Principles: receptor theory in pharmacology.

[1]  D. Lewis,et al.  The CB1 Cannabinoid Receptor Can Sequester G-Proteins, Making Them Unavailable to Couple to Other Receptors , 1999, The Journal of Neuroscience.

[2]  K. Blumer,et al.  Mechanisms governing the activation and trafficking of yeast G protein-coupled receptors. , 1998, Molecular biology of the cell.

[3]  Terry Kenakin,et al.  A guide to drug discovery: Predicting therapeutic value in the lead optimization phase of drug discovery , 2003, Nature Reviews Drug Discovery.

[4]  Terry Kenakin,et al.  Efficacy at g-protein-coupled receptors , 2002, Nature Reviews Drug Discovery.

[5]  H. Schild Drug antagonism and pAx. , 1957, Pharmacological reviews.

[6]  A. Trkola,et al.  Co-receptors for HIV-1 entry. , 1997, Current opinion in immunology.

[7]  R. Furchgott The Classification of Adrenoceptors (Adrenergic Receptors). An Evaluation from the Standpoint of Receptor Theory , 1972 .

[8]  R. Lefkowitz,et al.  A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. , 1980, The Journal of biological chemistry.

[9]  A. J. Clark The Rate of Action of Drugs on Cells , 1937 .

[10]  T. Hall The limitations of molecular pharmacology. , 1971, The Journal of clinical pharmacology and new drugs.

[11]  J. Blanck,et al.  Kinetics of Drug Action , 1977, Handbuch der experimentellen Pharmakologie / Handbook of Experimental Pharmacology.

[12]  S. Rees,et al.  GPCR drug discovery through the exploitation of allosteric drug binding sites. , 2002, Receptors & channels.

[13]  R. Lefkowitz,et al.  Agonist-induced increase in apparent β-adrenergic receptor size , 1978 .

[14]  C. Shayo,et al.  Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model. , 2003, Molecular pharmacology.

[15]  T. Kenakin Efficacy as a vector: the relative prevalence and paucity of inverse agonism. , 2004, Molecular pharmacology.

[16]  L. Bačáková,et al.  Activation of muscarinic acetylcholine receptors via their allosteric binding sites. , 1996, Proceedings of the National Academy of Sciences of the United States of America.

[17]  Terry Kenakin,et al.  Drug efficacy at G protein-coupled receptors. , 2002, Annual review of pharmacology and toxicology.

[18]  T. Gardella,et al.  Amino-terminal modifications of human parathyroid hormone (PTH) selectively alter phospholipase C signaling via the type 1 PTH receptor: implications for design of signal-specific PTH ligands. , 1999, Biochemistry.

[19]  W. Paton,et al.  A theory of drug action based on the rate of drug-receptor combination , 1961, Proceedings of the Royal Society of London. Series B. Biological Sciences.

[20]  J. Schwartz,et al.  Histamine H3‐receptor‐mediated [35S]GTPγ[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors , 2002, British journal of pharmacology.

[21]  T. Kenakin,et al.  Inverse, protean, and ligand‐selective agonism: matters of receptor conformation , 2001, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[22]  P. Morgan,et al.  The Cubic Ternary Complex ReceptorOccupancy Model I. Model Description , 1996 .

[23]  Ted L. Anderson,et al.  On the Application of R -Curves and Maximum Load Toughness to Structures , 1988 .

[24]  T. Costa,et al.  Agonist Efficacy and Aliosteric Models of Receptor Action a , 1997, Annals of the New York Academy of Sciences.

[25]  T. Schwartz,et al.  High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist. , 2003, Molecular endocrinology.

[26]  P. Leff Inverse agonism: theory and practice. , 1995, TIPS - Trends in Pharmacological Sciences.

[27]  J. Kukkonen,et al.  Protean agonism at alpha2A-adrenoceptors. , 1998, Molecular pharmacology.

[28]  Terry Kenakin,et al.  Ligand-selective receptor conformations revisited: the promise and the problem. , 2003, Trends in pharmacological sciences.

