The RBI Handbook of Receptor Classification and ... - ACS Publications

Biochemicals International, Natick, MA. 1995. vii +. 196 pp. 22.5 × 27.5cm. ISBN0-96405548-1-7. $35.00. When I reviewed the first edition of The RBI ...
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J. Med. Chem. 1996, 39, 2277-2279

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Book Reviews The RBI Handbook of Receptor Classification and Signal Transduction. Edited by Keith J. Watling, John W. Kebabian, and John L. Neumeyer. Research Biochemicals International, Natick, MA. 1995. vii + 196 pp. 22.5 × 27.5 cm. ISBN 0-96405548-1-7. $35.00. When I reviewed the first edition of The RBI Handbook of Receptor Classification, I commented, “I found the handbook to be a wonderful consolidation of information...useful to anyone working in the field of receptor biology.” With the second edition, there is absolutely no reason to change my thoughts. As noted in the revised title, the handbook is now expanded to include signal transduction pathways. In fact, the reference also contains valuable descriptions of the synthetic and metabolic pathways for different neurotransmitters (acetylcholine, dopamine, norepinephrine, GABA, glutamate, histamine, and serotonin). The number of chapters has increased from 35 to 67, and the handbook now incorporates discussions of cyclic nucleotide phosphodiesterases, cytokines, G-proteins, intracellular receptors, peptidases, phospholipases, prenyltransferases, and kinases (serine, threonine, and tyrosine) as well as a host of neurotransmitter receptors not addressed in the first edition. Each of the 35 chapters in the original handbook are retained, and in some cases (e.g., GABA), these have been further subdivided to reflect rapid advances in the field. All of the chapters are updated to reflect new “gold standards”. Likewise, the product listings from RBI, New England Nuclear, and Amersham are current, and in one instance, I located a radioligand not identified in the vendors catalog sitting in my office. The utility of the handbook and the enthusiasm with which the first edition was received are reflected by the willingness of new authors to contribute to the second edition; the list of contributors now numbers 113 (up from 37). As was the case before, each of these is a leader in some portion of receptor pharmacology. Chapters continue to provide explanatory footnotes as needed and are accompanied by complete and current references. It is without question that The RBI Handbook of Recetor Classification and Signal Transduction will be of value to anyone working in the field of receptor biology. Because of its expanded subject matter, this now includes scientists other than neuropharmacologists. The handbook has already disappeared from my office on several occasions; at $35.00, I have urged my colleagues to purchase their own. John Wm. Ferkany OREAD BioSafety Center Division of Pharmacology Farmington, Connecticut 06032 JM960107Q S0022-2623(96)00107-0

Benzodiazepine Receptor Inverse Agonists. Edited by M. Starter, D. J. Nutt, and R. G. Lister. WileyLiss, Inc., New York. 1995. x + 304 pp. 16 × 23.5 cm. ISBN 0-471-56173-8. $75.00. This book is, as the editors point out in the preface, written for the sole purpose of reviewing the status of the pharmacology of benzodiazepine receptor (BZR) inverse agonists. For those whose interests lie within the field of BZR inverse agonist research but are only indirectly involved in the pharmacological aspects, this book suffers from the same general shortcoming common to other pharmacological treatises. Compounds are referred to only by the numbers given to them by pharmaceutical companies (often unreferenced) and never by structural formula. For anyone interested in correlating structural features with differences in pharmacological activities, it makes for rather difficult reading. In general the individual chapters are informative, well written, and readable. The excellent practice of including a summary at the end of each chapter will be invaluable to the reader. There are 11 individual chapters, of which the first four cover such topics as subpopulations of receptors, interactions with other transmitter systems, sensitization and tolerance after chronic treatment, and an attempt to derive a new model for ligand-receptor binding for inverse agonists. The next six chapters deal with different aspects of pharmacology, within the range of activities exhibited by the BZR inverse agonists. The final chapter discusses the potential for utility of these agents as therapeutic drugs. The first chapter gives an excellent summary of work carried out on subpopulations of BZRs. It would have been enhanced had it been followed by a discussion of recent biochemical assays using a variety of cloned receptors. Such techniques might be of value in classifying the different types of BZR, since some of the terms used in the chapter of human pharmacology, e.g., “weak inverse agonists” or “antagonist with weak inverse agonist properties” and “more inverse than flumazenil”, make evaluation of data by the reader somewhat difficult. This is especially true when Haefly, in his classification, pointed out that antagonists reverse the effects of both agonists and inverse agonists. The fact that most ligands for the BZR are probably either partial agonists or partial inverse agonists makes clearcut definitions almost impossible. Reading through the various chapters, one is consistently impressed by the authors concern over the difficulties in establishing reliable testing paradigms for these compounds. Again, this may be more due to the individual spectrum of activity for each compound rather than to the testing procedure. It is clear that much has yet to be done, both by the medicinal chemist and by the pharmacologist, in order to separate the broad spectrum of biological activities

