P Delagrange

Summary

Affiliation: Institut de Recherches Servier
Country: France

Publications

  1. ncbi request reprint Therapeutic perspectives for melatonin agonists and antagonists
    P Delagrange
    Institut de Recherches Internationales Servier, 6 place des Pleiades, 92415 Courbevoie Cedex, France
    J Neuroendocrinol 15:442-8. 2003
  2. ncbi request reprint Purification of the recombinant human serotonin N-acetyltransferase (EC 2.3.1.87): further characterization of and comparison with AANAT from other species
    Gilles Ferry
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125, chemin de Ronde 78290 Croissy sur Seine, France
    Protein Expr Purif 38:84-98. 2004
  3. ncbi request reprint Quinone reductase 2 substrate specificity and inhibition pharmacology
    Jean A Boutin
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Chem Biol Interact 151:213-28. 2005
  4. ncbi request reprint Therapeutic potential of melatonin ligands
    Philippe Delagrange
    Département des Sciences Expérimentales, Institut de Recherches Servier, Suresnes, France
    Chronobiol Int 23:413-8. 2006
  5. ncbi request reprint Comparative pharmacological studies of melatonin receptors: MT1, MT2 and MT3/QR2. Tissue distribution of MT3/QR2
    O Nosjean
    , Institut de Recherches Servier, 78290-Croissy-sur-Seine, France
    Biochem Pharmacol 61:1369-79. 2001
  6. ncbi request reprint Characterization and regulation of a CHO cell line stably expressing human serotonin N-acetyltransferase (EC 2.3.1.87)
    G Ferry
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, Croissy sur Seine, France
    Cell Mol Life Sci 59:1395-405. 2002
  7. ncbi request reprint Effects of S-21007, a potent 5-HT3 partial agonist, in mouse anxiety
    P Delagrange
    Institut de Recherches Internationales Servier, 92415 Courbevoie, France
    Zhongguo Yao Li Xue Bao 20:805-12. 1999
  8. ncbi request reprint [Melatonin and regulation of the cardiovascular system]
    E Scalbert
    Division de Thérapeutique Expérimentale, Institut de Recherches Internationales Servier, Courbevoie, France
    Therapie 53:459-65. 1998
  9. pmc The end of a myth: cloning and characterization of the ovine melatonin MT(2) receptor
    F Coge
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, Suresnes, France
    Br J Pharmacol 158:1248-62. 2009
  10. ncbi request reprint Melatonin and energy homeostasis: peripheral versus central regulation
    P Delagrange
    Institut de Recherches Internationales Servier, Courbevoie, France
    Minerva Endocrinol 28:313-20. 2003

Collaborators

  • E Fuchs
  • M Migaud
  • J A Boutin
  • P Renard
  • O Nosjean
  • B Malpaux
  • G Ferry
  • R Jockers
  • Perry Barrett
  • Valérie Audinot
  • S Yous
  • Peter J Morgan
  • Jean Claude Thiery
  • Jean Marc Chillon
  • David Hazlerigg
  • E Savaskan
  • J E Drew
  • François Mailliet
  • Angelique Levoye
  • Fanny Vella
  • Daniel Lesieur
  • Caroline Bennejean
  • Mohammed A Ayoub
  • Jean Luc Guillaume
  • Pascale Chomarat
  • Marie Claude Viaud-Massuard
  • Philippe Chavatte
  • F Coge
  • Mohamed Ettaoussi
  • Hassina Ould Hamouda
  • Celine Legros
  • Marie Françoise Boussard
  • Francis Coge
  • Catherine Mallet
  • Alain Chavanieu
  • Gérard Grassy
  • Cyril Sarrauste de Menthiere
  • François Dupuis
  • Carlos Larraya
  • Bruno Pfeiffer
  • Marc Claret
  • Gerald Guillaumet
  • Elizabeth Scalbert
  • Anne Bonnaud
  • Bénédicte Prunet-Marcassus
  • Isabelle Charton
  • STEPHEN T O'ROURKE
  • Cecile Pegurier
  • Oxana R Kunduzova
  • Carole Descamps-François
  • Jean Paul Nicolas
  • Véronique Leclerc
  • Valérie Wallez
  • C Slugocki
  • S Devavry
  • N Renault
  • C Legros
  • W Cohen
  • C Ouvry
  • S P Guenin
  • I Fery
  • Pascal Berthelot
  • Frédérique Klupsch
  • Daniel H Caignard
  • Basile Pérès
  • Patty Chen
  • Avais M Daulat
  • Rivka Ravid
  • Stephanie Giraudet
  • Elisabeth Mocaer
  • Sophie P Guénin
  • Pascal Maurice
  • Stephane Leonce
  • Stéphanie Chalivoix
  • Nejla Sözer-Topçular
  • Nadine Nagel
  • Cecilia Gabriel
  • E Scalbert
  • Anne Rousseau-Rojas
  • Sophie Descamps
  • Julie Dam
  • Michel Wierzbicki
  • Monique Droual
  • Sylvie Briss
  • Cyril Couturier
  • Sandrine Truche
  • Sylvie Berger
  • Sophie Pénélope Guenin
  • Carmen Gorostiaga
  • Patrick Limiñana

