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Chemical Compound Review

capsazepin     N-[2-(4-chlorophenyl)ethyl]- 9,10-dihydroxy...

Synonyms: capsazepine, Lopac-C-191, Tocris-0464, CHEMBL391997, C191_SIGMA, ...
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Disease relevance of Lopac-C-191

  • Further examinations revealed that TRPV1-induced toxicity was accompanied by increases in intracellular Ca(2+), and mitochondrial damage; these effects were inhibited by capsazepine, I-RTX, and the intracellular Ca(2+) chelator BAPTA-AM [1].
  • Vasorelaxation by abn-cbd is endothelium-dependent, pertussis toxin-sensitive, and is inhibited by the BK(Ca) channel inhibitor charybdotoxin, but not by the nitric-oxide synthase inhibitor N(omega)-nitro-L-arginine methyl ester or by the vanilloid VR1 receptor antagonist capsazepine [2].
  • Intraperitoneal administration of the competitive TRPV1 antagonist capsazepine inhibited hyperalgesia induced by tumor cell-inoculation in either plantar- or thigh-inoculated animals [3].
  • AT-induced effects including reduction of hypotension (n = 5) and inhibition of induction of iNOS (n = 4 or 5) and TNF- alpha (n = 5) in the lungs of endotoxin-treated animals were completely reversed by pretreatment with capsazepine (CPZ) (n = 4 or 5), a vanilloid receptor antagonist, or CGRP(8-37), a CGRP receptor antagonist (n = 4 or 5) [4].
  • CONCLUSIONS: In the isolated guinea pig heart, moderate acidosis is associated with CGRP release dependent on influx of extracellular Ca2+ and formation of PGI2, with subsequent stimulation of capsazepine sensitive receptors [5].

Psychiatry related information on Lopac-C-191


High impact information on Lopac-C-191


Chemical compound and disease context of Lopac-C-191


Biological context of Lopac-C-191


Anatomical context of Lopac-C-191

  • In sensory neurons, OEA-induced Ca2+ rises that were selective for capsaicin-sensitive cells, inhibited by the TRPV1 blocker, capsazepine, and occurred in a PKC-dependent manner [21].
  • The inward currents at a holding potential of -60 mV in hENaCdeltabetagamma-expressing oocytes were markedly enhanced by the application of capsazepine (> or =1 microM), and the capsazepine-induced current was mostly abolished by the addition of 100 microM amiloride [22].
  • Furthermore, activation of TRPV1 receptors seems to play a role of stabilization of the plasma membranes in capacitated sperm, as demonstrated by the high incidence of spontaneous AR occurring during the cultural period when TRPV1 activity was antagonized by capsazepine [23].
  • The competitive vanilloid receptor antagonist capsazepine inhibited [(3)H]RTX binding to HEK293/VR1 cells with a K(i) value of 6.2 microM and binding to DRG membranes with a K(i) value of 8.6 microM [24].
  • Finally, JYL1421 and KJM429 had little or no effect on ATP-induced calcium uptake in CHO cells lacking rVR1, unlike capsazepine [25].

Associations of Lopac-C-191 with other chemical compounds

  • A subset of animals were administered the VR-1 antagonist capsazepine, famotidine, or omeprazole one hour before surgery [26].
  • CT responses were recorded in the presence of Bz (a specific blocker of the epithelial Na(+) channel [ENaC]) or the vanilloid receptor-1 (VR-1) antagonists capsazepine or SB-366791, which also block the Bz-insensitive salt taste receptor, a VR-1 variant [27].
  • First, we tried to block the effects of AM404 with selective antagonists for the CB1 or VR1 receptors, i.e. SR141716A and capsazepine, respectively [28].
  • 4. Lactic acid-evoked increases in RL were unaffected by VR1 blockade with capsazepine, consistent with a separate lactic acid-induced reflex mechanism [17].
  • METHODS: A metabolically stable analog of AEA, methanandamide (MethA, 300 nmol/kg per min), was infused into the left renal medulla of anesthetized Wistar rats with or without a selective TRPV1 antagonist, capsazepine (Capz, 150 nmol/kg per min) or a selective cannabinoid receptor 1 (CB1) antagonist, AM251 (Am, 150 nmol/kg per min) [29].

