-
2
-
-
80855148142
-
An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects
-
Round P, Priestley A, Robinson J. An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects. Br J Clin Pharmacol 2011; 72: 921-931.
-
(2011)
Br J Clin Pharmacol
, vol.72
, pp. 921-931
-
-
Round, P.1
Priestley, A.2
Robinson, J.3
-
3
-
-
0030777012
-
The capsaicin receptor: a heat-activated ion channel in the pain pathway
-
Caterina MJ, Schumacher MA, Tominaga M, Rosen TA, Levine JD, Julius D. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature 1997; 389: 816-824.
-
(1997)
Nature
, vol.389
, pp. 816-824
-
-
Caterina, M.J.1
Schumacher, M.A.2
Tominaga, M.3
Rosen, T.A.4
Levine, J.D.5
Julius, D.6
-
4
-
-
0032169804
-
The cloned capsaicin receptor integrates multiple pain-producing stimuli
-
Tominaga M, Caterina MJ, Malmberg AB, Rosen TA, Gilbert H, Skinner K, Raumann BE, Basbaum AI, Julius D. The cloned capsaicin receptor integrates multiple pain-producing stimuli. Neuron 1998; 21: 531-543.
-
(1998)
Neuron
, vol.21
, pp. 531-543
-
-
Tominaga, M.1
Caterina, M.J.2
Malmberg, A.B.3
Rosen, T.A.4
Gilbert, H.5
Skinner, K.6
Raumann, B.E.7
Basbaum, A.I.8
Julius, D.9
-
5
-
-
0033984992
-
The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1)
-
Smart D, Gunthorpe MJ, Jerman JC, Nasir S, Gray J, Muir AI, Chambers JK, Randall AD, Davis JB. The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1). Br J Pharmacol 2000; 129: 227-230.
-
(2000)
Br J Pharmacol
, vol.129
, pp. 227-230
-
-
Smart, D.1
Gunthorpe, M.J.2
Jerman, J.C.3
Nasir, S.4
Gray, J.5
Muir, A.I.6
Chambers, J.K.7
Randall, A.D.8
Davis, J.B.9
-
6
-
-
0037062411
-
An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors
-
Huang SM, Bisogno T, Trevisani M, Al-Hayani A, De Petrocellis L, Fezza F, Tognetto M, Petros TJ, Krey JF, Chu CJ, Miller JD, Davies SN, Geppetti P, Walker JM, Di Marzo V. An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors. Proc Natl Acad Sci U S A 2002; 99: 8400-8405.
-
(2002)
Proc Natl Acad Sci U S A
, vol.99
, pp. 8400-8405
-
-
Huang, S.M.1
Bisogno, T.2
Trevisani, M.3
Al-Hayani, A.4
De Petrocellis, L.5
Fezza, F.6
Tognetto, M.7
Petros, T.J.8
Krey, J.F.9
Chu, C.J.10
Miller, J.D.11
Davies, S.N.12
Geppetti, P.13
Walker, J.M.14
Di Marzo, V.15
-
7
-
-
0035927651
-
Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5)P2-mediated inhibition
-
Chuang H-H, Prescott ED, Kong H, Shields S, Jordt S-E, Basbaum AI, Chao MV, Julius D. 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
Shields, S.4
Jordt, S.-E.5
Basbaum, A.I.6
Chao, M.V.7
Julius, D.8
-
8
-
-
0034926291
-
The vanilloid receptor: a molecular gateway to the pain pathway
-
Caterina MJ, Julius D. The vanilloid receptor: a molecular gateway to the pain pathway. Annu Rev Neurosci 2001; 24: 487-517.
-
(2001)
Annu Rev Neurosci
, vol.24
, pp. 487-517
-
-
Caterina, M.J.1
Julius, D.2
-
9
-
-
0141738818
-
Vanilloid receptors take a TRP beyond the sensory afferent
-
Caterina MJ. Vanilloid receptors take a TRP beyond the sensory afferent. Pain 2003; 105: 5-9.
-
(2003)
Pain
, vol.105
, pp. 5-9
-
-
Caterina, M.J.1
-
11
-
-
34047118624
-
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation
-
Gavva NR, Bannon AW, Surapaneni S, Hovland DN Jr, Lehto SG, Gore A, Juan T, Deng H, Han B, Klionsky L, Kuang R, Le A, Tamir R, Wang J, Youngblood B, Zhu D, Norman MH, Magal E, Treanor JJ, Louis JC. The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J Neurosci 2007; 27: 3366-3374.
