Author
This tenth volume of the Esteve Foundation gathers existing data, new findings and future perspectives related to reverse agonism. Its contents is the result of the symposium held in S’Agaró (Girona) in 2002, moderated by Adriaan Ijzerman, from the Leiden/Amsterdam Center for Drug Research. Twenty-three submissions were presented, one of them by the only Spanish representative, Pilar D’Ocon, from the University of Valencia. All submissions are gathered in this volume of Esteve Foundation Symposia, published by Elsevier Science. The objective is to advance a little further in the field of reverse agonism, a pharmacological phenomenon still largely unknown.
| Chapters | ||
| Introduction | A.P. IJzerman | [wpdm id=287 type=”btn”] |
| List of participants | [wpdm id=288 type=”btn”] | |
| 1. Different mechanisms of negative efficacy. Distinguishing inverse agonists from negative antagonists | T. Costa / C. Ambrosio / D. Riitano / P. Molinari | [wpdm id=265 type=”btn”] |
| 2. Novel approaches to enhance the detection of receptor constitutive activity and inverse agonists | G. Milligan | [wpdm id=266 type=”btn”] |
| 3. From inverse agonism to \’Paradoxical Pharmacology\’ | R.A. Bond / K.L.J. Evans / Z. Callaerts-Vegh | [wpdm id=267 type=”btn”] |
| 4. Different inverse agonist activities of B-adrenergic receptor antagonists—pharmacological characterization and therapeutical implications in the treatment of chronic heart failure | C. Maack / M. Böhm | [wpdm id=268 type=”btn”] |
| 5. Inverse agonism at p»radrenergic receptors | M.J. Lohse / C. Hoffmann / S. Engelhardt | [wpdm id=269 type=”btn”] |
| 6. Physiological and pathological role of the constitutively active a1D adrenoceptors | P. D\’Ocon | [wpdm id=270 type=”btn”] |
| 7. Inverse agonism at cannabinoid receptors | R.G. Pertwee | [wpdm id=271 type=”btn”] |
| 8. Inverse agonism at adenosine A! receptors | R.A.F. de Ligt /, A. Lorenzen / A.P. IJzerman | [wpdm id=272 type=”btn”] |
| 9. Differential ligand efficacy at h5-HT1A receptor-coupled G-protein subtypes: a commentary | A. Newman-Tancredi | [wpdm id=273 type=”btn”] |
| 10. 5-HT2c constitutive receptor activity: effector pathway dependence | K.A. Berg / W.P. Clarke | [wpdm id=274 type=”btn”] |
| 11. Modulation of constitutive GPCR activity: a way of life? | R. Leurs / R.A. Bakker / P. Casarosa / D. Verzijl / H. Timmerman / M.J. Smit | [wpdm id=275 type=”btn”] |
| 12. Constitutive activity of the recombinant and native histamine H3 receptor | J.M. Arrang / S. Morisset / A. Rouleau / F. Gbahou / X. Ligneau / J. Tardivel-Lacombe / H. Stark / W. Schunack / C.R. Ganellin / J.C. Schwartz | [wpdm id=276 type=”btn”] |
| 13. Inverse agonism of the antipsychotic drugs at the D2 dopamine receptor | P.G. Strange | [wpdm id=277 type=”btn”] |
| 14. Inverse agonism at dopamine D2 receptors: a receptor recalcitrant to high levels of constitutive activation | T. Wurch / E.A. Boutet-Robinet / P.J. Pauwels | [wpdm id=278 type=”btn”] |
| 15. Platelet-activating factor receptor: differential regulation and signaling by agonists and inverse agonists | D.J. Dupré / M. Rola-Pleszczynski / J. Stañková | [wpdm id=279 type=”btn”] |
| 16. AgRP, physiological role of an inverse agonist | R.A.H. Adán / W.A.J. Nijenhuis / M.J.H. Kas | [wpdm id=280 type=”btn”] |
| 17. Inverse agonism at neurotensin receptors NTS1 and NTS2 | P. Kitabgi | [wpdm id=281 type=”btn”] |
| 18. The thyrotropin receptor, a GPCR with a built-in inverse agonist | G. Vassart / S. Costagliola | [wpdm id=282 type=”btn”] |
| 19. Inverse agonism and the PTH/PTHrP receptor | R. Gensure / P.H. Carter / T.J. Gardella | [wpdm id=283 type=”btn”] |
| 20. Inverse agonists to explore the mechanisms of metabotropic glutamate receptor activity | L. Prezeau / M.L. Parmentier / R. Carroll / J.R Pin | [wpdm id=284 type=”btn”] |
| 21. Control of constitutive activity of metabotropic glutamate receptors by Homer proteins | Laurent Fagni / F. Ango / L. Prezeau / P.F. Worley / J.P. Pin / J. Bockaert | [wpdm id=285 type=”btn”] |
