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Chemical Compound Review

histamine     2-(3H-imidazol-4-yl)ethanamine

Synonyms: Ergamine, Histamin, Istamina, Theramine, Eramin, ...
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Disease relevance of peremin

  • Compared to histamine, which causes constriction of airways and edema formation, the leukotrienes are three to four orders of magnitude more potent and the effects have longer duration [1].
  • Blood specimens were obtained from each arm serially over a one-hour interval, and serum speciments were assessed for histamine, eosinophil chemotactic factor of anaphylaxis, and complement components [2].
  • Topical glucocorticosteroids significantly reduced both the symptoms and the levels of histamine, TAME-esterase activity, and kinins in the early, late, and rechallenge allergic reactions [3].
  • Autoantibodies against the high-affinity IgE receptor as a cause of histamine release in chronic urticaria [4].
  • The severity of pruritus was scored weekly, and plasma histamine levels were measured at the beginning and end of each five-week period [5].
  • The ingestion of histamine-rich food or of alcohol or drugs that release histamine or block DAO may provoke diarrhea, headache, rhinoconjunctival symptoms, asthma, hypotension, arrhythmia, urticaria, pruritus, flushing, and other conditions in patients with histamine intolerance [6].
  • From the above we conclude that the histamine H(3) agonism may augment motor dyskinesia in Parkinson's disease (PD) patients and presumably worsen L-DOPA therapy [7].

Psychiatry related information on peremin

  • In a classical conditioning procedure in which an immunologic challenge was paired with the presentation of an odor, guinea pigs showed a plasma histamine increase when presented with the odor alone [8].
  • We hypothesize that the activity of histamine cells is linked to the maintenance of waking, in contrast to activity in noradrenergic and serotonergic neurons, which is more tightly coupled to the maintenance of muscle tone in waking and its loss in REM sleep and cataplexy [9].
  • We now report that, in contrast to these other monoaminergic "REM-off" cell groups, histamine neurons are active in cataplexy at a level similar to or greater than that in quiet waking [9].
  • Here we provide several lines of evidence that orexin A induces wakefulness by means of the TMN and histamine H(1) receptor (H1R) [10].
  • Effects of the histamine H(1) receptor blocker, pyrilamine, on spontaneous locomotor activity of rats with long-term portacaval anastomosis [11].

High impact information on peremin


Chemical compound and disease context of peremin


Biological context of peremin


Anatomical context of peremin

  • We present a model for the control of immunoglobulin E (IgE)-mediated histamine release from human basophils [23].
  • Letter: Reagin-mediated histamine release from human leukocytes by human IgG [24].
  • The serum histamine concentration rose, with an augmentation of eosinophil and neutrophil chemotactic activities [25].
  • Following an initial treatment with histamine, endothelial cells were unable to respond to histamine for 3 hr, after which the PGI2 biosynthetic response rapidly returned to normal by 4 1/2 hr [26].
  • A positive clinical response was associated with an increase in the number of T-cell histamine H2 receptors to normal levels and with correction of the other immunologic abnormalities [27].

Associations of peremin with other chemical compounds


Gene context of peremin

  • Within minutes after stimulation with phorbol esters or histamine, human endothelial cells become adhesive for neutrophils; this interaction is inhibited by antibodies to GMP-140 [34].
  • The synergism between PlGF and VEGF was specific, as PlGF deficiency impaired the response to VEGF, but not to bFGF or histamine [35].
  • In contrast to IL-3, other cytokines (IL-5, granulocyte/macrophage colony-stimulating factor, and nerve growth factor) that also prime basophils for enhanced histamine and leukotriene C4 release did not promote IgER-induced IL-4 synthesis [36].
  • IL 3 and GM-CSF possessed significant histamine-releasing activity in 8 of 10 and 12 of 14 subjects, respectively [37].
  • These results suggest that mast cells may sustain chronic inflammatory processes by upregulating self-induction of IL-1 through histamine release [38].
  • The histamine-induced CTGF expression was mediated through the histamine receptor (HR1) and could be completely abolished by TNF-alpha [39].
  • Histamine increased IL-1beta-induced GM-CSF release and markedly reduced TNF-alpha-induced RANTES release by both asthmatic and nonasthmatic cells to a similar extent, but did not modulate PGE(2) release [40].
  • Using specific pharmacological inhibitors and small interfering RNA technology, we determined that PKCdelta and ERK, but not p38 and JNK, mediate histamine-induced Egr-1 expression [41].
  • Our data suggest that histamine stimulates phospholipase C-signaling in myometrial smooth muscle cells through H(1) histamine receptors and that GRK2 recruitment is a key mechanism in the regulation of H(1) histamine receptor signaling in human uterine smooth muscle [42].