-
(2007)
J Neurosci
, vol.27
, pp. 3366-3374
-
-
Gavva, N.R.1
Bannon, A.W.2
Surapaneni, S.3
Hovland Jr., D.N.4
Lehto, S.G.5
Gore, A.6
Juan, T.7
Deng, H.8
Han, B.9
Klionsky, L.10
Kuang, R.11
Le, A.12
Tamir, R.13
Wang, J.14
Youngblood, B.15
Zhu, D.16
Norman, M.H.17
Magal, E.18
Treanor, J.J.19
Louis, J.C.20
more..
-
12
-
-
34447504896
-
Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors
-
Steiner AA, Turek VF, Almeida MC, Burmeister JJ, Oliveira DL, Roberts JL, Bannon AW, Norman MH, Louis JC, Treanor JJ, Gavva NR, Romanovsky AA. Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors. J Neurosci 2007; 27: 7459-7468.
-
(2007)
J Neurosci
, vol.27
, pp. 7459-7468
-
-
Steiner, A.A.1
Turek, V.F.2
Almeida, M.C.3
Burmeister, J.J.4
Oliveira, D.L.5
Roberts, J.L.6
Bannon, A.W.7
Norman, M.H.8
Louis, J.C.9
Treanor, J.J.10
Gavva, N.R.11
Romanovsky, A.A.12
-
13
-
-
11244351600
-
Lipopolysaccharide fever is initiated via a capsaicin-sensitive mechanism independent of the subtype-1 vanilloid receptor
-
Dogan MD, Patel S, Rudaya AY, Steiner AA, Szekely M, Romanovsky AA. Lipopolysaccharide fever is initiated via a capsaicin-sensitive mechanism independent of the subtype-1 vanilloid receptor. Br J Pharmacol 2004; 143: 1023-1032.
-
(2004)
Br J Pharmacol
, vol.143
, pp. 1023-1032
-
-
Dogan, M.D.1
Patel, S.2
Rudaya, A.Y.3
Steiner, A.A.4
Szekely, M.5
Romanovsky, A.A.6
-
14
-
-
33745212224
-
Cold-seeking behavior as a thermoregulatory strategy in systemic inflammation
-
Almeida MC, Steiner AA, Branco LG, Romanovsky AA. Cold-seeking behavior as a thermoregulatory strategy in systemic inflammation. Eur J Neurosci 2006; 23: 3359-3367.
-
(2006)
Eur J Neurosci
, vol.23
, pp. 3359-3367
-
-
Almeida, M.C.1
Steiner, A.A.2
Branco, L.G.3
Romanovsky, A.A.4
-
15
-
-
0021737076
-
Capsaicin and central control of thermoregulation
-
Hori T. Capsaicin and central control of thermoregulation. Pharmacol Ther 1984; 26: 389-416.
-
(1984)
Pharmacol Ther
, vol.26
, pp. 389-416
-
-
Hori, T.1
-
16
-
-
0034646740
-
Impaired nociception and pain sensation in mice lacking the capsaicin receptor
-
Caterina MJ, Leffler A, Malmberg AB, Martin WJ, Trafton J, Petersen-Zeitz KR, Koltzenburg M, Basbaum AI, Julius D. Impaired nociception and pain sensation in mice lacking the capsaicin receptor. Science 2000; 288: 306-313.
-
(2000)
Science
, vol.288
, pp. 306-313
-
-
Caterina, M.J.1
Leffler, A.2
Malmberg, A.B.3
Martin, W.J.4
Trafton, J.5
Petersen-Zeitz, K.R.6
Koltzenburg, M.7
Basbaum, A.I.8
Julius, D.9
-
17
-
-
20144376596
-
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
-
Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI. 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: 1857-1872.
-
(2005)
J Med Chem
, vol.48
, pp. 1857-1872
-
-
Swanson, D.M.1
Dubin, A.E.2
Shah, C.3
Nasser, N.4
Chang, L.5
Dax, S.L.6
Jetter, M.7
Breitenbucher, J.G.8
Liu, C.9
Mazur, C.10
Lord, B.11
Gonzales, L.12
Hoey, K.13
Rizzolio, M.14
Bogenstaetter, M.15
Codd, E.E.16
Lee, D.H.17
Zhang, S.P.18
Chaplan, S.R.19
Carruthers, N.I.20
more..
-
18
-
-
60049089359
-
Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia
-
Honore P, Chandran P, Hernandez G, Gauvin DM, Mikusa JP, Zhong C, Joshi SK, Ghilardi JR, Sevcik MA, Fryer RM, Segreti JA, Banfor PN, Marsh K, Neelands T, Bayburt E, Daanen JF, Gomtsyan A, Lee CH, Kort ME, Reilly RM, Surowy CS, Kym PR, Mantyh PW, Sullivan JP, Jarvis MF, Faltynek CR. Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia. Pain 2009; 142: 27-35.
-
(2009)
Pain
, vol.142
, pp. 27-35
-
-
Honore, P.1
Chandran, P.2
Hernandez, G.3
Gauvin, D.M.4
Mikusa, J.P.5
Zhong, C.6
Joshi, S.K.7
Ghilardi, J.R.8
Sevcik, M.A.9
Fryer, R.M.10
Segreti, J.A.11
Banfor, P.N.12
Marsh, K.13
Neelands, T.14
Bayburt, E.15
Daanen, J.F.16
Gomtsyan, A.17
Lee, C.H.18
Kort, M.E.19
Reilly, R.M.20
Surowy, C.S.21
Kym, P.R.22
Mantyh, P.W.23
Sullivan, J.P.24
Jarvis, M.F.25
Faltynek, C.R.26
more..
-
19
-
-
34548825160
-
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade
-
Gavva NR, Bannon AW, Hovland DN Jr, Lehto SG, Klionsky L, Surapaneni S, Immke DC, 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 MH, Louis JC, Magal E, Treanor JJ. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther 2007; 323: 128-137.
-
(2007)
J Pharmacol Exp Ther
, vol.323
, pp. 128-137
-
-
Gavva, N.R.1
Bannon, A.W.2
Hovland Jr., D.N.3
Lehto, S.G.4
Klionsky, L.5
Surapaneni, S.6
Immke, D.C.7
Henley, C.8
Arik, L.9
Bak, A.10
Davis, J.11
Ernst, N.12
Hever, G.13
Kuang, R.14
Shi, L.15
Tamir, R.16
Wang, J.17
Wang, W.18
Zajic, G.19
Zhu, D.20
Norman, M.H.21
Louis, J.C.22
Magal, E.23
Treanor, J.J.24
more..
-
20
-
-
58149107126
-
Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway
-
Gunthorpe MJ, Chizh BA. Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway. Drug Discov Today 2009; 14: 56-67.
-
(2009)
Drug Discov Today
, vol.14
, pp. 56-67
-
-
Gunthorpe, M.J.1
Chizh, B.A.2
-
21
-
-
79954617292
-
Randomised clinical trial: the efficacy of a transient receptor potential vanilloid 1 antagonist AZD1386 in human oesophageal pain
-
Krarup AL, Ny L, Astrand M, Bajor A, Hvid-Jensen F, Hansen MB, Simren M, Funch-Jensen P, Drewes AM. Randomised clinical trial: the efficacy of a transient receptor potential vanilloid 1 antagonist AZD1386 in human oesophageal pain. Aliment Pharmacol Ther 2011; 33: 1113-1122.
-
(2011)
Aliment Pharmacol Ther
, vol.33
, pp. 1113-1122
-
-
Krarup, A.L.1
Ny, L.2
Astrand, M.3
Bajor, A.4
Hvid-Jensen, F.5
Hansen, M.B.6
Simren, M.7
Funch-Jensen, P.8
Drewes, A.M.9
-
22
-
-
41749117999
-
Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans
-
Gavva NR, Treanor JJ, Garami A, Fang L, Surapaneni S, Akrami A, Alvarez F, Bak A, Darling M, Gore A, Jang GR, Kesslak JP, Ni L, Norman MH, Palluconi G, Rose MJ, Salfi M, Tan E, Romanovsky AA, Banfield C, Davar G. 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.2
Garami, A.3
Fang, L.4
Surapaneni, S.5
Akrami, A.6
Alvarez, F.7
Bak, A.8
Darling, M.9
Gore, A.10
Jang, G.R.11
Kesslak, J.P.12
Ni, L.13
Norman, M.H.14
Palluconi, G.15
Rose, M.J.16
Salfi, M.17
Tan, E.18
Romanovsky, A.A.19
Banfield, C.20
Davar, G.21
more..
-
23
-
-
53849138741
-
(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, McGaraughty S, El Kouhen R, Han P, Chu KL, McDonald HA, Vos M, Niforatos W, Bayburt EK, Gomtsyan A, Lee CH, Honore P, Sullivan JP, Jarvis MF, Faltynek CR. (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
McGaraughty, S.4
El Kouhen, R.5
Han, P.6
Chu, K.L.7
McDonald, H.A.8
Vos, M.9
Niforatos, W.10
Bayburt, E.K.11
Gomtsyan, A.12
Lee, C.H.13
Honore, P.14
Sullivan, J.P.15
Jarvis, M.F.16
Faltynek, C.R.17
-
24
-
-
39149117718
-
Identification of (R)-1-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
-
Gomtsyan A, Bayburt EK, Schmidt RG, Surowy CS, Honore P, Marsh KC, Hannick SM, McDonald HA, Wetter JM, Sullivan JP, Jarvis MF, Faltynek CR, Lee C-H. Identification of (R)-1-(5-tert-Butyl-2, 3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management. J Med Chem 2008; 51: 392-395.