Gene context of Lopac-C-191

  • In our psychophysical experiments, direct infusion of acidic solutions (pH > or = 6.0) into human skin caused localized pain, which was blocked by amiloride, an inhibitor of ASICs, but not by capsazepine, an inhibitor of VR1 [30].
  • VR1 was functionally implicated in these events as they were completely abrogated by the VR1 antagonist, capsazepine (CPZ) [31].
  • In conclusion, capsazepine acts on ENaCdelta and acts together with protons [22].
  • Capsazepine treatment significantly reduced the level of NK1R endocytosis, and this was associated with similar reductions in pancreatic MPO activity and histological severity of pancreatitis [32].
  • In these cells, PCs induced an increase in [Ca2+]i that was inhibited by capsazepine, a TRPV1 antagonist, and/or by amiloride, an ASIC antagonist [33].

Analytical, diagnostic and therapeutic context of Lopac-C-191


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  9. Immunological role of neuronal receptor vanilloid receptor 1 expressed on dendritic cells. Basu, S., Srivastava, P. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
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  11. Evidence that TRPM8 is an androgen-dependent Ca2+ channel required for the survival of prostate cancer cells. Zhang, L., Barritt, G.J. Cancer Res. (2004) [Pubmed]
  12. Substance P and capsaicin-induced mechanical hyperalgesia in the rat knee joint; the involvement of bradykinin B1 and B2 receptors. Davis, A.J., Perkins, M.N. Br. J. Pharmacol. (1996) [Pubmed]
  13. Anandamide and methanandamide induce both vanilloid VR1- and cannabinoid CB1 receptor-mediated changes in heart rate and blood pressure in anaesthetized rats. Malinowska, B., Kwolek, G., Göthert, M. Naunyn Schmiedebergs Arch. Pharmacol. (2001) [Pubmed]
  14. Capsaicin evokes hypothermia independent of cannabinoid CB1 and CB2 receptors. Ding, Z., Cowan, A., Rawls, S.M. Brain Res. (2005) [Pubmed]
  15. A novel capsaicin derivative VOA induced relaxation in rat mesenteric and aortic arteries: involvement of CGRP, NO, cGMP, and endothelium-dependent activities. Lo, Y.C., Hsiao, H.C., Wu, D.C., Lin, R.J., Liang, J.C., Yeh, J.L., Chen, I.J. J. Cardiovasc. Pharmacol. (2003) [Pubmed]
  16. Phorboid 20-homovanillates induce apoptosis through a VR1-independent mechanism. Macho, A., Lucena, C., Calzado, M.A., Blanco, M., Donnay, I., Appendino, G., Muñoz, E. Chem. Biol. (2000) [Pubmed]
  17. Mechanisms of capsaicin- and lactic acid-induced bronchoconstriction in the newborn dog. Nault, M.A., Vincent, S.G., Fisher, J.T. J. Physiol. (Lond.) (1999) [Pubmed]
  18. Mechanisms of acid-induced activation of airway afferent nerve fibres in guinea-pig. Kollarik, M., Undem, B.J. J. Physiol. (Lond.) (2002) [Pubmed]
  19. TRPV1 receptors mediate particulate matter-induced apoptosis. Agopyan, N., Head, J., Yu, S., Simon, S.A. Am. J. Physiol. Lung Cell Mol. Physiol. (2004) [Pubmed]
  20. Effects of ruthenium red and capsazepine on C-fibres in the rabbit iris. Wang, Z.Y., Håkanson, R. Br. J. Pharmacol. (1993) [Pubmed]
  21. Activation of TRPV1 by the satiety factor oleoylethanolamide. Ahern, G.P. J. Biol. Chem. (2003) [Pubmed]
  22. Capsazepine is a novel activator of the delta subunit of the human epithelial Na+ channel. Yamamura, H., Ugawa, S., Ueda, T., Nagao, M., Shimada, S. J. Biol. Chem. (2004) [Pubmed]
