Histamine receptor antagonists chemistry

Buyniski, L. et al., SARs among Newer Histamine H2 Anatagonists. Second Camerino Symposium on Recent Advances in Receptor Antagonist Chemistry (Camerino), 1983. 

Although most of the medicinal chemistry effort in the H3 receptor field has been focused on the development of antagonists, there is some interest in agonists as well. Histamine H3 receptor agonists decrease the release of histamine in the central and peripheral nervous system and lead to a weakened histaminergic tone. In the brain, their effects will therefore be comparable to those of Hi receptor antagonists, with sedation and induction of sleep as a prominent observation. Indeed, H3 agonists such as the imidazoles... 

Zhang MQ, Leurs R, Timmerman H. Histamine H receptor antagonists. In Burger s Medicinal Chemistry and Drug Discovery. Wolff M E (Ed.).)ohn Wiley Sons, 1997. 

Histamine receptors were reviewed in 1973 before the advent of the H2 antagonists later developments are described in reference 4, and the subject was mentioned briefly in these reports in 1975 and 1977. The classification and distribution of histamine receptors has been discussed by Black and reviewed by Chand and Eyre. The Physiological Society of Philadelphia held a symposium on histamine receptors in 1977, the proceedings of which are in press. A symposium was held in 1978 at the Vlth International Conference on Medicinal Chemistry, Brighton, England (proceedings to be published). In addition, there have been several symposia on H2-receptor histamine antagonists, mainly concerned with clinical aspects. 

The reactivity of 1,2,5-thiadiazole 1,1-dioxide derivatives, as many other aspects of their chemistry, has not been fully explored, and only a heterogeneous series of generally unrelated reactions is known. Nevertheless, the discovery of the potential of thiadiazole 1,1-dioxides as urea equivalent fragments (82JMC207,82JMC210) in the development of new histamine Hj-receptor antagonists (Section VI) may perhaps increase the interest in this field. 

Stark, H., Kathmann, M., Schlicker, E., Schunack, W., Schlegel, B., and Sippl, W. (2004) Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists. Mini Reviews in Medicinal Chemistry, 4, 965—977. 

Stark, H., Purand, K., Ligneau, X., Rouleau, A., Arrang. J.-M., Garbarg, M., Schwartz, J.-C., and Schunack, W. (1996) Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity. Journal of Medicinal Chemistry, 39, 1157-1163. 

Durant, G.J., Emmett, J.C., GanelUn, C.R. et al. (1977) Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine. Journal of Medicinal Chemistry, 20, 901-906. 

Young R.C., R.C. Mitchell, T.H. Brown, C.R. Ganellin, R. Griffiths, M. Jones, K.K. Rana, D. Saunders, 1. R. Smith, N.E. Sore, and T.J. Wilks (1988). Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists. Journal of Medicinal Chemistry 31 656-671. 

Ganellin, G. R., Durant, G. J. Histamine H2-Receptor Agonists and Antagonists. In M. E. Wolff (Ed.), Burger s Medicinal Chemistry, (4th ed., Chapter 48). New York Wiley Sons, 1981. 

This was one of several strategies tried out by the SK F workers. To begin with, a study of known agonists and antagonists in other fields of medicinal chemistry was carried out. The structural differences between agonists and antagonists for a particular receptor were identified and then similar alterations were tried on histamine. 

Ganellin, C. R. Discovery of dmetidine, ranitidine and other H2-receptor histamine antagonists. In Medicinal Chemistry The Role of Organic Chemistry in Drug Research. (Ganellin, C. R., Roberts, S. M., Eds.), Academic Press London, 1993, pp. 227—255. 

Ganellin, C.R. (1993) Discovery of cimetidine, ranitidine and other H2-receptor Histamine Antagonists. In Ganellin, C.R. and Roberts, S.M. (eds). Medicinal Chemistry. The Role of Organic Chemistry in Drug Research, pp. 228-255. Academic Press, London. 

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