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Structural Requirements for Histamine H2 Agonists and H2 Antagonists

  • Chapter
Histamine and Histamine Antagonists

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 97))

Abstract

This chapter reviews the structural requirements for H2 agonists and antagonists. Section B discusses the agonists, which are divided into three classes: the non-selective histamine analogues, showing H2 activity as well as H1 and H3 activity; dimaprit, a selective, but moderately active agonist which allows no substitution without a dramatic fall in activity; and, thirdly, the impromidine-related compounds including very potent H2 agonists, some of which also show Η1 antagonism and some are rather potent H3 antagonists as well. Section C reviews more than 1000 different H2 antagonists; these compounds belong to rather different classes of compounds. It is therefore clear that the structural requirements for H2 antagonism are much less restrictive than might have been originally thought. Finally, in Section D the structural requirements for interference with the P-450 enzyme(s) are summarized. The inhibitory effects of H2 antagonists on the P-450-mediated metabolic pathways are probably the cause of the major side effects of some H2 antagonists. This interaction may lead to a less extensive metabolism of certain other drugs, given together with H2 antagonists interfering with P-450. As was to be expected, it has been found that this inhibitory effect is related neither to the potency of these H2 antagonists nor to the general structural features which determine affinity for the H2 receptors.

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Authors
  1. H. van der Goot
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  2. A. Bast
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  3. H. Timmerman
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  1. Department of Pharmacology, Karolinska Institutet, Box 60400, S-104 01, Stockholm, Sweden

    Börje Uvnäs M.D.

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van der Goot, H., Bast, A., Timmerman, H. (1991). Structural Requirements for Histamine H2 Agonists and H2 Antagonists. In: Uvnäs, B. (eds) Histamine and Histamine Antagonists. Handbook of Experimental Pharmacology, vol 97. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-75840-9_27

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