Analytical, diagnostic and therapeutic context of peremin

  • We compared this regimen with immunotherapy using insect venoms or placebo in groups of 20 patients matched for history and sensitivity, as judged by venom skin test, histamine release and IgE antibody to venom [43].
  • We monitored their responses by means of symptom scores and measurements of the levels of histamine, tosyl-L-arginine methyl ester (TAME)-esterase activity, and kinins in nasal lavages [3].
  • The percentage of T lymphocytes bearing histamine Type 2 receptors was lower in the atopic group than in the control group (P less than 0.001), but the percentage of cells with Type 1 receptors was the same in both groups [44].
  • When the initial histamine treatment was carried out under mildly alkaline conditions, the complete return of activity was delayed to 8 hr after treatment [26].
  • We undertook a 10-week placebo-controlled, double-blind, crossover study in a group of patients receiving hemodialysis who had severe pruritus, to investigate the effects of recombinant human erythropoietin on their pruritus and plasma histamine levels [5].


  1. Leukotrienes. Hammarström, S. Annu. Rev. Biochem. (1983) [Pubmed]
  2. Cold urticaria: release into the circulation of histamine and eosinophil chemotactic factor of anaphylaxis during cold challenge. Soter, N.A., Wasserman, S.I., Austen, K.F. N. Engl. J. Med. (1976) [Pubmed]
  3. Inhibition of mediator release in allergic rhinitis by pretreatment with topical glucocorticosteroids. Pipkorn, U., Proud, D., Lichtenstein, L.M., Kagey-Sobotka, A., Norman, P.S., Naclerio, R.M. N. Engl. J. Med. (1987) [Pubmed]
  4. Autoantibodies against the high-affinity IgE receptor as a cause of histamine release in chronic urticaria. Hide, M., Francis, D.M., Grattan, C.E., Hakimi, J., Kochan, J.P., Greaves, M.W. N. Engl. J. Med. (1993) [Pubmed]
  5. Relief of pruritus and decreases in plasma histamine concentrations during erythropoietin therapy in patients with uremia. De Marchi, S., Cecchin, E., Villalta, D., Sepiacci, G., Santini, G., Bartoli, E. N. Engl. J. Med. (1992) [Pubmed]
  6. Histamine and histamine intolerance. Maintz, L., Novak, N. Am. J. Clin. Nutr. (2007) [Pubmed]
  7. Histamine H(3) receptor ligands modulate L-dopa-evoked behavioral responses and L-dopa derived extracellular dopamine in dopamine-denervated rat striatum. Nowak, P., Bortel, A., Dabrowska, J., Biedka, I., Slomian, G., Roczniak, W., Kostrzewa, R.M., Brus, R. Neurotox. Res (2008) [Pubmed]
  8. Learned histamine release. Russell, M., Dark, K.A., Cummins, R.W., Ellman, G., Callaway, E., Peeke, H.V. Science (1984) [Pubmed]
  9. Cataplexy-active neurons in the hypothalamus: implications for the role of histamine in sleep and waking behavior. John, J., Wu, M.F., Boehmer, L.N., Siegel, J.M. Neuron (2004) [Pubmed]
  10. Arousal effect of orexin A depends on activation of the histaminergic system. Huang, Z.L., Qu, W.M., Li, W.D., Mochizuki, T., Eguchi, N., Watanabe, T., Urade, Y., Hayaishi, O. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  11. Effects of the histamine H(1) receptor blocker, pyrilamine, on spontaneous locomotor activity of rats with long-term portacaval anastomosis. Lozeva, V., Valjakka, A., Lecklin, A., Olkkonen, H., Hippeläinen, M., Itkonen, M., Plumed, C., Tuomisto, L. Hepatology (2000) [Pubmed]
  12. Preventing bronchoconstriction in exercise-induced asthma with inhaled heparin. Ahmed, T., Garrigo, J., Danta, I. N. Engl. J. Med. (1993) [Pubmed]
