Histamine H4 receptor

Histamine H4 receptor High expression on bone marrow and peripheral hematopoietic cells, eosinophils, neutrophils, DC,T cells, basophils, mast cells Low expression in nerve cells, hepatocytes peripheral tissues, spleen, thymus, lung, small intestine, colon and heart Enhanced Ca +, inhibition of cAMP ... 

Histamine H receptor Histamine Hj receptor Histamine H3 receptor Histamine H4 receptor... 

O Reilly M, Alpert R, Jenkinson S, Gladue RP, Foo S, Trim S, Peter B, Trevethick M, Fidock M Identification of a histamine H4 receptor on human eosinophils - role in eosinophil chemotaxis. J Recept Signal Transduct Res 2002 22 431-448. 

Ling P, Ngo K, Nguyen S, Thurmond RL, Edwards JP, Karlsson L, Fung-Leung WP Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol 2004 142 161-171. 

Jablonowski JA, Grice CA, Chai W, et al. The first potent and selective non-imidazole human histamine H4 receptor antagonist. / Med Chem 2003 46 3957-60. 

The histamine H4-receptor which was discovered in 2001 has been shown to have a role in chemo-taxis and mediator release in various types of immune cells including mast cells, eosinophils, dendritic cells and T cells. H4-receptor antagonists have been shown to have anti-inflammatory properties and efficacy in a number of disease models, such as those for asthma and colitis in vivo. Cinnarizine has a high affinity for the H4-receptor. Recently other H4-receptor antagonists have been developed with high receptor affinity and specificity. The first few studies into the function of H4-receptors suggested... 

Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R. Evaluation of histamine HI-, H2-, and H3-receptor ligands at the human histamine H4 receptor identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 2005 314 1310-21. 

Histamine H.i receptors. 699. 727 Histamine H4 receptors. 699 Histamine receptna. 698-699 Histiocytes. 198 Histones, 833t 835... 

Jablonowski JA, Carruthers Nl, Thurmond RL. The histamine H4 receptor and potential therapeutic uses for H4 ligands. Mini-Revs Med Chem 2004 4 993-1000. 

Thurmond RL, Desai PJ, Dunford PJ, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther 2004 309 404-413. 

Kiss, R., Kiss, B., Kdnczdl, A., Szalai, F., Jelinek, 1., Laszlo, V., Noszal, B., Falus, A., and Keresii, G.M. (2008) Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. Journal of Medicinal Chemistry, 51, 3145-3153. 

Virtual Screening on the Homology Model of Histamine H4 Receptor [16]... 

Kiss, R. and Keseru, G.M. (2009) Histamine H4 receptor ligands and their potential therapeutic applications. Expert Opinion on Therapeutic Patents, 19 (2), 119-135. 

In 2011, in the synthesis of a new series of tricyclic pyrimidine compounds as histamine H4 receptor antagonists, Savall and coworkers first tried to convert the pyrimidinone compound to the chloropyrimidine compound for the subsequent S Ar displacement reaction. However, this attempted chlorination was not successful with a variety of chlorination reagents. Alternatively, they synthesized this target compound via direct amination of the tautomerizable heterocycle using BOP in the presence of DBU in DMF (11BMCL6577). 

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