-
(2008)
J Med Chem
, vol.51
, pp. 392-395
-
-
Gomtsyan, A.1
Bayburt, E.K.2
Schmidt, R.G.3
Surowy, C.S.4
Honore, P.5
Marsh, K.C.6
Hannick, S.M.7
McDonald, H.A.8
Wetter, J.M.9
Sullivan, J.P.10
Jarvis, M.F.11
Faltynek, C.R.12
Lee, C.-H.13
-
25
-
-
84863187892
-
Pharmacokinetics of the TRPV1 antagonist ABT-102 in healthy human volunteers: population analysis of data from 3 phase 1 trials
-
Othman AA, Nothaft W, Awni WM, Dutta S. Pharmacokinetics of the TRPV1 antagonist ABT-102 in healthy human volunteers: population analysis of data from 3 phase 1 trials. J Clin Pharmacol 2012; 52: 1028-1041.
-
(2012)
J Clin Pharmacol
, vol.52
, pp. 1028-1041
-
-
Othman, A.A.1
Nothaft, W.2
Awni, W.M.3
Dutta, S.4
-
26
-
-
79954584227
-
Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial
-
Rowbotham MC, Nothaft W, Duan WR, Wang Y, Faltynek C, McGaraughty S, Chu KL, Svensson P. Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial. Pain 2011; 152: 1192-1200.
-
(2011)
Pain
, vol.152
, pp. 1192-1200
-
-
Rowbotham, M.C.1
Nothaft, W.2
Duan, W.R.3
Wang, Y.4
Faltynek, C.5
McGaraughty, S.6
Chu, K.L.7
Svensson, P.8
-
28
-
-
0003747347
-
-
Part V. San Francisco, CA: Division of Clinical Pharmacology, University of California
-
Beal SL, Sheiner LB. NONMEM Users Guide, Part V. San Francisco, CA: Division of Clinical Pharmacology, University of California, 1979-1992.
-
(1979)
NONMEM Users Guide
-
-
Beal, S.L.1
Sheiner, L.B.2
-
30
-
-
35848952270
-
Conditional weighted residuals (CWRES): a model diagnostic for the FOCE method
-
Hooker AC, Staatz CE, Karlsson MO. Conditional weighted residuals (CWRES): a model diagnostic for the FOCE method. Pharm Res 2007; 24: 2187-2197.
-
(2007)
Pharm Res
, vol.24
, pp. 2187-2197
-
-
Hooker, A.C.1
Staatz, C.E.2
Karlsson, M.O.3
-
31
-
-
84872249123
-
An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin
-
Accepted Article doi: 10.1111/j.1365-2125.2012.04377.x, Epub: 2012 Jul 10.
-
Schaffler K, Reeh P, Duan WR, Best AE, Othman AA, Faltynek CR, Locke C, Nothaft W. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin. Br J Clin Pharmacol. Accepted Article doi: 10.1111/j.1365-2125.2012.04377.x, Epub: 2012 Jul 10.
-
Br J Clin Pharmacol
-
-
Schaffler, K.1
Reeh, P.2
Duan, W.R.3
Best, A.E.4
Othman, A.A.5
Faltynek, C.R.6
Locke, C.7
Nothaft, W.8
-
33
-
-
0029415374
-
A pharmacokinetic-pharmacodynamic model of tolerance to morphine analgesia during infusion in rats
-
Ouellet DM, Pollack GM. A pharmacokinetic-pharmacodynamic model of tolerance to morphine analgesia during infusion in rats. J Pharmacokinet Biopharm 1995; 23: 531-549.
-
(1995)
J Pharmacokinet Biopharm
, vol.23
, pp. 531-549
-
-
Ouellet, D.M.1
Pollack, G.M.2
-
34
-
-
0027732751
-
Quantification of effect delay and acute tolerance development to morphine in the rat
-
Gardmark M, Ekblom M, Bouw R, Hammarlund-Udenaes M. Quantification of effect delay and acute tolerance development to morphine in the rat. J Pharmacol Exp Ther 1993; 267: 1061-1067.
-
(1993)
J Pharmacol Exp Ther
, vol.267
, pp. 1061-1067
-
-
Gardmark, M.1
Ekblom, M.2
Bouw, R.3
Hammarlund-Udenaes, M.4
|