![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
Vol. 304, Issue 1, 56-62, January 2003
Novartis Institute for Medical Sciences, London, United Kingdom
Vanilloid receptor type 1 (VR1) (TRPV1) is a ligand-gated ion channel
expressed on sensory nerves that responds to noxious heat, protons, and
chemical stimuli such as capsaicin. Herein, we have examined the
activity of the VR1 antagonist capsazepine in models of inflammatory
and neuropathic pain in the rat, mouse, and guinea pig. In
naïve animals, subcutaneous administration of capsazepine
(10-100 mg/kg s.c.) did not affect withdrawal thresholds to noxious
thermal or mechanical stimuli. However, pretreatment with capsazepine
prevented the development of mechanical hyperalgesia induced by
intraplantar injection of capsaicin, with a similar potency in all
three species. Capsazepine (up to 100 mg/kg s.c.) did not affect
mechanical hyperalgesia in the Freund's complete adjuvant
(FCA)-inflamed hind paw of the rat or mouse. Strikingly, capsazepine
(3-30 mg/kg s.c.) produced up to 44% reversal of FCA-induced mechanical hyperalgesia in the guinea pig. Capsazepine also produced significant reversal of carageenan-induced thermal hyperalgesia in the
guinea pig at 30 mg/kg s.c., but was ineffective in the rat. Similarly,
in the partial sciatic nerve ligation model of neuropathic pain,
capsazepine was surprisingly effective in the guinea pig, producing up
to 80% reversal of mechanical hyperalgesia (1-30 mg/kg s.c.) but had
no effect in the rat or mouse. These data show that VR1 antagonists
have antihyperalgesic activity in animal models of chronic inflammatory
and neuropathic pain, and illustrate species differences in the in vivo
pharmacology of VR1 that correlate with differences in pharmacology
previously seen in vitro.
This article has been cited by other articles:
|
|
 |
|
  J. Vriens, G. Appendino, and B. Nilius Pharmacology of Vanilloid Transient Receptor Potential Cation Channels Mol. Pharmacol., June 1, 2009; 75(6): 1262 - 1279. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Ohta, T. Imagawa, and S. Ito Involvement of Transient Receptor Potential Vanilloid Subtype 1 in Analgesic Action of Methylsalicylate Mol. Pharmacol., February 1, 2009; 75(2): 307 - 317. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H.-Y. Zhou, S.-R. Chen, H. Chen, and H.-L. Pan Sustained Inhibition of Neurotransmitter Release from Nontransient Receptor Potential Vanilloid Type 1-Expressing Primary Afferents by {micro}-Opioid Receptor Activation-Enkephalin in the Spinal Cord J. Pharmacol. Exp. Ther., November 1, 2008; 327(2): 375 - 382. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 I. Vetter, W. Cheng, M. Peiris, B. D. Wyse, S. J. Roberts-Thomson, J. Zheng, G. R. Monteith, and P. J. Cabot Rapid, Opioid-sensitive Mechanisms Involved in Transient Receptor Potential Vanilloid 1 Sensitization J. Biol. Chem., July 11, 2008; 283(28): 19540 - 19550. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. G. Lehto, R. Tamir, H. Deng, L. Klionsky, R. Kuang, A. Le, D. Lee, J.-C. Louis, E. Magal, B. H. Manning, et al. 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., July 1, 2008; 326(1): 218 - 229. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Ohta, T. Imagawa, and S. Ito 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., April 4, 2008; 283(14): 9377 - 9387. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H. U. De Schepper, J. G. De Man, N. E. Ruyssers, A. Deiteren, L. Van Nassauw, J.-P. Timmermans, W. Martinet, A. G. Herman, P. A. Pelckmans, and B. Y. De Winter TRPV1 receptor signaling mediates afferent nerve sensitization during colitis-induced motility disorders in rats Am J Physiol Gastrointest Liver Physiol, January 1, 2008; 294(1): G245 - G253. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Bhattacharya, B. P. Scott, N. Nasser, H. Ao, M. P. Maher, A. E. Dubin, D. M. Swanson, N. P. Shankley, A. D. Wickenden, and S. R. Chaplan Pharmacology and Antitussive Efficacy of 4-(3-Trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic Acid (5-Trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a Transient Receptor Potential Vanilloid 1 Antagonist in Guinea Pigs J. Pharmacol. Exp. Ther., November 1, 2007; 323(2): 665 - 674. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
N. R. Gavva, A. W. Bannon, D. N. Hovland Jr., S. G. Lehto, L. Klionsky, S. Surapaneni, D. C. Immke, C. Henley, L. Arik, A. Bak, et al. Repeated Administration of Vanilloid Receptor TRPV1 Antagonists Attenuates Hyperthermia Elicited by TRPV1 Blockade J. Pharmacol. Exp. Ther., October 1, 2007; 323(1): 128 - 137. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. J. Gunthorpe, S. L. Hannan, D. Smart, J. C. Jerman, S. Arpino, G. D. Smith, S. Brough, J. Wright, J. Egerton, S. C. Lappin, et al. 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., June 1, 2007; 321(3): 1183 - 1192. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. A. Retamal, K. A. Schalper, K. F. Shoji, M. V. L. Bennett, and J. C. Saez Opening of connexin 43 hemichannels is increased by lowering intracellular redox potential PNAS, May 15, 2007; 104(20): 8322 - 8327. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