  13. Tryptase levels as an indicator of mast-cell activation in systemic anaphylaxis and mastocytosis. Schwartz, L.B., Metcalfe, D.D., Miller, J.S., Earl, H., Sullivan, T. N. Engl. J. Med. (1987) [Pubmed]
  14. Improved diagnosis of mastocytosis by measurement of urinary histamine metabolites. Keyzer, J.J., de Monchy, J.G., van Doormaal, J.J., van Voorst Vader, P.C. N. Engl. J. Med. (1983) [Pubmed]
  15. Role of platelet-activating factor-acether in mediating guinea pig anaphylaxis. Darius, H., Lefer, D.J., Smith, J.B., Lefer, A.M. Science (1986) [Pubmed]
  16. Prostaglandins, leukotrienes, and platelet-activating factor in shock. Feuerstein, G., Hallenbeck, J.M. Annu. Rev. Pharmacol. Toxicol. (1987) [Pubmed]
  17. Cromolyn therapy in patients with bronchial asthma. Effect on inhalation challenge with allergen, histamine, and methacholine. Ryo, U.Y., Kang, B., Townley, R.G. JAMA (1976) [Pubmed]
  18. Immediate hypersensitivity to hog trypsin resulting from industrial exposure. Colten, H.R., Polakoff, P.L., Weinstein, S.F., Strieder, D.J. N. Engl. J. Med. (1975) [Pubmed]
  19. Histamine and nocturnal wheezing. Drazen, J. N. Engl. J. Med. (1980) [Pubmed]
  20. Evidence that histamine is the causative toxin of scombroid-fish poisoning. Morrow, J.D., Margolies, G.R., Rowland, J., Roberts, L.J. N. Engl. J. Med. (1991) [Pubmed]
  21. Engagement of the high-affinity IgE receptor activates src protein-related tyrosine kinases. Eiseman, E., Bolen, J.B. Nature (1992) [Pubmed]
  22. Histamine plays a part in induction of drinking by food intake. Kraly, F.S. Nature (1983) [Pubmed]
  23. A model of cell activation and desensitization by surface immunoglobin: the case of histamine release from human basophils. Dembo, M., Goldstein, B. Cell (1980) [Pubmed]
  24. Letter: Reagin-mediated histamine release from human leukocytes by human IgG. Vijay, H.M., Perelmutter, L. N. Engl. J. Med. (1975) [Pubmed]
  25. Release of mast-cell mediators and alterations in lung function in patients with cholinergic urticaria. Soter, N.A., Wasserman, S.I., Austen, K.F., McFadden, E.R. N. Engl. J. Med. (1980) [Pubmed]
  26. Regulation of histamine-mediated prostacyclin synthesis in cultured human vascular endothelial cells. Baenziger, N.L., Fogerty, F.J., Mertz, L.F., Chernuta, L.F. Cell (1981) [Pubmed]
  27. Histiocytosis-X. Osband, M.E., Lipton, J.M., Lavin, P., Levey, R., Vawter, G., Greenberger, J.S., McCaffrey, R.P., Parkman, R. N. Engl. J. Med. (1981) [Pubmed]
  28. Nosocomial pneumonia in intubated patients given sucralfate as compared with antacids or histamine type 2 blockers. The role of gastric colonization. Driks, M.R., Craven, D.E., Celli, B.R., Manning, M., Burke, R.A., Garvin, G.M., Kunches, L.M., Farber, H.W., Wedel, S.A., McCabe, W.R. N. Engl. J. Med. (1987) [Pubmed]
  29. Allergic reactions in healthy plateletpheresis donors caused by sensitization to ethylene oxide gas. Leitman, S.F., Boltansky, H., Alter, H.J., Pearson, F.C., Kaliner, M.A. N. Engl. J. Med. (1986) [Pubmed]
  30. Differential release of serotonin and histamine from mast cells. Theoharides, T.C., Bondy, P.K., Tsakalos, N.D., Askenase, P.W. Nature (1982) [Pubmed]
  31. Histamine directly and synergistically with lipopolysaccharide stimulates cyclooxygenase-2 expression and prostaglandin I(2) and E(2) production in human coronary artery endothelial cells. Tan, X., Essengue, S., Talreja, J., Reese, J., Stechschulte, D.J., Dileepan, K.N. J. Immunol. (2007) [Pubmed]
