In the early eighties when the H3 receptor was identified, many
thought that an H3 ligand, an agonist or an antagonist, would
become available as a therapeutic agent. This has not occurred. The
reason for this could be the fact that many investigators consider
histamine mainly, if not only, as a mediator present in for example
mast cells being released during allergic events. However, it has
become apparent that histamine is an important neurotransmitter.
Its role in the nervous system, especially in the central part of
it, is rather extensive.
The H3 receptor is mainly found as a presynaptic one, both on
histaminergic neurons (the auto-type) and on other neuronal systems
(the hetero-type). Both the H3 agonist and the H3 antagonist cause
important pharmacological effects. Several ligands have become
available now, including radiolabelled analogues.
In this book, the current state of affairs with regards to the
medicinal chemistry and pharmacology of the H3 receptor and the
several ligands available are presented by a number of experts in
the field. The book presents an extended review of what has
happened since the first H3 paper appeared. The editors hope that
publication of this work will lead to an increase in interest of
both academia and industry for the H3 receptor, especially as a
target for drug development.
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