 로고
    • The activation mechanism of rat vanilloid receptor 1 by capsaicin involves the pore domain and differs from the activation by either acid or heat
    • Welch JM, Simon SA, and Reinhart PH (2000) The activation mechanism of rat vanilloid receptor 1 by capsaicin involves the pore domain and differs from the activation by either acid or heat. Proc Natl Acad Sci USA 97:13889-13894.
    • (2000) Proc Natl Acad Sci USA , vol.97 , pp. 13889-13894
    • Welch, J.M.1    Simon, S.A.2    Reinhart, P.H.3
  • 41
    • 0025031914 scopus 로고
    • Application of liquid chromatography with on-line radiochemical detection to metabolism studies on a novel class of analgesics
    • Wehmeyer KR, Kasting GB, Powell JH, Kuhlenbeck DL, Underwood RA, and Bowman LA (1990) Application of liquid chromatography with on-line radiochemical detection to metabolism studies on a novel class of analgesics. J Pharm Biomed Anal 8:177-183.
    • (1990) J Pharm Biomed Anal , vol.8 , pp. 177-183
    • Wehmeyer, K.R.1    Kasting, G.B.2    Powell, J.H.3    Kuhlenbeck, D.L.4    Underwood, R.A.5    Bowman, L.A.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.