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Chemical Compound Review

imetit     2-(3H-imidazol-4- yl)ethylsulfanylmethanimi...

Synonyms: Lopac-I-135, Tocris-0729, CHEMBL19439, SureCN114670, AG-K-69848, ...
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Disease relevance of imetit


High impact information on imetit


Biological context of imetit


Anatomical context of imetit


Associations of imetit with other chemical compounds

  • The electrically-evoked tritium overflow (0.3 Hz) was inhibited by histamine or the H3 receptor agonist imetit, acting via H3 receptors. and by prostaglandin E2 or the EP3 receptor agonist sulprostone, acting via EP3 receptors [16].
  • In vivo microdialysis established that neither imetit nor thioperamide altered extraneuronal levels of dopamine and its metabolites in the striatum of 6-OHDA-lesioned rats [17].
  • In previous research we found that pre-training administration of histamine H3 receptor agonists such as (R)-alpha-methylhistamine and imetit impaired rat performance in object recognition and a passive avoidance response at the same doses at which they inhibited the release of cortical acetylcholine in vivo [18].
  • The H3 receptor agonists R(alpha)methyl-HA, BP 2-94 or imetit injected intraperitoneally (ip) had no effect on basal secretion of ACTH or PRL but inhibited the ACTH and PRL responses to restraint stress and the ACTH response to LPS endotoxin [19].
  • In spontaneously hypertensive rats (SHRs), imetit also inhibited the overflow of tritium [20].

Gene context of imetit

  • RAMHA, NAMHA, and imetit inhibited forskolin-induced cAMP accumulation in HH4R-expressing cells [21].
  • Imetit potencies relative to HA were less than 0.1% and only 0.6% at HA H1 and H2 receptor reference systems, respectively [13].
  • The inhibitory effect of imetit on catecholamine-induced release of ACTH may be due to an activation of H3 receptors located presynaptically on non-histaminergic neurons, e.g. aminergic neurons [22].
  • Imetit was found not to be a substrate or an inhibitor of HMT [13].
  • Histamine, imetit, and impentamine were full agonists in the cAMP assay, but imetit exhibited only partial agonist activity through the chimeric G protein [23].