L. Tang, Y. Chen, Z. Chen, P. M. Blumberg, A. P. Kozikowski, and Z. J. Wang 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., May 1, 2007; 321(2): 791 - 798. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. Kiselyov, A. Soyombo, and S. Muallem TRPpathies J. Physiol., February 1, 2007; 578(3): 641 - 653. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Cui, P. Honore, C. Zhong, D. Gauvin, J. Mikusa, G. Hernandez, P. Chandran, A. Gomtsyan, B. Brown, E. K. Bayburt, et al. TRPV1 Receptors in the CNS Play a Key Role in Broad-Spectrum Analgesia of TRPV1 Antagonists. J. Neurosci., September 13, 2006; 26(37): 9385 - 9393. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. M. Patwardhan, N. A. Jeske, T. J. Price, N. Gamper, A. N. Akopian, and K. M. Hargreaves The cannabinoid WIN 55,212-2 inhibits transient receptor potential vanilloid 1 (TRPV1) and evokes peripheral antihyperalgesia via calcineurin PNAS, July 25, 2006; 103(30): 11393 - 11398. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. Balonov, A. Khodorova, and G. R. Strichartz Tactile Allodynia Initiated by Local Subcutaneous Endothelin-1 Is Prolonged by Activation of TRPV-1 Receptors. Experimental Biology and Medicine, June 1, 2006; 231(6): 1165 - 1170. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
V. Vellani, M. Colucci, R. Lattanzi, E. Giannini, L. Negri, P. Melchiorri, and P. A. McNaughton Sensitization of transient receptor potential vanilloid 1 by the prokineticin receptor agonist Bv8. J. Neurosci., May 10, 2006; 26(19): 5109 - 5116. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. C. Wick, S. G. Hoge, S. W. Grahn, E. Kim, L. A. Divino, E. F. Grady, N. W. Bunnett, and K. S. Kirkwood Transient receptor potential vanilloid 1, calcitonin gene-related peptide, and substance P mediate nociception in acute pancreatitis Am J Physiol Gastrointest Liver Physiol, May 1, 2006; 290(5): G959 - G969. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
N. R. Gavva, R. Tamir, L. Klionsky, M. H. Norman, J.-C. Louis, K. D. Wild, and J. J. S. Treanor Proton Activation Does Not Alter Antagonist Interaction with the Capsaicin-Binding Pocket of TRPV1 Mol. Pharmacol., December 1, 2005; 68(6): 1524 - 1533. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
P. Honore, C. T. Wismer, J. Mikusa, C. Z. Zhu, C. Zhong, D. M. Gauvin, A. Gomtsyan, R. El Kouhen, C.-H. Lee, K. Marsh, et al. 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., July 1, 2005; 314(1): 410 - 421. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. Radhakrishnan and K. A. Sluka Acetazolamide, a Carbonic Anhydrase Inhibitor, Reverses Inflammation-Induced Thermal Hyperalgesia in Rats J. Pharmacol. Exp. Ther., May 1, 2005; 313(2): 921 - 927. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
N. R. Gavva, R. Tamir, Y. Qu, L. Klionsky, T. J. Zhang, D. Immke, J. Wang, D. Zhu, T. W. Vanderah, F. Porreca, 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., April 1, 2005; 313(1): 474 - 484. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
G. Appendino, L. De Petrocellis, M. Trevisani, A. Minassi, N. Daddario, A. S. Moriello, D. Gazzieri, A. Ligresti, B. Campi, G. Fontana, et al. Development of the First Ultra-Potent "Capsaicinoid" Agonist at Transient Receptor Potential Vanilloid Type 1 (TRPV1) Channels and Its Therapeutic Potential J. Pharmacol. Exp. Ther., February 1, 2005; 312(2): 561 - 570. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. Hong and J. W. Wiley Early Painful Diabetic Neuropathy Is Associated with Differential Changes in the Expression and Function of Vanilloid Receptor 1 J. Biol. Chem., January 7, 2005; 280(1): 618 - 627. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
W. Rong, K. Hillsley, J. B Davis, G. Hicks, W. J Winchester, and D. Grundy Jejunal afferent nerve sensitivity in wild-type and TRPV1 knockout mice J. Physiol., November 1, 2004; 560(3): 867 - 881. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. R. Butelman, T. J. Harris, and M. J. Kreek Antiallodynic Effects of Loperamide and Fentanyl against Topical Capsaicin-Induced Allodynia in Unanesthetized Primates J. Pharmacol. Exp. Ther., October 1, 2004; 311(1): 155 - 163. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R.-R. Ji and G. Strichartz Cell Signaling and the Genesis of Neuropathic Pain Sci. Signal., September 28, 2004; 2004(252): re14 - re14. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. Phillips, A. Reeve, S. Bevan, and P. McIntyre Identification of Species-specific Determinants of the Action of the Antagonist Capsazepine and the Agonist PPAHV on TRPV1 J. Biol. Chem., April 23, 2004; 279(17): 17165 - 17172. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Toth, P. M. Blumberg, Z. Chen, and A. P. Kozikowski Design of a High-Affinity Competitive Antagonist of the Vanilloid Receptor Selective for the Calcium Entry-Linked Receptor Population Mol. Pharmacol., February 1, 2004; 65(2): 282 - 291. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. D. Pomonis, J. E. Harrison, L. Mark, D. R. Bristol, K. J. Valenzano, and K. Walker 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., July 1, 2003; 306(1): 387 - 393. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
K. J. Valenzano, E. R. Grant, G. Wu, M. Hachicha, L. Schmid, L. Tafesse, Q. Sun, Y. Rotshteyn, J. Francis, J. Limberis, 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., July 1, 2003; 306(1): 377 - 386. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