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Book Reviews

for the inverse agonist ligands into compounds with specific properties that would make therapeutic agents.

product, all available strengths, forms, and package sizes, its national drug code number, and its average wholesale price. Drugs are indexed by brand and generic name, therapeutic category, and specific indications. A visual drug identification section, organized by generic name and providing actual size color photographs of different generic products, is also provided. Other features include a directory of poison control centers, a directory of drug information centers, a directory of pharmaceutical manufacturers, a table of drugs by FDA Pregnancy Category, a summary of new molecular entities approved by the FDA in 1994, and adverse reaction reporting forms. All in the healthcare community will benefit from PDR Generics. Some will want to use it in conjunction with the classic Physicians’ Desk Reference, whereas others may find either of these monumental and complete sources of drug product information more appropriate for their needs.

R. Ian Fryer Department of Chemistry Rutgers, The State University of New Jersey Newark, New Jersey 07102 JM960109A S0022-2623(96)00109-4

Physicians’ Desk Reference. 50th Edition. Medical Consultant: Ronald Arky. Medical Economics Co., Montvale, NJ. 1996. vi + 2879 pp. 23 × 28 cm. ISBN 1-56363-152-0. $69.95. This is the golden anniversary edition of the Physicians’ Desk Reference (PDR). As usual, the 1996 PDR provides vital information about all FDA-approved prescription drugs. It is the largest annual medical reference in the United States. Complete, FDA-approved prescribing information with an exact copy of the product’s FDA-approved labeling and the latest available information are provided for more than 2500 specific pharmaceutical products, including over 200 completely new listings. The PDR is the most extensive single-volume prescription drug reference currently available. It provides actual size color pictures of the most widely prescribed drugs. Complete brand and generic name, manufacturer, and therapeutic/pharmacologic category indexes provide convenient ways in which to readily access drug information. The PDR is used by almost every physician and healthcare facility in the United States. A desk copy or convenient access to this prescription drug standard will benefit all concerned with pharmaceuticals, from researchers and administrators to all others in the healthcare community. Access to PDR information has now been enhanced by introduction of a new Windowscompatible disc, PDR Electronic Library, on CD-ROM. Staff JM960110+ S0022-2623(96)00110-0

PDR Generics. 1995. First Edition. Medical Consultant: Ronald Arky. Medical Economics Data Production Co., Montvale, NJ. 1995. cxx + 2991 pp. 23 × 28 cm. ISBN 1-56363-118-0. $69.95. PDR Generics serves as a companion volume to the classic Physicians’ Desk Reference. Like the Physicians’ Desk Reference, PDR Generics includes FDA-approved prescribing information. This information is augmented with comparative cost and supplementary prescribing information that has become increasingly important with the advent of the extensive use of generic drugs. This is a comprehensive compendium of almost all single-source and multisource prescription drugs in current use with information on nearly 24 000 products. The drug products are organized alphabetically by generic name. Each monograph lists all suppliers of the

