Leurs / Timmerman The Histamine H3 Receptor

A Target for New Drugs
1. Auflage 1998
ISBN: 978-0-08-053400-8
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 290 Seiten, Web PDF

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.

Autoren/Hrsg.

Leurs, R.

Timmerman, H.

Inhaltsverzeichnis

1;Cover;1
2;Contents;12
3;Preface;10
4;Chapter 1. Subclassification of histamine receptors, H3-receptor subtypes? Localization of H3 receptors in the brain;14
5;Chapter 2. Modulation of in vitro neurotransmission in the CNS and in the retina via H3 heteroreceptors;26
6;Chapter 3. H3 receptor modulation of the release of neurotransmitters in vivo;40
7;Chapter 4. H3 receptor modulation of neuroendocrine responses to histamine and stress;54
8;Chapter 5. Functional role of histamine H3 receptors in peripheral tissues;72
9;Chapter 6. Biochemical properties of the histamine H3 receptor;126
10;Chapter 7. Radioligands for the histamine H3 receptor and their use in pharmacology;140
11;Chapter 8. Substituted imidazoles, the key to histaminergic receptors;158
12;Chapter 9. Synthesis of radioligands for the histamine H3 receptor;172
13;Chapter 10. Medicinal chemistry of histamine H3 receptor agonists;188
14;Chapter 11. Medicinal chemistry of histamine H3 receptor antagonists;210
15;Chapter 12. Molecular modelling studies of histamine H3 receptor ligands;236
16;Chapter 13. Brain histamine in pathophysiological conditions and brain diseases;256
17;Chapter 14. Histamine H3 antagonists as potential therapeutics in the CNS;268
18;Chapter 15. Clinical application of HA H3 receptor antagonists in learning and memory disorders;282
19;Author index;300
20;Subject index;302