Quantitative versus qualitative data: The numerical dimensions of drug action

Biochemical Pharmacology

Volumn 87, Issue 1, 2014, Pages 25-39

  Bylund, David B ^a   Toews, Myron L ^a  

^a NEBRASKA MEDICAL CENTER   (United States)

Author keywords

Concentration effect; Dose response; Drug action; Efficacy; Potency

Indexed keywords

DRUG RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR; NEW DRUG; PARTIAL AGONIST;

AGONIST; ALLOSTERISM; ARTICLE; DISSOCIATION CONSTANT; DOSE RESPONSE; DRUG ANTAGONISM; DRUG CONCENTRATION; DRUG DEVELOPMENT; DRUG MECHANISM; DRUG POTENCY; MASS ACTION; MICHAELIS MENTEN KINETICS; PRIORITY JOURNAL; QUALITATIVE ANALYSIS; QUANTITATIVE ANALYSIS; REACTION TIME; RECEPTOR BINDING; RECEPTOR OCCUPANCY; SIGNAL TRANSDUCTION;

CONCENTRATION-EFFECT; DOSE-RESPONSE; DRUG ACTION; EFFICACY; POTENCY;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MODELS, CHEMICAL; PHARMACEUTICAL PREPARATIONS; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; RECEPTORS, CELL SURFACE;

EID: 84892364422     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2013.07.027     Document Type: Article

References (45)

