The Pharmacology of Functional, Biochemical, and Recombinant Receptor SystemsT. Kenakin, J. A. Angus Springer Science & Business Media, 06.12.2012 - 448 Seiten This, the 148th volume of the Handbook of Experimental Pharmacology series, focuses on the very core of pharmacology, namely receptor theory. It is fitting that the originator of receptor pharmacology, A. J. CLARK, authored the fourth volume of this series 63 years ago. In that volume CLARK further developed his version of receptor theory first described four years earlier in his classic book The Mode of Action of Drugs. An examination of the topics covered in volume 4 reveals a striking similarity to the topics covered in this present volume; pharmacologists today are still as interested in unlocking the secrets of dose-response relationships to reveal the biological and che mical basis of drug action as they were over half a century ago. Sections in that 1937 volume such as "Curves relating exposure to drugs with biological effects" and "Implications of monomolecular theory" show Clark's keen insight into the essential questions that required answers to move pharma cology forward. With the advent of molecular biological cloning of human receptors has come a transformation of receptor pharmacology. Thus the expression of human receptors into surrogate host cells helped unlock secrets of receptor mechanisms and stimulus-transduction pathways. To a large extent, this elim inates the leap of faith required to apply receptor activity of drugs tested on animal receptor systems to the human therapeutic arena. However, a new leap of faith concerning the veracity of the effects found in recombinant systems with respect to natural ones is now required. |
Inhalt
1 | |
Pharmacodynamic Analyses | 15 |
Vascular Reactivity in Human Primary Hypertension | 28 |
Pharmacology of Vascular Conduits for CoronaryBypass | 37 |
References | 47 |
CHAPTER 2 | 50 |
Reconciliation | 59 |
H Adenylate Cyclase and αAdrenoceptors | 66 |
Biological Definitions of Efficacy | 221 |
Molecular Definitions of Efficacy | 227 |
E A Stochastic Model of Molecular Efficacy | 238 |
References | 254 |
CHAPTER 9 | 261 |
B CoAgonism | 267 |
General Observations | 279 |
Light as the Ligand | 287 |
R University of Texas South Western Medical School | 69 |
CHAPTER 3 | 73 |
Is There a Functional role for Cardiac ẞAdrenoceptors? | 80 |
F 5HT4 Receptors | 90 |
G CrossTalk Between Cardiac GCoupled Receptors | 95 |
H Physiological Pathophysiological and Therapeutic Relevance | 101 |
Epilogue | 107 |
New Theoretical Concepts and Molecular Mechanisms | 117 |
Parameters Contributing to Ligand Efficacy | 126 |
Concluding Remarks | 143 |
TwoState Theory | 149 |
F General Application of the Cubic Model | 155 |
G Conclusion | 163 |
Mutations and Diseases of Spontaneous Receptor Activity | 173 |
CHAPTER 7 | 183 |
E Limitations of Agonist Potency Ratios | 201 |
H Conclusions | 215 |
Peptides as Ligands | 298 |
Concluding Remarks | 302 |
CHAPTER 11 | 311 |
Perspective | 328 |
CHAPTER 12 | 335 |
E Conclusions | 356 |
CHAPTER 13 | 363 |
G Proteincoupled Receptors | 370 |
Gα | 376 |
F Conclusions | 383 |
CHAPTER 14 | 390 |
B Use of Reporter Gene Systems in Pharmacology | 401 |
412 | |
Melanophore Recombinant Receptor Systems | 415 |
Lawn Format | 428 |
435 | |
Andere Ausgaben - Alle anzeigen
The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems Terrence P. Kenakin,James A. Angus Eingeschränkte Leseprobe - 2000 |
The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems T Kenakin,J A Angus Keine Leseprobe verfügbar - 2000 |
The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems T. Kenakin,J. A. Angus Keine Leseprobe verfügbar - 2012 |
Häufige Begriffe und Wortgruppen
5-HT receptors Acad Sci USA acetylcholine adenylate adenylyl cyclase adrenoceptor aequorin affinity agonism allosteric ANGUS antagonism antagonist assay atrial B₁ basal Biochem Biol Chem Ca2+ calcium cardiac cell lines cellular channels cloning concentration conformational constitutive activity coronary arteries curves dissociation drug effector effects endogenous equilibrium expression factor function G protein G protein-coupled receptors glycine GPCRs heart human atrium hypertension increase inhibition inotropic insect cells interaction intracellular inverse agonists isoproterenol KAUMANN kinase Lefkowitz RJ levels ligand mammalian maximal response measured mediated melanophores membrane Mol Pharmacol molecular molecules muscarinic mutations myogenic noradrenaline overexpression parameters partial agonists pathways patients peptide pertussis toxin pharmacology phosphorylation pithed rat potency protein activation protein-coupled receptors recep receptor activation receptor and G recombinant regulation relative relaxation reporter gene rhodopsin selective Sf9 cells signal transduction smooth muscle ẞ₁ stimulation stimulus-response studies subtypes subunits ternary complex model tion tissue transfected vascular