TY - BOOK AU - Seifert,Roland AU - Wieland,Thomas TI - G protein-coupled receptors as drug targets: analysis of activation and constitutive activity SN - 9783527308194 U1 - 615.7 PY - 2005/// CY - Weinheim PB - Wiley-VCH KW - G proteins KW - Drug targeting N1 - Includes bibliographical references and index; Preface. - A personal foreword. - List of contributors. - Abbreviations and terminology. - I. General concepts. - 1. Historical background and introduction. - 2. The nature of constitutive activity and inverse agonism. - 3. Molecular mechanisms of GPCR activation. - 4. Molecular and cellular determinants of GPCR splice variant constitutive activity. - 5. Naturally occurring constitutively active receptors: physiologic and pharmacologic implications. - 6. The impact of G-Proteins on constitutive GPCR activity. - 7. (Patho)physiological and therapeutic relevance of constitutive GPCR activity and inverse agonism at GProtein-coupled receptors. - 8. Methodological approaches. - II. Constitutive activity of selected GPCR systems. - 9. Constitutive activity of -adrenoceptors: analysis in membrane systems. - 10. Constitutive activity of -adrenoceptors: analysis by physiological methods. - 11. Constitutive activity at the 1-Adrenoceptors: past and future implications. - 12. Constitutive activity of muscarinic acetylcholine receptors: implications for receptor activation and physiological relevance. - 13.Constitutively active histamine receptors.- 14. Constitutively active serotonin receptors. - 15. Virally encoded constitutively active chemokine receptors. - Index ER -