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Gene Review

Hrh3  -  histamine receptor H3

Mus musculus

Synonyms: AW049250, Eae8, H3R, HH3R, Histamine H3 receptor
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Disease relevance of Hrh3


Psychiatry related information on Hrh3


High impact information on Hrh3

  • In the developing mouse brain, histamine H3 receptor blockade, which increases histamine release, has detrimental sex-dependent effects on object recognition, spatial learning in the water maze, and pre-pulse inhibition in adulthood [8].
  • Histamine H3 receptor agonist Nalpha-methylhistamine and antagonist thioperamide had no effect [9].
  • Synthesis, X-ray crystallography, and pharmacokinetics of novel azomethine prodrugs of (R)-alpha-methylhistamine: highly potent and selective histamine H3 receptor agonists [10].
  • Azomethine derivatives of the highly potent histamine H3 receptor agonist (R)-alpha-methylhistamine (1) were prepared as lipophilic prodrugs to improve the bioavailability of the hydrophilic drug, particularly its entry into the brain [10].
  • 2 Carcinine was highly selective for the histamine H3 receptor over H1 or H2 receptor (Ki (microM)=0.2939+/-0.2188 vs 3621.2+/-583.9 or 365.3+/-232.8 microM, respectively) [11].

Biological context of Hrh3


Anatomical context of Hrh3


Associations of Hrh3 with chemical compounds


Physical interactions of Hrh3

  • The ability of histamine H3 receptor ligands to interact with 5-HT3 receptors in NG108-15 cells was studied using the whole cell patch clamp recording technique [24].