1. T.P. Kenakin A pharmacology primer 3rd ed. 2011 Elsevier Academic Press Burlington, VT
2. K. Starke A history of Naunyn-Schmiedeberg's archives of pharmacology Naunyn Schmiedebergs Arch Pharmacol 358 1998 1 109
3. H.H. Dale The action of certain esters and ethers of choline, and their relation to muscarine J Pharmacol Exp Ther 6 1914 174 190
4. J.H. Gaddum The action of adrenalin and ergotamine on the uterus of the rabbit J Physiol 61 1926 141 150
5. J.N. Langley On the physiology of the salivary secretion J Physiol 1 1878 339 369
6. R.P. Ahlquist Comparative effects of sympathomimetic amines on the vasomotor resistance of the kidney, mesentery and leg Fed Proc 7 1948 202
7. M. Cazzola, C.P. Page, and P. Rogliani Matera MG, β2-agonist therapy in lung disease Am J Respir Crit Care Med 187 2013 690 696
8. M.A. Weber The role of the new beta-blockers in treating cardiovascular disease Am J Hypertens 18 2005 169S 176S (Pubitemid 41803605)
9. T. Kenakin Defining and characterizing drug/compound function Biochem Pharmacol 87 2014 40 63
10. J.N. Langley On the reaction of cells and of nerve-endings to certain poisons, chiefly as regards the reaction of striated muscle to nicotine and to curari J Physiol 33 1905 374 413
11. P. Ehrlich Address in pathology, on chemiotherapy: delivered before the seventeenth international congress of medicine Br Med J 2 1913 353 359
12. R. Hurst, H. Rollema, and D. Bertrand Nicotinic acetylcholine receptors: from basic science to therapeutics Pharmacol Ther 137 2013 22 54
13. R.M. Eglen Muscarinic receptor subtypes in neuronal and non-neuronal cholinergic function Auton Autacoid Pharmacol 26 2006 219 233 (Pubitemid 43898622)
14. D.B. Bylund Pharmacological characteristics of alpha-2 adrenergic receptor subtypes Ann N Y Acad Sci 763 1995 1 7
15. T.P. Kenakin New concepts in pharmacological efficacy at 7TM receptors: IUPHAR review Br J Pharmacol 168 2013 554 575
16. C.P. Mpamhanga, J.L. Sharman, and A.J. Harmar How to use the IUPHAR receptor database to navigate pharmacological data Methods Mol Biol 897 2012 15 29
17. A.J. Clark The reaction between acetyl choline and muscle cells J Physiol 61 1926 530 546
18. A.J. Clark, R. Gaddie, and C.P. Stewart The aerobic metabolism of the isolated frog's heart poisoned by iodoacetic acid J Physiol 90 1937 335 346
19. I. Langmuir The adsorption of gases on plane surfaces of glass, mica and platinum J Am Chem Soc 40 1918 1361
20. J. Fan, and I.A.M. de Lannoy Pharmacokinetics Biochem Pharmacol 2014 this volume
21. E.W. Lund Guldberg and Waage and the law of mass action J Chem Educ 42 1965 548 550
22. C.T. Dollery Intracellular drug concentrations Clin Pharmacol Ther 93 2013 263 266
23. F.L. Holmes From elective affinities to chemical equilibria: Berthollet's Law of Mass Action Chymia 8 1962 105 147
24. D. Colquhoun The quantitative analysis of drug-receptor interactions: a short history Trends Pharmacol Sci 27 2006 149 157
25. T. Kenakin, D.B. Bylund, M.L. Toews, K. Mullane, R. Winquist, and M. Williams Replicated, replicable and relevant-target engagement and pharmacological experimentation in the 21st Century Biochem Pharmacol 87 2014 40 63
26. L.E. Limbird Cell surface receptors: a short course on theory and methods 3rd ed. 2005 Springer New York, NY
27. R.P. Stephenson A modification of receptor theory Br J Pharmacol Chemother 11 1956 379 393
28. R.F. Furchgott The pharmacology of vascular smooth muscle Pharmacol Rev 7 1955 183 265
29. C.J. Langmead, and A. Christopoulos Supra-physiological efficacy at GPCRs: superstition or super agonists? Br J Pharmacol 169 2013 353 356
30. R.M. Shymko, M.P. De, and R. Thomas Logical analysis of timing-dependent receptor signalling specificity: application to the insulin receptor metabolic and mitogenic signalling pathways Biochem J 326 Pt 2 1997 463 469 (Pubitemid 27417224)
31. P.J. Tummino, and R.A. Copeland Residence time of receptor-ligand complexes and its effect on biological function Biochemistry 47 2008 5481 5492 (Pubitemid 351711169)
32. G.K. Popescu Modes of glutamate receptor gating J Physiol 590 2012 73 91
33. J. Tremblay, R. Desjardins, D. Hum, J. Gutkowska, and P. Hamet Biochemistry and physiology of the natriuretic peptide receptor guanylyl cyclases Mol Cell Biochem 230 2002 31 47 (Pubitemid 34257240)
34. E.J. Ariens Affinity intrinsic activity in the theory of competitive inhibition. I. Problems and theory Arch Int Pharmacodyn Ther 99 1954 32 49
35. T. Kenakin, S. Jenkinson, and C. Watson Determining the potency and molecular mechanism of action of insurmountable antagonists J Pharmacol Exp Ther 319 2006 710 723
36. R.A. Bond, and A.P. Ijzerman Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery Trends Pharmacol Sci 27 2006 92 96 (Pubitemid 43184030)
37. T. Kenakin G protein coupled receptors as allosteric proteins and the role of allosteric modulators J Recept Signal Transduct Res 30 2010 313 321
38. A.C. Foster, and J.A. Kemp Glutamate- and GABA-based CNS therapeutics Curr Opin Pharmacol 6 2006 7 17 (Pubitemid 43103814)
39. W. Froestl An historical perspective on GABAergic drugs Future Med Chem 3 2011 163 175
40. M. Nickerson Receptor occupancy and tissue response Nature 178 1956 697 698
41. B.T. Zhu The competitive and noncompetitive antagonism of receptor-mediated drug actions in the presence of spare receptors J Pharmacol Toxicol Methods 29 1993 85 91
42. H.O. Schild pA, a new scale for the measurement of drug antagonism Br J Pharmacol Chemother 2 1947 189 206
43. H.O. Schild Drug antagonism and pAx Pharmacol Rev 9 1957 242 246
44. J.H. Gaddum The quantitative effect of antagonist drugs J Physiol (Lond) 89 1937 7P 9P
45. J.H. Gaddum Theories of drug antagonism Pharmacol Rev 9 1957 211 218