The Histamine H Receptor: A Target for New Drugs

✍ Scribed by Rob Leurs and Henk Timmerman (Eds.)

Publisher: Elsevier, Academic Press
Year: 1998
Tongue: English
Leaves: 304
Series: Pharmacochemistry Library 30
Edition: 1st
Category: Library

No coin nor oath required. For personal study only.

✦ Synopsis

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.

✦ Table of Contents

Content:
Editorial Board
Page v

Preface
Page ix
H. Timmerman, R. Leurs

Subclassification of histamine receports, H₃-receptor subtypes? Localization of H₃ receptors in the brain Original Research Article
Pages 1-12
J-M. Arrang, S. Morisset, C. Pillot, J-C. Schwartz

Modulation of in vitro neurotransmission in the CNS and in the retina via H₃ heteroreceptors Original Research Article
Pages 13-26
E. Schlicker, M. Kathmann

H₃ receptor modulation of the release of neurotransmitters in vivo Original Research Article
Pages 27-40
P. Blandina, L. Bacciottini, M.G. Giovannini, P.F. Mannaioni

H3 receptor modulation of neuroendocrine responses to histamine and stress Original Research Article
Pages 41-58
Ulrich Knigge, Andreas Kj˦r, Henrik Jørgensen, Jørgen Warberg

Functional role of histamine H₃ receptors in peripheral tissues Original Research Article
Pages 59-111
G. Bertaccini, G. Coruzzi, E. Poli

Biochemical properties of the histamine H₃ receptor Original Research Article
Pages 113-126
Marcel Hoffmann, Henk Timmermann, Rob Leurs

Radioligands for the histamine H₃ receptor and their use in pharmacology Original Research Article
Pages 127-144
F.P. Jansen, R. Leurs, H. Timmerman

Substituted imidazoles, the key to histaminergic receptors Original Research Article
Pages 145-158
W.M.P.B. Menge, H. Timmerman

Synthesis of radioligands for the histamine H₃ receptor Original Research Article
Pages 159-174
Albert D. Windhorst, Rob Leurs, Wiro M.P.B. Menge, Henk Timmerman, Jacobus D.M. Herscheid

Medicinal chemistry of histamine H₃ receptor agonists Original Research Article
Pages 175-196
M. Krause, H. Stark, W. Schunack

Medicinal chemistry of histamine H3 receptor antagonists Original Research Article
Pages 197-222
James G. Phillips, Syed M. Ali

Molecular modelling studies of histamine H₃ receptor ligands Original Research Article
Pages 223-241
Iwan J.P. De Esch, Paul H.J. Nederkoorn, Henk Timmerman

Brain histamine in pathophysiological conditions and brain diseases Original Research Article
Pages 243-253
P. Panula, T. Sallmen, O. Anichtchik, K. Kuokkanen, M. Lintunen, J.O. Rinne, M. Mättö, J. Kaslin, K.S. Eriksson, K. Karlstedt

Histamine H₃ antagonists as potential therapeutics in the CNS Original Research Article
Pages 255-267
Kenji Onodera, Takehiko Watanabe

Clinical application of HA H₃ receptor antagonists in learning and memory disorders Original Research Article
Pages 269-286
C.E. Tedford

Author index
Page 287

Subject index
Pages 289-291

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