Other interactions of Hrh3


Analytical, diagnostic and therapeutic context of Hrh3


  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. Impaired drinking response in histamine H3 receptor knockout mice following dehydration or angiotensin-II challenge. Yoshimoto, R., Miyamoto, Y., Takahashi, K., Kotani, H., Kanatani, A., Tokita, S. Pharmacol. Biochem. Behav. (2006) [Pubmed]
  3. Chapter 19: What can we learn from seasonal animals about the regulation of energy balance? Morgan, P.J., Ross, A.W., Mercer, J.G., Barrett, P. Prog. Brain Res. (2006) [Pubmed]
  4. Thioperamide, the selective histamine H3 receptor antagonist, attenuates stimulant-induced locomotor activity in the mouse. Clapham, J., Kilpatrick, G.J. Eur. J. Pharmacol. (1994) [Pubmed]
  5. Inhibition of histamine versus acetylcholine metabolism as a mechanism of tacrine activity. Morisset, S., Traiffort, E., Schwartz, J.C. Eur. J. Pharmacol. (1996) [Pubmed]
  6. Enhancement of prepulse inhibition of startle in mice by the H3 receptor antagonists thioperamide and ciproxifan. Browman, K.E., Komater, V.A., Curzon, P., Rueter, L.E., Hancock, A.A., Decker, M.W., Fox, G.B. Behav. Brain Res. (2004) [Pubmed]
  7. Histamine and selective H3-receptor ligands: a possible role in the mechanism and management of epilepsy. Vohora, D., Pal, S.N., Pillai, K.K. Pharmacol. Biochem. Behav. (2001) [Pubmed]
  8. Histamine receptor-mediated signaling during development and brain function in adulthood. Raber, J. Cell. Mol. Life Sci. (2007) [Pubmed]
  9. Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. Ashida, Y., Denda, M., Hirao, T. J. Invest. Dermatol. (2001) [Pubmed]
  10. Synthesis, X-ray crystallography, and pharmacokinetics of novel azomethine prodrugs of (R)-alpha-methylhistamine: highly potent and selective histamine H3 receptor agonists. Krause, M., Rouleau, A., Stark, H., Luger, P., Lipp, R., Garbarg, M., Schwart, J.C., Schunack, W. J. Med. Chem. (1995) [Pubmed]
  11. Pharmacological effects of carcinine on histaminergic neurons in the brain. Chen, Z., Sakurai, E., Hu, W., Jin, C., Kiso, Y., Kato, M., Watanabe, T., Wei, E., Yanai, K. Br. J. Pharmacol. (2004) [Pubmed]
  12. Combining restriction digestion and touchdown PCR permits detection of trace isoforms of histamine H3 receptor. Ding, W., Zou, H., Dai, J., Duan, Z. BioTechniques (2005) [Pubmed]
  13. Structure-activity relationships of novel azomethine prodrugs of the histamine H3-receptor agonist (R)-alpha-methylhistamine: from alkylaryl to substituted diaryl derivatives. Krause, M., Rouleau, A., Stark, H., Garbarg, M., Schwartz, J.C., Schunack, W. Die Pharmazie. (1996) [Pubmed]
  14. New potent azomethine prodrugs of the histamine H3-receptor agonist (R)-alpha-methylhistamine containing a heteroarylphenyl partial structure. Krause, M., Rouleau, A., Stark, H., Luger, P., Garbarg, M., Schwartz, J.C., Schunack, W. Arch. Pharm. (Weinheim) (1996) [Pubmed]
  15. 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]
  16. Binding of histamine H3-receptor antagonists to hematopoietic progenitor cells. Evidence for a histamine transporter unrelated to histamine H3 receptors. Corbel, S., Traiffort, E., Stark, H., Schunack, W., Dy, M. FEBS Lett. (1997) [Pubmed]
  17. Steroid-sensitivity of agonist binding to pituitary cell line histamine H3 receptors. West, R.E., Myers, J., Zweig, A., Siegel, M.I., Egan, R.W., Clark, M.A. Eur. J. Pharmacol. (1994) [Pubmed]
  18. High affinity histamine H3 receptors regulate ACTH release by AtT-20 cells. Clark, M.A., Korte, A., Myers, J., Egan, R.W. Eur. J. Pharmacol. (1992) [Pubmed]
  19. Improvement by FUB 181, a novel histamine H3-receptor antagonist, of learning and memory in the elevated plus-maze test in mice. Onodera, K., Miyazaki, S., Imaizumi, M., Stark, H., Schunack, W. Naunyn Schmiedebergs Arch. Pharmacol. (1998) [Pubmed]
  20. Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Yokoyama, H., Onodera, K., Maeyama, K., Sakurai, E., Iinuma, K., Leurs, R., Timmerman, H., Watanabe, T. Eur. J. Pharmacol. (1994) [Pubmed]
  21. Replacement of imidazole by a piperidine moiety differentially affects the potency of histamine H3-receptor antagonists. Liedtke, S., Flau, K., Kathmann, M., Schlicker, E., Stark, H., Meier, G., Schunack, W. Naunyn Schmiedebergs Arch. Pharmacol. (2003) [Pubmed]
  22. Role of the histamine system in nefopam-induced antinociception in mice. Girard, P., Pansart, Y., Coppé, M.C., Verniers, D., Gillardin, J.M. Eur. J. Pharmacol. (2004) [Pubmed]
  23. Synergistic interaction between fentanyl and the histamine H3 receptor agonist R-(alpha)-methylhistamine, on the inhibition of nociception and plasma extravasation in mice. Poveda, R., Fernández-Dueñas, V., Fernández, A., Sánchez, S., Puig, M.M., Planas, E. Eur. J. Pharmacol. (2006) [Pubmed]
  24. Agonist and antagonist effects of histamine H3 receptor ligands on 5-HT3 receptor-mediated ion currents in NG108-15 cells. Allen, M.C. Eur. J. Pharmacol. (1998) [Pubmed]
  25. Effects of the histamine H3 receptor ligands thioperamide and (R)-alpha-methylhistamine on histidine decarboxylase activity of mouse brain. Sakai, N., Sakurai, A., Sakurai, E., Yanai, K., Maeyama, K., Watanabe, T. Biochem. Biophys. Res. Commun. (1992) [Pubmed]
  26. Effects of iodoproxyfan, a potent and selective histamine H3 receptor antagonist, on alpha 2 and 5-HT3 receptors. Schlicker, E., Pertz, H., Bitschnau, H., Purand, K., Kathmann, M., Elz, S., Schunack, W. Inflamm. Res. (1995) [Pubmed]
  27. Effect of thioperamide on modified forced swimming test-induced oxidative stress in mice. Akhtar, M., Pillai, K.K., Vohora, D. Basic & clinical pharmacology & toxicology. (2005) [Pubmed]
  28. Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands. Sasse, A., Ligneau, X., Sadek, B., Elz, S., Pertz, H.H., Ganellin, C.R., Arrang, J.M., Schwartz, J.C., Schunack, W., Stark, H. Arch. Pharm. (Weinheim) (2001) [Pubmed]
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