Autor
Este décimo volumen de la Fundación Dr. Antonio Esteve recoge los datos existentes, los nuevos hallazgos y las perspectivas de futuro entorno al agonismo inverso. Sus contenidos son fruto del simposio celebrado en 2002 en S’Agaró (Girona) y que moderó Adriaan Ijzerman, delLeiden/Amsterdam Center for Drug Research. Se presentaron 23 ponencias, una de ellas defendida por Pilar D’Ocon, de la Universidad de Valencia y única representante española, que han quedado recogidas en este volumen de Esteve Foundation Symposia y que ha sido publicado por Elsevier Science. Con él se pretende avanzar un poco más en el campo científico del agonismo inverso, un fenómeno farmacológico del que todavía queda mucho por conocer.
| Capítulos | ||
| 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”] | |
- 2. Novel approaches to enhance the detection of receptor constitutive activity and inverse agonists
- G. Milligan
- Descargar
- 10. 5-HT2c constitutive receptor activity: effector pathway dependence
- K.A. Berg / W.P. Clarke
- Descargar
- 18. The thyrotropin receptor, a GPCR with a built-in inverse agonist
- G. Vassart / S. Costagliola
- Descargar
- 3. From inverse agonism to \'Paradoxical Pharmacology\'
- R.A. Bond / K.L.J. Evans / Z. Callaerts-Vegh
- Descargar
- 11. Modulation of constitutive GPCR activity: a way of life?
- R. Leurs / R.A. Bakker / P. Casarosa / D. Verzijl / H. Timmerman / M.J. Smit
- Descargar
- 19. Inverse agonism and the PTH/PTHrP receptor
- R. Gensure / P.H. Carter / T.J. Gardella
- Descargar
- 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
- Descargar
- 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
- Descargar
- 20. Inverse agonists to explore the mechanisms of metabotropic glutamate receptor activity
- L. Prezeau / M.L. Parmentier / R. Carroll / J.R Pin
- Descargar
- 5. Inverse agonism at p»radrenergic receptors
- M.J. Lohse / C. Hoffmann / S. Engelhardt
- Descargar
- 13. Inverse agonism of the antipsychotic drugs at the D2 dopamine receptor
- P.G. Strange
- Descargar
- 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
- Descargar
- 6. Physiological and pathological role of the constitutively active a1D adrenoceptors
- P. D'Ocon
- Descargar
- 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
- Descargar
- General discussion
- Descargar
- Inverse agonism Introduction
- A.P. IJzerman
- Descargar
- 7. Inverse agonism at cannabinoid receptors
- R.G. Pertwee
- Descargar
- 15. Platelet-activating factor receptor: differential regulation and signaling by agonists and inverse agonists
- D.J. Dupré / M. Rola-Pleszczynski / J. Stañková
- Descargar
- 3. From inverse agonism to \'Paradoxical Pharmacology\'
- R.A. Bond / K.L.J. Evans / Z. Callaerts-Vegh
- Descargar
- Inverse agonism List of participants
- Descargar
- 8. Inverse agonism at adenosine A! receptors
- R.A.F. de Ligt /, A. Lorenzen / A.P. IJzerman
- Descargar
- 16. AgRP, physiological role of an inverse agonist
- R.A.H. Adán / W.A.J. Nijenhuis / M.J.H. Kas
- Descargar
- Inverse agonism General discussion
- Descargar
- 1. Different mechanisms of negative efficacy. Distinguishing inverse agonists from negative antagonists
- T. Costa / C. Ambrosio / D. Riitano / P. Molinari
- Descargar
- 9. Differential ligand efficacy at h5-HT1A receptor-coupled G-protein subtypes: a commentary
- A. Newman-Tancredi
- Descargar
- 17. Inverse agonism at neurotensin receptors NTS1 and NTS2
- P. Kitabgi
- Descargar
