By Katherine Figueroa, Nigel Shankley (auth.), Robin L. Thurmond PhD (eds.)
The yr 2010 marks the centennial for the id of histamine and the 1st glimpse of its many physiological capabilities. From those preliminary findings a wealthy tapestry of analysis has exposed roles for histamine in virtually each physiological technique with new findings rising each year. those assorted roles of histamine have made for fertile floor for the invention of novel therapeutics, and those medicinal drugs were such a success that the time period “antihistamine” has entered the typical lexicon. This quantity is an try to supply a photo in time as to the present realizing of the function of histamine in exactly one vital healing area—inflammation. the 1st 3 chapters offer a few heritage context for the remainder of the publication beginning out with a historic viewpoint by way of Figueroa and Shankley. Bongers et al offer an summary of the pharmacology of the 4 histamine receptors and the bankruptcy via Hiroshi Ohtsu describes how histamine is synthesized in addition to the insights derived from mice the place this synthesis is disrupted. the subsequent a number of chapters speak about sickness parts the place histamine is understood to be concerned. bankruptcy four through Thomas Taylor-Clark outlines the function of histamine in allergic rhinitis, a space have been antihistamines are standard. this is often additionally real for ocular hypersensitivity as mentioned through Ohbayashi et al. either one of those chapters spotlight elements of those stipulations which are nonetheless no longer well-controlled and recommend the application of recent antihistamines concentrating on different histamine receptors.
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Additional info for Histamine in Inflammation
5 Epigenetic Regulation of HDC Gene Expression In hematopoietic cell lineages, HDC gene expression has been reported in mast cells and basophils. 5 A correlation between HDC expression and hypomethylation was also found in primary mast cells and methylation of a HDC promoter-luciferase reporter construct resulted in decreased luciferase activity in a transient expression system. 27 The induction of gene expression is correlated with the demethylation of the promoter. Consistently, forced demethylation by 5-azacytidine treatment induced high expression of HDC mRNA in P815 cells.
1,2 Histamine regulates smooth muscle contraction, immune responses, vascular permeability, neurotransmission and the stimulation of gastric acid secretion. 3 HDC is expressed in the liver of developing fetuses and in the stomach, brain, thymus, kidney, spleen and bones. Restricted and cell-specific expression of HDC in peripheral tissues is controlled both transcriptionally by processes such as DNA methylation4,5 and posttranslationally where levels can be controlled by the ubiquitin-proteasome system,6,7 caspases8 and other mechanisms.
Elz S, Kramer K, Pertz HH et al. Histaprodifens: synthesis, pharmacological in vitro evaluation and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists. J Med Chem 2000; 43(6):1071-1084. 21. Malinowska B, Piszcz J, Schlicker E et al. Histaprodifen, methylhistaprodifen and dimethylhistaprodifen are potent H1-receptor agonists in the pithed and in the anaesthetized rat. Naunyn Schmiedebergs Arch Pharmacol 1999; 359(1):11-16. 22. Menghin S, Pertz HH, Kramer K et al.