Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature

Journal of Pharmacology and Experimental Therapeutics

Volumn 342, Issue 2, 2012, Pages 416-428

  Reilly, Regina M ^a   McDonald, Heath A ^a   Puttfarcken, Pamela S ^a   Joshi, Shailen K ^a   Lewis, LaGeisha ^a   Pai, Madhavi ^a   Franklin, Pamela H ^a   Segreti, Jason A ^a   Neelands, Torben R ^a   Han, Ping ^a   Chen, Jun ^a   Mantyh, Patrick W ^b   Ghilardi, Joseph R ^c   Turner, Teresa M ^a   Voight, Eric A ^a   Daanen, Jerome F ^a   Schmidt, Robert G ^a   Gomtsyan, Arthur ^a   Kort, Michael E ^a   Faltynek, Connie R ^a   Kym, Philip R ^a   more..

^a ABBOTT LABORATORIES   (United States)

^b UNIVERSITY OF ARIZONA COLLEGE OF MEDICINE   (United States)

^c VA MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(5 TERT BUTYL 2,3 DIHYDRO 1H INDEN 1 YL) 3 (1H INDAZOL 4 YL)UREA; A 1106625; A 1165422; A 1165442; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 1 ANTAGONIST;

ANALGESIC ACTIVITY; ANIMAL CELL; ARTICLE; CALCIUM TRANSPORT; CANCER PAIN; CONCENTRATION RESPONSE; CONTROLLED STUDY; CORE TEMPERATURE; DRUG BINDING SITE; DRUG EFFICACY; DRUG MECHANISM; DRUG SAFETY; DRUG TREATMENT FAILURE; HUMAN; HUMAN CELL; IC 50; MALE; NERVE CELL; NONHUMAN; OSTEOARTHRITIS; PHARMACOLOGICAL BLOCKING; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; STRUCTURE ACTIVITY RELATION; THERMOREGULATION; TREATMENT RESPONSE;

ANALGESICS; ANIMALS; BODY TEMPERATURE; CALCITONIN GENE-RELATED PEPTIDE; CALCIUM; CAPSAICIN; CELL LINE, TRANSFORMED; FEVER; HEK293 CELLS; HUMANS; MALE; MICE; MICE, INBRED C3H; NEURONS; PAIN; PROTONS; RATS; RATS, SPRAGUE-DAWLEY; RECOMBINANT PROTEINS; TRPV CATION CHANNELS;

EID: 84864147863     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.111.190314     Document Type: Article

References (45)