  23. Characterization of the endocannabinoid system in boar spermatozoa and implications for sperm capacitation and acrosome reaction. Maccarrone, M., Barboni, B., Paradisi, A., Bernabò, N., Gasperi, V., Pistilli, M.G., Fezza, F., Lucidi, P., Mattioli, M. J. Cell. Sci. (2005) [Pubmed]
  24. The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons. Szallasi, A., Blumberg, P.M., Annicelli, L.L., Krause, J.E., Cortright, D.N. Mol. Pharmacol. (1999) [Pubmed]
  25. High affinity antagonists of the vanilloid receptor. Wang, Y., Szabo, T., Welter, J.D., Toth, A., Tran, R., Lee, J., Kang, S.U., Suh, Y.G., Blumberg, P.M., Lee, J. Mol. Pharmacol. (2002) [Pubmed]
  26. Attenuation of acid induced oesophagitis in VR-1 deficient mice. Fujino, K., de la Fuente, S.G., Takami, Y., Takahashi, T., Mantyh, C.R. Gut (2006) [Pubmed]
  27. Ethanol modulates the VR-1 variant amiloride-insensitive salt taste receptor. I. Effect on TRC volume and Na+ flux. Lyall, V., Heck, G.L., Phan, T.H., Mummalaneni, S., Malik, S.A., Vinnikova, A.K., DeSimone, J.A. J. Gen. Physiol. (2005) [Pubmed]
  28. Compounds acting at the endocannabinoid and/or endovanilloid systems reduce hyperkinesia in a rat model of Huntington's disease. Lastres-Becker, I., de Miguel, R., De Petrocellis, L., Makriyannis, A., Di Marzo, V., Fernández-Ruiz, J. J. Neurochem. (2003) [Pubmed]
  29. Differential mechanisms mediating depressor and diuretic effects of anandamide. Li, J., Wang, D.H. J. Hypertens. (2006) [Pubmed]
  30. Amiloride-blockable acid-sensing ion channels are leading acid sensors expressed in human nociceptors. Ugawa, S., Ueda, T., Ishida, Y., Nishigaki, M., Shibata, Y., Shimada, S. J. Clin. Invest. (2002) [Pubmed]
  31. Distinct thymocyte subsets express the vanilloid receptor VR1 that mediates capsaicin-induced apoptotic cell death. Amantini, C., Mosca, M., Lucciarini, R., Perfumi, M., Morrone, S., Piccoli, M., Santoni, G. Cell Death Differ. (2004) [Pubmed]
  32. Capsaicin vanilloid receptor-1 mediates substance P release in experimental pancreatitis. Nathan, J.D., Patel, A.A., McVey, D.C., Thomas, J.E., Prpic, V., Vigna, S.R., Liddle, R.A. Am. J. Physiol. Gastrointest. Liver Physiol. (2001) [Pubmed]
  33. Vanilloid receptor activation by 2- and 10-microm particles induces responses leading to apoptosis in human airway epithelial cells. Agopyan, N., Bhatti, T., Yu, S., Simon, S.A. Toxicol. Appl. Pharmacol. (2003) [Pubmed]
  34. The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain. Walker, K.M., Urban, L., Medhurst, S.J., Patel, S., Panesar, M., Fox, A.J., McIntyre, P. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  35. Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats. Kwolek, G., Zakrzeska, A., Schlicker, E., Göthert, M., Godlewski, G., Malinowska, B. Br. J. Pharmacol. (2005) [Pubmed]
  36. Contribution of capsaicin-sensitive sensory neurons to stress-induced increases in gastric tissue levels of prostaglandins in rats. Harada, N., Okajima, K., Uchiba, M., Katsuragi, T. Am. J. Physiol. Gastrointest. Liver Physiol. (2003) [Pubmed]
  37. A capsaicin-receptor antagonist, capsazepine, reduces inflammation-induced hyperalgesic responses in the rat: evidence for an endogenous capsaicin-like substance. Kwak, J.Y., Jung, J.Y., Hwang, S.W., Lee, W.T., Oh, U. Neuroscience (1998) [Pubmed]
  38. Neurobehavioral activity in mice of N-vanillyl-arachidonyl-amide. Di Marzo, V., Breivogel, C., Bisogno, T., Melck, D., Patrick, G., Tao, Q., Szallasi, A., Razdan, R.K., Martin, B.R. Eur. J. Pharmacol. (2000) [Pubmed]
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