| General discussion | [wpdm id=286 type=”btn”] | |
- 12. Constitutive activity of the recombinant and native histamine H3 receptor
- J.M. Arrang / S. Morisset / A. Rouleau / F. Gbahou / X. Ligneau / J. Tardivel-Lacombe / H. Stark / W. Schunack / C.R. Ganellin / J.C. Schwartz
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- Inverse agonism General discussion
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- 3. From inverse agonism to \'Paradoxical Pharmacology\'
- R.A. Bond / K.L.J. Evans / Z. Callaerts-Vegh
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- General discussion
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- 21. Control of constitutive activity of metabotropic glutamate receptors by Homer proteins
- Laurent Fagni / F. Ango / L. Prezeau / P.F. Worley / J.P. Pin / J. Bockaert
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- 20. Inverse agonists to explore the mechanisms of metabotropic glutamate receptor activity
- L. Prezeau / M.L. Parmentier / R. Carroll / J.R Pin
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- 19. Inverse agonism and the PTH/PTHrP receptor
- R. Gensure / P.H. Carter / T.J. Gardella
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- 18. The thyrotropin receptor, a GPCR with a built-in inverse agonist
- G. Vassart / S. Costagliola
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- 17. Inverse agonism at neurotensin receptors NTS1 and NTS2
- P. Kitabgi
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- 16. AgRP, physiological role of an inverse agonist
- R.A.H. Adán / W.A.J. Nijenhuis / M.J.H. Kas
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- 15. Platelet-activating factor receptor: differential regulation and signaling by agonists and inverse agonists
- D.J. Dupré / M. Rola-Pleszczynski / J. Stañková
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- 14. Inverse agonism at dopamine D2 receptors: a receptor recalcitrant to high levels of constitutive activation
- T. Wurch / E.A. Boutet-Robinet / P.J. Pauwels
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- 13. Inverse agonism of the antipsychotic drugs at the D2 dopamine receptor
- P.G. Strange
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- Inverse agonism Introduction
- A.P. IJzerman
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- 11. Modulation of constitutive GPCR activity: a way of life?
- R. Leurs / R.A. Bakker / P. Casarosa / D. Verzijl / H. Timmerman / M.J. Smit
- Download
- 10. 5-HT2c constitutive receptor activity: effector pathway dependence
- K.A. Berg / W.P. Clarke
- Download
- 9. Differential ligand efficacy at h5-HT1A receptor-coupled G-protein subtypes: a commentary
- A. Newman-Tancredi
- Download
- 8. Inverse agonism at adenosine A! receptors
- R.A.F. de Ligt /, A. Lorenzen / A.P. IJzerman
- Download
- 7. Inverse agonism at cannabinoid receptors
- R.G. Pertwee
- Download
- 6. Physiological and pathological role of the constitutively active a1D adrenoceptors
- P. D'Ocon
- Download
- 5. Inverse agonism at p»radrenergic receptors
- M.J. Lohse / C. Hoffmann / S. Engelhardt
- Download
- 4. Different inverse agonist activities of B-adrenergic receptor antagonists—pharmacological characterization and therapeutical implications in the treatment of chronic heart failure
- C. Maack / M. Böhm
- Download
- 3. From inverse agonism to \'Paradoxical Pharmacology\'
- R.A. Bond / K.L.J. Evans / Z. Callaerts-Vegh
- Download
- 2. Novel approaches to enhance the detection of receptor constitutive activity and inverse agonists
- G. Milligan
- Download
- 1. Different mechanisms of negative efficacy. Distinguishing inverse agonists from negative antagonists
- T. Costa / C. Ambrosio / D. Riitano / P. Molinari
- Download
- Inverse agonism List of participants
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