  1. Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus. Yoshimoto, R., Miyamoto, Y., Shimamura, K., Ishihara, A., Takahashi, K., Kotani, H., Chen, A.S., Chen, H.Y., Macneil, D.J., Kanatani, A., Tokita, S. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  2. Modification of formalin-induced nociception by different histamine receptor agonists and antagonists. Farzin, D., Nosrati, F. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology (2007) [Pubmed]
  3. Histamine H3 receptor agonists reduce L-dopa-induced chorea, but not dystonia, in the MPTP-lesioned nonhuman primate model of Parkinson's disease. Gomez-Ramirez, J., Johnston, T.H., Visanji, N.P., Fox, S.H., Brotchie, J.M. Mov. Disord. (2006) [Pubmed]
  4. Decreased intracellular calcium mediates the histamine H3-receptor-induced attenuation of norepinephrine exocytosis from cardiac sympathetic nerve endings. Silver, R.B., Poonwasi, K.S., Seyedi, N., Wilson, S.J., Lovenberg, T.W., Levi, R. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  5. Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors. Whyment, A.D., Blanks, A.M., Lee, K., Renaud, L.P., Spanswick, D. J. Neurophysiol. (2006) [Pubmed]
  6. G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations. Krueger, K.M., Witte, D.G., Ireland-Denny, L., Miller, T.R., Baranowski, J.L., Buckner, S., Milicic, I., Esbenshade, T.A., Hancock, A.A. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  7. Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Ling, P., Ngo, K., Nguyen, S., Thurmond, R.L., Edwards, J.P., Karlsson, L., Fung-Leung, W.P. Br. J. Pharmacol. (2004) [Pubmed]
  8. Histamine induces cytoskeletal changes in human eosinophils via the H(4) receptor. Buckland, K.F., Williams, T.J., Conroy, D.M. Br. J. Pharmacol. (2003) [Pubmed]
  9. Inhibitory H3 receptors on sympathetic nerves of the pithed rat: activation by endogenous histamine and operation in spontaneously hypertensive rats. Godlewski, G., Malinowska, B., Buczko, W., Schlicker, E. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
  10. Cardiovascular effects of selective agonists and antagonists of histamine H3 receptors in the anaesthetized rat. Coruzzi, G., Gambarelli, E., Bertaccini, G., Timmerman, H. Naunyn Schmiedebergs Arch. Pharmacol. (1995) [Pubmed]
  11. Pharmaco-ontogeny of bombesin's suppression of food intake and its attenuation by histamine H3 receptor agonists. Kent, P., Plamondon, H., Merali, Z. Brain Res. Dev. Brain Res. (1997) [Pubmed]
  12. Autoregulation of enterochromaffin-like cell histamine secretion via the histamine 3 receptor subtype. Kidd, M., Tang, L.H., Miu, K., Lawton, G.P., Sandor, A., Modlin, I.M. The Yale journal of biology and medicine. (1996) [Pubmed]
  13. S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist. Garbarg, M., Arrang, J.M., Rouleau, A., Ligneau, X., Tuong, M.D., Schwartz, J.C., Ganellin, C.R. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  14. Novel histamine H3 receptor antagonists: affinities in an H3 receptor binding assay and potencies in two functional H3 receptor models. Schlicker, E., Kathmann, M., Reidemeister, S., Stark, H., Schunack, W. Br. J. Pharmacol. (1994) [Pubmed]
  15. Modulatory effect of imetit, a histamine H3 receptor agonist, on C-fibers, cholinergic fibers and mast cells in rabbit lungs in vitro. Nemmar, A., Delaunois, A., Beckers, J.F., Sulon, J., Bloden, S., Gustin, P. Eur. J. Pharmacol. (1999) [Pubmed]
  16. Mutual interactions of the presynaptic histamine H3 and prostaglandin EP3 receptors on the noradrenergic terminals in the mouse brain. Schlicker, E., Marr, I. Neuroscience (1997) [Pubmed]
  17. Histamine H(3) receptor agonist- and antagonist-evoked vacuous chewing movements in 6-OHDA-lesioned rats occurs in an absence of change in microdialysate dopamine levels. Nowak, P., Dabrowska, J., Bortel, A., Biedka, I., Szczerbak, G., S??omian, G., Kostrzewa, R.M., Brus, R. Eur. J. Pharmacol. (2006) [Pubmed]
  18. Effects of histamine H3 receptor agonists and antagonists on cognitive performance and scopolamine-induced amnesia. Giovannini, M.G., Bartolini, L., Bacciottini, L., Greco, L., Blandina, P. Behav. Brain Res. (1999) [Pubmed]
  19. Stress-induced release of anterior pituitary hormones: effect of H3 receptor-mediated inhibition of histaminergic activity or posterior hypothalamic lesion. Knigge, U., Søe-Jensen, P., Jorgensen, H., Kjaer, A., Møller, M., Warberg, J. Neuroendocrinology (1999) [Pubmed]
  20. Identification of histamine H3 receptors in the tail artery from normotensive and spontaneously hypertensive rats. Godlewski, G., Malinowska, B., Schlicker, E., Bucher, B. J. Cardiovasc. Pharmacol. (1997) [Pubmed]
  21. Molecular cloning and characterization of a new human histamine receptor, HH4R. Nakamura, T., Itadani, H., Hidaka, Y., Ohta, M., Tanaka, K. Biochem. Biophys. Res. Commun. (2000) [Pubmed]
  22. Effect of blockade of postsynaptic H1 or H2 receptors or activation of presynaptic H3 receptors on catecholamine-induced stimulation of ACTH and prolactin secretion. Willems, E., Knigge, U., Jorgensen, H., Kjaer, A., Warberg, J. Eur. J. Endocrinol. (2000) [Pubmed]
  23. The role of transmembrane helix 5 in agonist binding to the human H3 receptor. Uveges, A.J., Kowal, D., Zhang, Y., Spangler, T.B., Dunlop, J., Semus, S., Jones, P.G. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
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