[29]  J. Black,et al.  Operational models of pharmacological agonism , 1983, Proceedings of the Royal Society of London. Series B. Biological Sciences.

[30]  G. Liljestrand,et al.  Readings In Pharmacology , 1981 .

[31]  Lakshmi A. Devi,et al.  G-protein-coupled receptor heterodimerization modulates receptor function , 1999, Nature.

[32]  P. Chidiac,et al.  Agonist-induced modulation of inverse agonist efficacy at the beta 2-adrenergic receptor. , 1996, Molecular pharmacology.

[33]  G. Pasternak,et al.  3H-naloxone benzoylhydrazone binding in MOR-1-transfected Chinese hamster ovary cells: evidence for G-protein-dependent antagonist binding. , 1998, The Journal of pharmacology and experimental therapeutics.

[34]  R. Lefkowitz,et al.  A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model. , 1993, The Journal of biological chemistry.

[35]  A Herz,et al.  Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[36]  Melanie G. Lee,et al.  RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor , 1998, Nature.

[37]  A. Trautmann,et al.  Dissociation of the signalling and antiviral properties of SDF-1-derived small peptides , 1998, Current Biology.

[38]  A Karlin,et al.  On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine. , 1967, Journal of theoretical biology.

[39]  S. A. Mathis,et al.  Spontaneous Human B2 Bradykinin Receptor Activity Determines the Action of Partial Agonists as Agonists or Inverse Agonists , 1999, The Journal of Biological Chemistry.

[40]  S. Nishikawa,et al.  Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1 , 1996, Nature.

[41]  W. Paton On becoming and being a pharmacologist. , 1986, Annual review of pharmacology and toxicology.

[42]  F. Ehlert,et al.  Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. , 1988, Molecular pharmacology.

[43]  R P STEPHENSON,et al.  A MODIFICATION OF RECEPTOR THEORY , 1997, British journal of pharmacology and chemotherapy.

[44]  Ariens Ej,et al.  Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory. , 1954 .

[45]  A. Scheer,et al.  A Look at Receptor Efficacy. From the Signalling Network of the Cell to the Intramolecular Motion of the Receptor , 2000 .

[46]  M. Maguire,et al.  Relationship between the beta-adrenergic receptor and adenylate cyclase. , 1977, The Journal of biological chemistry.

[47]  J. Changeux,et al.  ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL. , 1965, Journal of molecular biology.

[48]  H. Rang,et al.  The uptake of atropine and related drugs by intestinal smooth muscle of the guinea-pig in relation to acetylcholine receptors , 1965, Proceedings of the Royal Society of London. Series B. Biological Sciences.

[49]  Christopher Haslett,et al.  Bombesin and Substance P Analogues Differentially Regulate G-protein Coupling to the Bombesin Receptor , 2001, The Journal of Biological Chemistry.

[50]  A. Maehle,et al.  The emergence of the drug receptor theory , 2002, Nature Reviews Drug Discovery.

[51]  B. Katz,et al.  A study of the ‘desensitization’ produced by acetylcholine at the motor end‐plate , 1957, The Journal of physiology.

[52]  Thron Cd On the analysis of pharmacological experiments in terms of an allosteric receptor model. , 1973 .

[53]  D. Mackay A Critical Survey of Receptor Theories of Drug Action , 1977 .

[54]  P. Casellas,et al.  A Selective Inverse Agonist for Central Cannabinoid Receptor Inhibits Mitogen-activated Protein Kinase Activation Stimulated by Insulin or Insulin-like Growth Factor 1 , 1997, The Journal of Biological Chemistry.

[55]  Bernard,et al.  Advances in Drug Research , 1964 .

[56]  G. Uhl,et al.  μ Opioid Receptor Phosphorylation, Desensitization, and Ligand Efficacy* , 1997, The Journal of Biological Chemistry.

[57]  Bernard Katz,et al.  Interaction at end-plate receptors between different choline derivatives , 1957, Proceedings of the Royal Society of London. Series B - Biological Sciences.