1. Ayoub SS, Hunter JC, and Simmons DL (2009) Answering the burning question of how transient receptor potential vanilloid-1 channel antagonists cause unwanted hyperthermia. Pharmacol Rev 61:225-227.
2. Bevan S and Geppetti P (1994) Protons: small stimulants of capsaicin-sensitive sensory nerves. Trends Neurosci 17:509-512. (Pubitemid 24347911)
3. Caterina MJ, Leffler A, Malmberg AB, Martin WJ, Trafton J, Petersen-Zeitz KR, Koltzenburg M, Basbaum AI, and Julius D (2000) Impaired nociception and pain sensation in mice lacking the capsaicin receptor. Science 288:306-313. (Pubitemid 30226186)
4. Caterina MJ, Schumacher MA, Tominaga M, Rosen TA, Levine JD, and Julius D (1997) The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature 389:816-824. (Pubitemid 27462969)
5. Chandran P, Pai M, Blomme EA, Hsieh GC, Decker MW, and Honore P (2009) Pharmacological modulation of movement-evoked pain in a rat model of osteoarthritis. Eur J Pharmacol 613:39-45.
6. Cui M, Honore P, Zhong C, Gauvin D, Mikusa J, Hernandez G, Chandran P, Gomtsyan A, Brown B, Bayburt EK, et al. (2006) TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J Neurosci 26:9385-9393. (Pubitemid 44396851)
7. Dray A and Read SJ (2007) Arthritis and pain. Future targets to control osteoarthritis pain. Arthritis Res Ther 9:212-225.
8. Earley S and Brayden JE (2010) Transient receptor potential channels and vascular function. Clin Sci 119:19-36.
9. 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. (Pubitemid 41058278)
10. Garami A, Pakai E, Oliveira DL, Steiner AA, Wanner SP, Almeida MC, Lesnikov VA, Gavva NR, and Romanovsky AA (2011) Thermoregulatory phenotype of the Trpv1 knockout mouse: thermoeffector dysbalance with hyperkinesis. J Neurosci 31:1721-1733.
11. Garami A, Shimansky YP, Pakai E, Oliveira DL, Gavva NR, and Romanovsky AA (2010) Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia. J Neurosci 30:1435-1440.
12. Gavva NR (2008) Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1. Trends Pharmacol Sci 29:550-557.
13. Gavva NR, Klionsky L, Qu Y, Shi L, Tamir R, Edenson S, Zhang TJ, Viswanadhan VN, Toth A, Pearce LV, et al. (2004) Molecular determinants of vanilloid sensitivity in TRPV1. J Biol Chem 279:20283-20295. (Pubitemid 38623474)
14. Gavva NR, Tamir R, Klionsky L, Norman MH, Louis JC, Wild KD, and Treanor JJ (2005) Proton activation does not alter antagonist interaction with the capsaicinbinding pocket of TRPV1. Mol Pharmacol 68:1524-1533. (Pubitemid 41654336)
15. Gavva NR, Treanor JJ, Garami A, Fang L, Surapaneni S, Akrami A, Alvarez F, Bak A, Darling M, Gore A, et al. (2008) Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. Pain 136:202-210.
16. Ghilardi JR, Freeman KT, Jimenez-Andrade JM, Coughlin K, Kaczmarska MJ, Castaneda-Corral G, Bloom AP, Kuskowski MA, and Mantyh PW (2012) Neuroplasticity of sensory and sympathetic nerve fibers in the painful arthritic joint. Arthritis Rheum http://dx.doi.org/10.1002/art.34385.
17. Gomtsyan A (2010) Aryl-urea class and related TRPV1 antagonists, in Vanilloid Receptor TRPV1 in Drug Discovery. Targeting Pain and Other Pathological Disorders (Gomtsyan A and Faltynek CR eds), pp 295-310, John Wiley & Sons, Hoboken, NJ.
18. Honore P, Chandran P, Hernandez G, Gauvin DM, Mikusa JP, Zhong C, Joshi SK, Ghilardi JR, Sevcik MA, Fryer RM, et al. (2009) Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia. Pain 142:27-35.
19. Honore P, Wismer CT, Mikusa J, Zhu CZ, Zhong C, Gauvin DM, Gomtsyan A, El Kouhen R, Lee CH, Marsh K, et al. (2005) A-425619 [1-isoquinolin-5-yl-3-(4- trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats. J Pharmacol Exp Ther 314:410-421. (Pubitemid 41058279)
20. Huang SM, Bisogno T, Trevisani M, Al-Hayani A, De Petrocellis L, Fezza F, Tognetto M, Petros TJ, Krey JF, Chu CJ, et al. (2002) An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors. Proc Natl Acad Sci U S A 99:8400-8405. (Pubitemid 34651064)
21. Institute of Laboratory Animal Resources (2011) Guide for the Care and Use of Laboratory Animals, Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington, DC.
22. Jancsó-Gábor A, Szolcsányi J, and Jancsó N (1970) Irreversible impairment of thermoregulation induced by capsaicin and similar pungent substances in rats and guinea-pigs. J Physiol 206:495-507.
23. Jara-Oseguera A, Simon SA, and Rosenbaum T (2008) TRPV1: on the road to pain relief. Curr Mol Pharmacol 1:255-269.
24. Johnson JM and Kellogg DL (2010) Thermoregulatory and thermal control in the human cutaneous circulation. Front Biosci (Schol Ed) 2:825-853.
