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Chemical Compound Review

Thioperamide     N-cyclohexyl-4-(3H-imidazol- 4...

Synonyms: Lopac-T-123, Tocris-0644, CHEMBL260374, CHEBI:529662, SN429, ...
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Disease relevance of Tocris-0644

  • The results showed that thioperamide, an H3R inverse agonist, increases, whereas imetit, an H3R agonist, decreases appetite and body weight in diet-induced obese (DiO) WT mice [1].
  • The inhibition was reversed by micromolar concentrations of the histamine H3 receptor antagonist thioperamide and was sensitive to cholera or pertussis toxin treatment [2].
  • The ICV administration of thioperamide (40.8, 122.4, and 408.5 micrograms/10 microL) did not suppress the 4-hour food intake induced by 16-hour fasting; however, thioperamide produced dose-dependent and strong inhibition of hyperphagia induced by a 3-microgram dose of PYY [3].
  • 3. R-alpha-MH caused a thioperamide-sensitive fall in mean arterial pressure (MAP) of 8+/-1 mmHg and tachycardia of 18+/-2 bpm (P<0.0005) [4].
  • We studied acid variations and plasma gastrin in cats harboring Helicobacter felis, harboring H. pylori, or free of gastric pathogens with reference to thioperamide (H(3) receptor antagonist) and SR-27417A (PAF receptor antagonist) [5].

Psychiatry related information on Tocris-0644


High impact information on Tocris-0644

  • In cultures with IL-4 plus anti-CD58 mAb, histamine-induced enhancement of IgE and IgG4 production was specifically blocked by thioperamide (H3 receptor antagonist), and was inhibited by anti-IL-10 antibody (Ab) [11].
  • Histamine also enhanced IgE and IgG4 production by in vivo-generated sIgE+ and sIgG4+ B cells, respectively, from atopic patients; enhancement was blocked by dimaprit and thioperamide, and was inhibited by anti-IL-6 mAb and anti-IL-10 Ab [11].
  • The expression of UCP1 in brown adipose tissue and of UCP3 in brown adipose tissue, white adipose tissue, and skeletal muscle is decreased in H3(-/-) mutants, and the anorexigenic activity of thioperamide is not observed [12].
  • Somatostatin antibody increased basal histamine secretion and abolished the decrease in histamine and acid secretion induced by thioperamide, confirming that changes in histamine and acid secretion induced by the activation of H3 receptors reflected changes in somatostatin secretion [13].
  • RESULTS: Superfusion with thioperamide (H3 antagonist) increased somatostatin and decreased gastrin and histamine secretion in all three species; superfusion with (r)-alpha-methylhistamine (H3 agonist) had the opposite effect [14].

Chemical compound and disease context of Tocris-0644


Biological context of Tocris-0644


Anatomical context of Tocris-0644


Associations of Tocris-0644 with other chemical compounds


Gene context of Tocris-0644


Analytical, diagnostic and therapeutic context of Tocris-0644

  • Intraperitoneal injection of an H3 antagonist (thioperamide) increased histamine output in mesenteric lymph and stimulated intestinal ornithine decarboxylase activity [37].
  • Systemic administration of either thioperamide (5 mg/kg, i.p.), a selective H3 receptor antagonist, or metoprine (10 mg/kg, i.p.), an inhibitor of HA-N-methyltransferase, caused an approximately twofold increase in the HA output 30-60 min after treatment [38].
  • 5. Thioperamide-induced antinociception was completely prevented by pretreatment with a non-hyperalgesic i.p. dose of (R)-alpha-methylhistamine in the mouse hot plate and abdominal constriction tests [39].
  • Autoradiography of sagittal and frontal sections evidenced specific labelling in a number of gray matter areas over a very low background, as determined using thioperamide, a selective H3-receptor antagonist, as competing drug [40].
  • Although highly potent H3 antagonists such as thioperamide lacked antinociceptive activity, homologs of burimamide and thioperamide containing N-aromatic substituents retained H3 antagonist activity and also showed potent, effective analgesia [41].


