H. Timmerman – författare

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.

Taxol®, a naturally occurring diterpenoid is one of the most exciting antitumor drugs available today. Its current indications (refractory ovarian and metastatic breast cancer) may soon be expanded since the drug is showing activity against lung and head-and-neck cancers.The book opens with a review of the naturally occurring taxoids, a chapter which is not a comprehensive list of all taxoids isolated to date, but attempts a systematic approact to describing the different classes of taxoids, with particular reference to all skeletal types and the various functionality patterns. Biosynthetic studies are also discussed, as well as some of the basic chemistry and common functionalities of taxoidic skeleton. Structural identification of taxoids, mostly by spectroscopic means; the formulation of taxanes; the metabolism and pharmacokinetics of Taxol® are also discussed, as are the chemistry of taxanes in relation to SAR studies; SAR aspects of the phenylisoserine side chain; and the mode of action of the taxanes and the mechanisms of resistance.The book is therefore written for medical chemists, in order to stimulate further research in this area and to provide the reader with the necessary background information to start a research program in the area.

Based on topics presented at the Annual Japanese (Quantitative) Structure-Activity Relationship Symposium and the Biennial China-Japan Drug Design and Development conference, the topics in this volume cover almost every procedure and subdiscipline in the SAR discipline.They are categorized in three sections. Section one includes topics illustrating newer methodologies relating to ligand-receptor, molecular graphics and receptor modelling as well as the three-dimensional (Q)SAR examples with the active analogue approach and the comparative molecular field analysis. In section 2 the hydrophobicity parameters, log P (1-octanol/water) for compound series of medicinal-chemical interest are analysed physico-organic chemically. Section 3 contains the examples based on the traditional Hansch QSAR approach.A variety of methodologies and procedures are presented in this single volume, along with their methodological philosophies.

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.

Pharmacochemistry Library, Volume 19: Small Peptides: Chemistry, Biology, and Clinical Studies focuses on the processes, reactions, properties, and characteristics of peptides, including analogues and proteases. The publication first takes a look at angiotensin II and bombesin/gastrin-releasing peptide. Topics include conformationally restricted analogues of bombesin, non-peptide antagonists of angiotensin II, receptor subtypes of angiotensin II, and bombesin/GRP antagonists and cancer. The text then elaborates on bradykinin, cholecystokinin, and enkephalin analogues. The manuscript examines luteinizing hormone releasing hormone and somatostatin. Topics include enzymic degradation of somatostatin and analogues, clinical applications of somatostatin analogues, and pharmacological and clinical studies with LHRH agonists and antagonists. The formulation of peptides and inhibitors of aspartyl proteases are also mentioned. The book is a valuable source of information for chemists, biologists, and readers interested in small peptides.

Volume 45 of "Progress in Drug Research" contains eight reviews and the various indexes which facilitate its use and establish the connection with the previous volumes. The articles in this volume deal with neuro­ peptides as native immune modulators, with Calmodulin and with effects of cell stimuli and drugs on cellular activation, with recent advances in benzodiazepine receptor binding studies, with the medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor, with Serotonin uptake inhibitors, with computer-aided drug design, with natri­ uretic hormones and with the recent developments in the chemotherapy of osteoporosis. In the 36 years that PDR has existed, the Editor has enjoyed the valu­ able help and advice of many colleagues. Readers, the authors of the reviews and, last but not least, the reviewers have all contributed greatly to the success of this series. Although the comments received so far have generally been favorable, it is nevertheless necessary to analyze and to reassess the current position and the future direction of such a series of monographs. So far, it has been the Editor''s intention to help disseminate information on the vast domain of drug research, and to provide the reader with a tool with which to keep abreast of the latest developments and trends. The reviews in PDR are useful to the nonspecialist, who can obtain an overview of a particular field of drug research in a relatively short time.