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Pharmacologic analysis of drug-receptor interaction
ELSEVIER
Toxicology
93 (1994)
301-302
Book review Pharmacologic Analysis of Drug-Receptor Interaction.
Second Edition. Terry Kenakin, Pages: 495, Raven Press, New York, 1993. Price: US $113.50. ISBN O-7817-0065-5 It always was and still is the ultimate fuhilment for every pharmacologist to find a specific receptor for ‘his’ drug or autacoid. Therefore it is no wonder that receptorology has found so much attention practically since the first formulation of the receptor concept by Paul Ehrlich early this century; it is no coincidence that the author of this book has chosen Paul Ehrlich’s one line description of a receptive as the motto for the first chapter of this book. All other chapters are headed by similarly thoughtful mottoes which season the sometimes difficult and very professional reading matter. Also it is interesting to observe the shift in the meaning of the term ‘key’: originally a receptor-fitting drug was compared with a key that perfectly fits the corresponding lock, but now the term is used to indicate important drugs or groups of drugs that play a ‘key’ role in the intellectual development of our understanding of drug actions and their therapeutic importance. The book is divided into fourteen chapters starting with the drug-receptor theory leading to considerations on stimulus-response mechanisms and response systems, thereby not dwelling too much on intracellular secondary signalling systems. The succeeding chapters are devoted, in addition to diffusion, to considerations about necessary drug concentrations in the receptor compartment, analysis of dose response data and efficacy. The important question of the possible relation between agonist affinity and receptor efficiency are carefully treated. Of course, in a book of this depth and calibre the treatment of the various types of receptor antagonisms is not omitted. Similarly there are chapters on receptor classification, kinetics of drug action, drug design and discovery and also on receptor binding experiments. However, on the whole the character of the book is designed to introduce the reader to the theoretical and intellectual background of receptorology, mostly expressed in mathematical terms. It is not a ‘cookbook’ for those who want to carry out receptor experiments in the laboratory. There is no information for experimentally oriented readers on respective sources of practical advice. The book is a dignified follower of the previous classics by A.J. Clark and E.J. Ariens, the latter of whom is cited with the following motto on the chapter on eflicacy: ‘The distinction between affinity and intrinsic activity therefore seems of general importance’. Other thoughtfully selected classical remarks introducing the various 0300-483x/94/.$07.00 0 1994 SSDI 0300-483X(94)02814-B
Elsevier Science Ireland
Ltd. All rights reserved
302
Book review / Toxicology 93 (1994) 301-302
chapters are the following: ‘The equilibrium dissociation constant defines the signalto-noise ratio in the chemical cacophony which surmount every cell’ (Sir James Black, 1982); ‘If your experiment needs statistics, you ought to have done a better experiment’ (Lord Ernest Rutherford, 1871-1937); ‘Although this may seem a paradox, all exact science is dominated by the idea of approximation’ (Bertrand Russell, 1872-1970). And finally the classic statement by Paul Ehrlich in 1913: ‘Corpora nonagunt nisi fixata’. The book gives its reader easy access to the enormous wealth in current knowledge about receptors, as exemplified by examples from the literature and digested and expressed by the use of proper mathematics. Each chapter is fortified by the necessary literature references. The printing and the illustrations are well done but by no means luxuriously. On the whole, the volume contains paradigmatically our current theoretical tools for understanding receptorology and hence will be advantageously used by a probably select but nevertheless broad readership of pharmacologists, drug developers, toxicologists, biophysicists, physiologists and students of these and possibly other disciplines. The author is to be congratulated on his achievement. The book should be seen in conjunction with the forthcoming publication of the Receptor Nomenclature and Drug Classification Committee of the International Union of Pharmacology (IUPHAR). K.J. Netter
Toxicology
93 (1994)
301-302
Book review Pharmacologic Analysis of Drug-Receptor Interaction.
Second Edition. Terry Kenakin, Pages: 495, Raven Press, New York, 1993. Price: US $113.50. ISBN O-7817-0065-5 It always was and still is the ultimate fuhilment for every pharmacologist to find a specific receptor for ‘his’ drug or autacoid. Therefore it is no wonder that receptorology has found so much attention practically since the first formulation of the receptor concept by Paul Ehrlich early this century; it is no coincidence that the author of this book has chosen Paul Ehrlich’s one line description of a receptive as the motto for the first chapter of this book. All other chapters are headed by similarly thoughtful mottoes which season the sometimes difficult and very professional reading matter. Also it is interesting to observe the shift in the meaning of the term ‘key’: originally a receptor-fitting drug was compared with a key that perfectly fits the corresponding lock, but now the term is used to indicate important drugs or groups of drugs that play a ‘key’ role in the intellectual development of our understanding of drug actions and their therapeutic importance. The book is divided into fourteen chapters starting with the drug-receptor theory leading to considerations on stimulus-response mechanisms and response systems, thereby not dwelling too much on intracellular secondary signalling systems. The succeeding chapters are devoted, in addition to diffusion, to considerations about necessary drug concentrations in the receptor compartment, analysis of dose response data and efficacy. The important question of the possible relation between agonist affinity and receptor efficiency are carefully treated. Of course, in a book of this depth and calibre the treatment of the various types of receptor antagonisms is not omitted. Similarly there are chapters on receptor classification, kinetics of drug action, drug design and discovery and also on receptor binding experiments. However, on the whole the character of the book is designed to introduce the reader to the theoretical and intellectual background of receptorology, mostly expressed in mathematical terms. It is not a ‘cookbook’ for those who want to carry out receptor experiments in the laboratory. There is no information for experimentally oriented readers on respective sources of practical advice. The book is a dignified follower of the previous classics by A.J. Clark and E.J. Ariens, the latter of whom is cited with the following motto on the chapter on eflicacy: ‘The distinction between affinity and intrinsic activity therefore seems of general importance’. Other thoughtfully selected classical remarks introducing the various 0300-483x/94/.$07.00 0 1994 SSDI 0300-483X(94)02814-B
Elsevier Science Ireland
Ltd. All rights reserved
302
Book review / Toxicology 93 (1994) 301-302
chapters are the following: ‘The equilibrium dissociation constant defines the signalto-noise ratio in the chemical cacophony which surmount every cell’ (Sir James Black, 1982); ‘If your experiment needs statistics, you ought to have done a better experiment’ (Lord Ernest Rutherford, 1871-1937); ‘Although this may seem a paradox, all exact science is dominated by the idea of approximation’ (Bertrand Russell, 1872-1970). And finally the classic statement by Paul Ehrlich in 1913: ‘Corpora nonagunt nisi fixata’. The book gives its reader easy access to the enormous wealth in current knowledge about receptors, as exemplified by examples from the literature and digested and expressed by the use of proper mathematics. Each chapter is fortified by the necessary literature references. The printing and the illustrations are well done but by no means luxuriously. On the whole, the volume contains paradigmatically our current theoretical tools for understanding receptorology and hence will be advantageously used by a probably select but nevertheless broad readership of pharmacologists, drug developers, toxicologists, biophysicists, physiologists and students of these and possibly other disciplines. The author is to be congratulated on his achievement. The book should be seen in conjunction with the forthcoming publication of the Receptor Nomenclature and Drug Classification Committee of the International Union of Pharmacology (IUPHAR). K.J. Netter