  32. Histamine action on vertebrate GABAA receptors: direct channel gating and potentiation of GABA responses. Saras, A., Gisselmann, G., Vogt-Eisele, A.K., Erlkamp, K.S., Kletke, O., Pusch, H., Hatt, H. J. Biol. Chem. (2008) [Pubmed]
  33. Helicobacter pylori vacuolating cytotoxin inhibits duodenal bicarbonate secretion by a histamine-dependent mechanism in mice. Tuo, B., Song, P., Wen, G., Sewald, X., Gebert-Vogl, B., Haas, R., Manns, M., Seidler, U. J. Infect. Dis. (2009) [Pubmed]
  34. Rapid neutrophil adhesion to activated endothelium mediated by GMP-140. Geng, J.G., Bevilacqua, M.P., Moore, K.L., McIntyre, T.M., Prescott, S.M., Kim, J.M., Bliss, G.A., Zimmerman, G.A., McEver, R.P. Nature (1990) [Pubmed]
  35. Synergism between vascular endothelial growth factor and placental growth factor contributes to angiogenesis and plasma extravasation in pathological conditions. Carmeliet, P., Moons, L., Luttun, A., Vincenti, V., Compernolle, V., De Mol, M., Wu, Y., Bono, F., Devy, L., Beck, H., Scholz, D., Acker, T., DiPalma, T., Dewerchin, M., Noel, A., Stalmans, I., Barra, A., Blacher, S., Vandendriessche, T., Ponten, A., Eriksson, U., Plate, K.H., Foidart, J.M., Schaper, W., Charnock-Jones, D.S., Hicklin, D.J., Herbert, J.M., Collen, D., Persico, M.G. Nat. Med. (2001) [Pubmed]
  36. Human peripheral blood basophils primed by interleukin 3 (IL-3) produce IL-4 in response to immunoglobulin E receptor stimulation. Brunner, T., Heusser, C.H., Dahinden, C.A. J. Exp. Med. (1993) [Pubmed]
  37. Human recombinant granulocyte-macrophage colony-stimulating factor and interleukin 3 cause basophil histamine release. Haak-Frendscho, M., Arai, N., Arai, K., Baeza, M.L., Finn, A., Kaplan, A.P. J. Clin. Invest. (1988) [Pubmed]
  38. Histamine enhances interleukin (IL)-1-induced IL-1 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells. Comparison with IL-1 receptor antagonist. Vannier, E., Dinarello, C.A. J. Clin. Invest. (1993) [Pubmed]
  39. Connective tissue growth factor expression is regulated by histamine in lung fibroblasts: potential role of histamine in airway remodeling. Kunzmann, S., Schmidt-Weber, C., Zingg, J.M., Azzi, A., Kramer, B.W., Blaser, K., Akdis, C.A., Speer, C.P. J. Allergy Clin. Immunol. (2007) [Pubmed]
  40. Histamine and tryptase modulate asthmatic airway smooth muscle GM-CSF and RANTES release. Chhabra, J., Li, Y.Z., Alkhouri, H., Blake, A.E., Ge, Q., Armour, C.L., Hughes, J.M. Eur. Respir. J. (2007) [Pubmed]
  41. Histamine induces Egr-1 expression in human aortic endothelial cells via the H1 receptor-mediated protein kinase Cdelta-dependent ERK activation pathway. Hao, F., Tan, M., Xu, X., Cui, M.Z. J. Biol. Chem. (2008) [Pubmed]
  42. Selective regulation of H1 histamine receptor signaling by G protein-coupled receptor kinase 2 in uterine smooth muscle cells. Willets, J.M., Taylor, A.H., Shaw, H., Konje, J.C., Challiss, R.A. Mol. Endocrinol. (2008) [Pubmed]
  43. A controlled trial of immunotherapy in insect hypersensitivity. Hunt, K.J., Valentine, M.D., Sobotka, A.K., Benton, A.W., Amodio, F.J., Lichtenstein, L.M. N. Engl. J. Med. (1978) [Pubmed]
  44. Abnormal histamine-induced suppressor-cell function in atopic subjects. Beer, D.J., Osband, M.E., McCaffrey, R.P., Soter, N.A., Rocklin, R.E. N. Engl. J. Med. (1982) [Pubmed]
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