25. Jordt SE and Julius D (2002) Molecular basis for species-specific sensitivity to "hot"chili peppers. Cell 108:421-430.
26. 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. (Pubitemid 30460785)
27. Kawasaki H, Eguchi S, Miyashita S, Chan S, Hirai K, Hobara N, Yokomizo A, Fujiwara H, Zamami Y, Koyama T, et al. (2009) Proton acts as a neurotransmitter for nicotine-induced adrenergic and calcitonin gene-related peptide-containing nerve-mediated vasodilation in the rat mesenteric artery. J Pharmacol Exp Ther 330:745-755.
28. Lehto SG, Tamir R, Deng H, Klionsky L, Kuang R, Le A, Lee D, Louis JC, Magal E, Manning BH, et al. (2008) Antihyperalgesic effects of (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl) -4-(trifluoromethyl)phenyl)-acrylamide (AMG8562), a novel transient receptor potential vanilloid type 1 modulator that does not cause hyperthermia in rats. J Pharmacol Exp Ther 326:218-229. (Pubitemid 351872146)
29. Mantyh PW (2006) Cancer pain and its impact on diagnosis, survival and quality of life. Nat Rev Neurosci 7:797-809.
30. McDonald HA, Neelands TR, Kort M, Han P, Vos MH, Faltynek CR, Moreland RB, and Puttfarcken PS (2008) Characterization of A-425619 at native TRPV1 receptors: a comparison between dorsal root ganglia and trigeminal ganglia. Eur J Pharmacol 596:62-69.
31. McIntyre P, McLatchie LM, Chambers A, Phillips E, Clarke M, Savidge J, Toms C, Peacock M, Shah K, Winter J, et al. (2001) Pharmacological differences between the human and rat vanilloid receptor 1 (VR1). Br J Pharmacol 132:1084-1094. (Pubitemid 32238914)
32. Neelands TR, Zhang XF, McDonald H, and Puttfarcken P (2010) Differential effects of temperature on acid-activated currents mediated by TRPV1 and ASIC channels in rat dorsal root ganglion neurons. Brain Res 1329:55-66.
33. Pomonis JD, Boulet JM, Gottshall SL, Phillips S, Sellers R, Bunton T, and Walker K (2005) Development and pharmacological characterization of a rat model of osteoarthritis pain. Pain 114:339-346. (Pubitemid 40385873)
34. Rades D, Schild SE, and Abrahm JL (2010) Treatment of painful bone metastases. Nat Rev Clin Oncol 7:220-229.
35. Rowbotham MC, Nothaft W, Duan WR, Wang Y, Faltynek C, McGaraughty S, Chu KL, and Svensson P (2011) Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial. Pain 152:1192-1200.
36. Schwei MJ, Honore P, Rogers SD, Salak-Johnson JL, Finke MP, Ramnaraine ML, Clohisy DR, and Mantyh PW (1999) Neurochemical and cellular reorganization of the spinal cord in a murine model of bone cancer pain. J Neurosci 19:10886-10897. (Pubitemid 30235733)
37. Sevcik MA, Ghilardi JR, Peters CM, Lindsay TH, Halvorson KG, Jonas BM, Kubota K, Kuskowski MA, Boustany L, Shelton DL, et al. (2005) Anti-NGF therapy profoundly reduces bone cancer pain and the accompanying increase in markers of peripheral and central sensitization. Pain 115:128-141.
38. Shimizu I, Iida T, Horiuchi N, and Caterina MJ (2005) 5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro. J Pharmacol Exp Ther 314:1378-1385. (Pubitemid 41206005)
39. Steiner AA, Turek VF, Almeida MC, Burmeister JJ, Oliveira DL, Roberts JL, Bannon AW, Norman MH, Louis JC, Treanor JJ, et al. (2007) Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors. J Neurosci 27:7459-7468. (Pubitemid 47066573)
40. Surowy CS, Neelands TR, Bianchi BR, McGaraughty S, El Kouhen R, Han P, Chu KL, McDonald HA, Vos M, Niforatos W, et al. (2008) (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 326:879-888.
41. Traynelis SF and Chesler M (2001) Proton release as a modulator of presynaptic function. Neuron 32:960-962. (Pubitemid 34075385)
42. Watabiki T, Kiso T, Kuramochi T, Yonezawa K, Tsuji N, Kohara A, Kakimoto S, Aoki T, and Matsuoka N (2011) Amelioration of neuropathic pain by novel transient receptor potential vanilloid 1 antagonist AS1928370 in rats without hyperthermic effect. J Pharmacol Exp Ther 336:743-750.
43. Witte DG, Cassar SC, Masters JN, Esbenshade T, and Hancock AA (2002) Use of a fluorescent imaging plate reader-based calcium assay to assess pharmacological differences between the human and rat vanilloid receptor. J Biomol Screen 7:466-475. (Pubitemid 135752863)
44. Zha XM, Wemmie JA, Green SH, and Welsh MJ (2006) Acid-sensing ion channel 1a is a postsynaptic proton receptor that affects the density of dendritic spines. Proc Natl Acad Sci U S A 103:16556-16561. (Pubitemid 44715234)
45. Zygmunt PM, Petersson J, Andersson DA, Chuang H, Sørgård M, Di Marzo V, Julius D, and Högestätt ED (1999) Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide. Nature 400:452-457. (Pubitemid 29361798)