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  2. Purification of a histamine H3 receptor negatively coupled to phosphoinositide turnover in the human gastric cell line HGT1. Cherifi, Y., Pigeon, C., Le Romancer, M., Bado, A., Reyl-Desmars, F., Lewin, M.J. J. Biol. Chem. (1992) [Pubmed]
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  5. Putative effect of Helicobacter pylori and gastritis on gastric acid secretion in cat. Sobhani, I., Canedo, S., Alchepo, B., Vissuzaine, C., Chevalier, C., Buyse, M., Moizo, L., Laigneau, J.P., Mignon, M., Lewin, J.M., Bado, A. Am. J. Physiol. Gastrointest. Liver Physiol. (2002) [Pubmed]
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  11. Histamine selectively enhances human immunoglobulin E (IgE) and IgG4 production induced by anti-CD58 monoclonal antibody. Kimata, H., Fujimoto, M., Ishioka, C., Yoshida, A. J. Exp. Med. (1996) [Pubmed]
  12. Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. Takahashi, K., Suwa, H., Ishikawa, T., Kotani, H. J. Clin. Invest. (2002) [Pubmed]
  13. Histamine, acting via H3 receptors, inhibits somatostatin and stimulates acid secretion in isolated mouse stomach. Vuyyuru, L., Schubert, M.L. Gastroenterology (1997) [Pubmed]
  14. Dual inhibitory pathways link antral somatostatin and histamine secretion in human, dog, and rat stomach. Vuyyuru, L., Schubert, M.L., Harrington, L., Arimura, A., Makhlouf, G.M. Gastroenterology (1995) [Pubmed]
  15. Activation of histamine H3 receptors inhibits carrier-mediated norepinephrine release in a human model of protracted myocardial ischemia. Hatta, E., Yasuda, K., Levi, R. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  16. Histamine H3 antagonist thioperamide dose-dependently enhances memory consolidation and reverses amnesia induced by dizocilpine or scopolamine in a one-trial inhibitory avoidance task in mice. Bernaerts, P., Lamberty, Y., Tirelli, E. Behav. Brain Res. (2004) [Pubmed]
  17. Reduction in brain infarction by augmentation of central histaminergic activity in rats. Motoki, A., Adachi, N., Semba, K., Liu, K., Arai, T. Brain Res. (2005) [Pubmed]
  18. The H3 antagonist thioperamide reveals conditioned preference for a context associated with an inactive small dose of cocaine in C57BL/6J mice. Brabant, C., Charlier, Y., Quertemont, E., Tirelli, E. Behav. Brain Res. (2005) [Pubmed]
  19. Histamine H3-receptor-mediated inhibition of calcitonin gene-related peptide release from cardiac C fibers. A regulatory negative-feedback loop. Imamura, M., Smith, N.C., Garbarg, M., Levi, R. Circ. Res. (1996) [Pubmed]
  20. Histamine H3 receptors modulate antigen-induced bronchoconstriction in guinea pigs. Ichinose, M., Barnes, P.J. J. Allergy Clin. Immunol. (1990) [Pubmed]
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  22. Changes in the histaminergic system during vestibular compensation in the cat. Tighilet, B., Trottier, S., Mourre, C., Lacour, M. J. Physiol. (Lond.) (2006) [Pubmed]
  23. Design of potent non-thiourea H3-receptor histamine antagonists. Ganellin, C.R., Hosseini, S.K., Khalaf, Y.S., Tertiuk, W., Arrang, J.M., Garbarg, M., Ligneau, X., Schwartz, J.C. J. Med. Chem. (1995) [Pubmed]
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  25. Liver-expressed chemokine/CC chemokine ligand 16 attracts eosinophils by interacting with histamine H4 receptor. Nakayama, T., Kato, Y., Hieshima, K., Nagakubo, D., Kunori, Y., Fujisawa, T., Yoshie, O. J. Immunol. (2004) [Pubmed]
  26. Basophil mediator release in atopic dermatitis. Bull, H.A., Courtney, P.F., Bunker, C.B., Rustin, M.H., Pearce, F.L., Dowd, P.M. J. Invest. Dermatol. (1993) [Pubmed]
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  28. Critical role of histamine H4 receptor in leukotriene B4 production and mast cell-dependent neutrophil recruitment induced by zymosan in vivo. Takeshita, K., Sakai, K., Bacon, K.B., Gantner, F. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  29. Stimulatory effect of histamine on cyclic AMP formation in chick pineal gland. Nowak, J.Z., Sek, B. J. Neurochem. (1994) [Pubmed]
  30. Histamine H3 receptor-mediated depression of synaptic transmission in the dentate gyrus of the rat in vitro. Brown, R.E., Reymann, K.G. J. Physiol. (Lond.) (1996) [Pubmed]
  31. Histamine protects against NMDA-induced necrosis in cultured cortical neurons through H receptor/cyclic AMP/protein kinase A and H receptor/GABA release pathways. Dai, H., Zhang, Z., Zhu, Y., Shen, Y., Hu, W., Huang, Y., Luo, J., Timmerman, H., Leurs, R., Chen, Z. J. Neurochem. (2006) [Pubmed]
  32. Effects of histamine H3 receptor ligands in experimental models of anxiety and depression. Pérez-García, C., Morales, L., Cano, M.V., Sancho, I., Alguacil, L.F. Psychopharmacology (Berl.) (1999) [Pubmed]
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  34. Histamine receptor subtypes mediating hyperpolarization in the isolated, perfused rat mesenteric pre-arteriolar bed. Adeagbo, A.S., Oriowo, M.A. Eur. J. Pharmacol. (1998) [Pubmed]
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  36. Histamine secretion from rat enterochromaffinlike cells. Prinz, C., Kajimura, M., Scott, D.R., Mercier, F., Helander, H.F., Sachs, G. Gastroenterology (1993) [Pubmed]
  37. Role of histamine receptors in intestinal repair after ischemia-reperfusion in rats. Tsunada, S., Fujimoto, K., Gotoh, Y., Sakai, T., Kang, M., Sakata, T., Granger, D.N., Tso, P. Gastroenterology (1994) [Pubmed]
  38. Characterization of histamine release from the rat hypothalamus as measured by in vivo microdialysis. Itoh, Y., Oishi, R., Nishibori, M., Saeki, K. J. Neurochem. (1991) [Pubmed]
  39. Role of histamine in rodent antinociception. Malmberg-Aiello, P., Lamberti, C., Ghelardini, C., Giotti, A., Bartolini, A. Br. J. Pharmacol. (1994) [Pubmed]
  40. A detailed autoradiographic mapping of histamine H3 receptors in rat brain areas. Pollard, H., Moreau, J., Arrang, J.M., Schwartz, J.C. Neuroscience (1993) [Pubmed]
  41. Novel qualitative structure-activity relationships for the antinociceptive actions of H2 antagonists, H3 antagonists and derivatives. Hough, L.B., Nalwalk, J.W., Li, B.Y., Leurs, R., Menge, W.M., Timmerman, H., Carlile, M.E., Cioffi, C., Wentland, M. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
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