By Katherine Figueroa, Nigel Shankley (auth.), Robin L. Thurmond PhD (eds.)
The yr 2010 marks the centennial for the identity of histamine and the 1st glimpse of its many physiological features. From those preliminary findings a wealthy tapestry of study 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 medications were such a success that the time period “antihistamine” has entered the typical lexicon. This quantity is an try and provide a photograph in time as to the present realizing of the function of histamine in exactly one very important healing area—inflammation. the 1st 3 chapters supply a few history context for the remainder of the ebook beginning out with a ancient viewpoint by way of Figueroa and Shankley. Bongers et al supply 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 ailment parts the place histamine is understood to be concerned. bankruptcy four by way of Thomas Taylor-Clark outlines the function of histamine in allergic rhinitis, a space have been antihistamines are primary. this is often additionally actual for ocular hypersensitive reaction as mentioned via Ohbayashi et al. either one of those chapters spotlight facets of those stipulations which are nonetheless now not well-controlled and recommend the software of latest antihistamines concentrating on different histamine receptors.
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Extra resources for Histamine in Inflammation
12,13 Recently, considerable progress has been made in the purification and crystallization of several members of the rhodopsin class of GPCRs,14-16 likely further enhancing the success of GPCR based drug discovery. Histamine Receptors, Signal Transduction and Their Ligands In the next paragraphs we will discuss various molecular pharmacological aspects of the four different receptor subtypes, including the availability of selective subtype selective agonists and antagonists. The Histamine H1 Receptor and Its Ligands The histamine H1 receptor (H1R) is found mainly on smooth muscle cells, endothelium and in the CNS.
Lim HD, Smits RA, Bakker RA et al. Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. J Med Chem 2006; 49(23):6650-6651. 81. Thurmond RL, Desai PJ, Dunford PJ et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther Apr 2004; 309(1):404-413. 82. Coruzzi G, Adami M, Guaita E et al. Anti-inflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation.
80. Lim HD, Smits RA, Bakker RA et al. Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. J Med Chem 2006; 49(23):6650-6651. 81. Thurmond RL, Desai PJ, Dunford PJ et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther Apr 2004; 309(1):404-413. 82. Coruzzi G, Adami M, Guaita E et al. Anti-inflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation.