Inverse Agonism: Proceedings of the Esteve Foundation Symposium X, S'Agaro (Girona), Spain, 2-5 October 2002(v. 1249 International Congress S.)

This volume reflects the contemporary state of thinking and debates with regard to inverse agonism. It constitutes the first book published on this issue and holds the contributions and recorded discussions of the 10th Esteve Foundation Symposium held in 2002. Inverse agonism at G-protein-coupled receptors is a novel pharmacological concept with important consequences for the understanding of receptor mechanisms and drug action. Since its first description in 1989 the concept of inverse agonism has dramatically changed the view on current and future medicines. Next to traditional agonists and antagonists the drug repertoire has been expanded now with a novel category of ligands, that is. "inverse agonists".

Table of Contents:
About the Esteve Foundation. Introduction. Different mechanisms of negative efficacy. Distinguishing inverse agonists from negative antagonists (T. Costa et al.). Novel approaches to enhance the detection of receptor constitutive activity and inverse agonists (G. Milligan). From inverse agonism to "Paradoxical Pharmacology" (R.A. Bond, K.L.J. Evans, Z. Callaerts-Vegh). Different inverse agonist activities of beta-adrenergic receptor antagonists - pharmacological characterization and therapeutical implications in the treatment of chronic heart failure (C. Maack, M. Bohm (Germany). Inverse agonism at beta1 -adrenergic receptors (M.J. Lohse, C. Hoffmann, S. Engelhardt). Physiological and pathological role of the constitutively active alpha1D-adrenoceptors (P. D'Ocon). Inverse agonism at cannabinoid receptors (R.G. Pertwee). Inverse agonism at adenosine A1 receptors (R.A.F. de Ligt, A. Lorenzen, A.P. IJzerman). Differential ligand efficacy at h5 HT1A receptor-coupled G-protein subtypes: a commentary (A. Newman-Tancredi). 5-HT2c constitutive receptor activity: effector pathway-dependence (K.A. Berg, W.P. Clarke). Modulation of constitutive GPCR activity: a way of life? (R. Leurs et al.). Constitutive activity of the recombinant and native histamine H3 receptor (J.M. Arrang et al.). Inverse agonism of the antipsychotic drugs at the D2 dopamine receptor (P.G. Strange). Inverse agonism at dopamine D2 receptors: a receptor recalcitrant to high levels of constitutive activation (T. Wurch, E.A. Boutet-Robinet, P.J. Pauwels). Platelet-activating factor receptor: differential regulation and signaling by agonists and inverse agonists (D.J. Dupre, M Rola-Pleszczynski, J. Stankova). AgRP, physiological role of an inverse agonist (R.A.H. Adan, W.A.J. Nijenhuis, M.J.H. Kas). Inverse agonism at neurotensin receptors NTS1 and NTS2 (P. Kitabgi). The thyrotropin receptor, a GPCR with a built in inverse agonist (G. Vassart). Inverse agonism and the PTH/PTHrP receptor (R. Gensure, P.H. Carter, T.J. Gardella). Inverse agonists to explore the mechanisms of metabotropic glutamate receptor activity (L. Prezeau et al.). Control of constitutive activity of metabotropic glutamate receptors by Homer proteins (L. Fagni et al.). General discussion. Author index.