Staff JM9601112 S0022-2623(96)00111-2

Reviews in Computational Chemistry. Volume 6. Edited by Kenny B. Lipkowitz and Donald B. Boyd. VCH Publishers, Inc., New York. 1995. xix + 480 pp. 16 × 24 cm. ISBN 1-56081-667-8. $90.00. This is the sixth volume in this series reviewing a wide range of topics of current interest in computational chemistry. As in the previous volumes in this series, the contributors have provided thorough coverage of background material, classical studies, and up to date work in their area. In addition, the book includes several useful features, such as e-mail addresses of the present contributors, a list of past contributors and titles, and extensive subject and author indexes. The first chapter discusses continuum solvation models, an area of intense research over the past 10 years and one of great importance in treating biological systems. The next two chapters move away from the typical realm of computational organic chemistry and deal with force fields for modeling inorganic and organometallic compounds and computational modeling aspects of polymers. Chapter 4, an extensive treatment of the computational methods and types of computers used in computational chemistry, is especially useful for those interested in programming techniques and computer hardware. This chapter also contains a helpful glossary of terminology used in computer science and an appendix providing a survey of parallel computing hardware and its use in several computational chemistry packages. Chapter 5 is a novel and interesting look at trends in the computational chemistry and molecular modeling literature over the past 15 years. A main focus of this chapter is investigating the utility of computational chemistry software, as judged by analyzing the large volume of publications in this area. This volume also contains an appendix of published force field parameters, including a large number of references. The book

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closes, as in previous volumes, with a large and updated list of computational chemistry programs and vendors. The chapters are well-written and nicely presented, and each contains a good number of appropriate and timely references. This volume, and the series in whole, is an excellent source of background information as well as of current research studies in computational chemistry.

The emphasis throughout the chapter examples is on the stereoselective synthesis of relatively small molecules. A valuable feature of the text discussion is the analyses of the various factors, such as molecular conformation and the interplay between steric and electronic effects, which give rise to asymmetric induction. A great deal of useful information from the literature is distilled and organized herein, with extensive use of three-dimensional representations for transition states and intermediates. Unfortunately, many of these structure drawings are not as clear as one would hope; the quality of the graphics is reminescent of 1980sera publications. Very few of the drawings successfully impart a three-dimensional view of the process being depicted. In addition, some material is given short shrift. Surely one of the most important breakthroughs in absolute asymmetric synthesis of the past several years is Jacobsen’s method for the oxidation of olefins which does not require the presence of allylic directing groups. This work is only mentioned briefly in a couple of sentences. Despite these shortcomings, the book does successfully organize and analyze a wealth of information regarding asymmetric transformations from a mechanistic and physical organic perspective. At a cost of $0.11/page, most practicing synthetic chemists will find it a cost-effective addition to their laboratory bookshelves.

Mark G. Bures Abbott Laboratories 100 Abbott Park Road D47E AP10 Abbott Park, Illinois 60064-3500 JM960112U S0022-2623(96)00112-4

Stereoselective Synthesis. Robert S. Atkinson. John Wiley and Sons Ltd., Chichester, England. 1995. xii + 529 pp. 15 × 23 cm. ISBN 0-471-95419-5. $59.95 (pbk). This book begins auspiciously with an extensive discussion of stereochemical nomenclature, an area of long-standing confusion. The first chapter details the use of stereochemical vocabulary in accordance with IUPAC rules with concrete examples. The following chapter presents the author’s own system for categorizing stereoselective reactions based on the number of chiral centers created in the product as compared to the number present in the starting material. This system is used as an organizational template throughout the following chapters to systematically discuss the various types of stereoselective synthetic methods.

Gregory S. Hamilton Guilford Pharmaceuticals, Inc. Baltimore, Maryland 21224 JM960113M S0022-2623(96)00113-6