Detail Information

Publications42

  1. ncbi request reprint Therapeutic perspectives for melatonin agonists and antagonists
    P Delagrange
    Institut de Recherches Internationales Servier, 6 place des Pleiades, 92415 Courbevoie Cedex, France
    J Neuroendocrinol 15:442-8. 2003
    ..Moreover, the functional role of each of the receptor subtypes has to be characterized to design selective ligands to treat specific diseases...
  2. ncbi request reprint Purification of the recombinant human serotonin N-acetyltransferase (EC 2.3.1.87): further characterization of and comparison with AANAT from other species
    Gilles Ferry
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125, chemin de Ronde 78290 Croissy sur Seine, France
    Protein Expr Purif 38:84-98. 2004
    ....
  3. ncbi request reprint Quinone reductase 2 substrate specificity and inhibition pharmacology
    Jean A Boutin
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Chem Biol Interact 151:213-28. 2005
    ..These compounds, co-substrate, substrate and inhibitors will permit to better know this enzyme, the role of which is still poorly understood...
  4. ncbi request reprint Therapeutic potential of melatonin ligands
    Philippe Delagrange
    Département des Sciences Expérimentales, Institut de Recherches Servier, Suresnes, France
    Chronobiol Int 23:413-8. 2006
    ..The development of specific ligands for each of these melatonin binding sites is necessary to link physiological and/or therapeutic effects...
  5. ncbi request reprint Comparative pharmacological studies of melatonin receptors: MT1, MT2 and MT3/QR2. Tissue distribution of MT3/QR2
    O Nosjean
    , Institut de Recherches Servier, 78290-Croissy-sur-Seine, France
    Biochem Pharmacol 61:1369-79. 2001
    ....
  6. ncbi request reprint Characterization and regulation of a CHO cell line stably expressing human serotonin N-acetyltransferase (EC 2.3.1.87)
    G Ferry
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, Croissy sur Seine, France
    Cell Mol Life Sci 59:1395-405. 2002
    ..This cell line was used to screen libraries of compounds in a living system and led to the discovery of several potent specific and non-toxic AANAT inhibitors...
  7. ncbi request reprint Effects of S-21007, a potent 5-HT3 partial agonist, in mouse anxiety
    P Delagrange
    Institut de Recherches Internationales Servier, 92415 Courbevoie, France
    Zhongguo Yao Li Xue Bao 20:805-12. 1999
    ..To study the effect of S-21007, a 5-HT3 partial agonist in different animal models of anxiety in mice...
  8. ncbi request reprint [Melatonin and regulation of the cardiovascular system]
    E Scalbert
    Division de Thérapeutique Expérimentale, Institut de Recherches Internationales Servier, Courbevoie, France
    Therapie 53:459-65. 1998
    ....
  9. pmc The end of a myth: cloning and characterization of the ovine melatonin MT(2) receptor
    F Coge
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, Suresnes, France
    Br J Pharmacol 158:1248-62. 2009
    ..For many years, it was suspected that sheep expressed only one melatonin receptor (closely resembling MT(1) from other mammal species). Here we report the cloning of another melatonin receptor, MT(2), from sheep...
  10. ncbi request reprint Melatonin and energy homeostasis: peripheral versus central regulation
    P Delagrange
    Institut de Recherches Internationales Servier, Courbevoie, France
    Minerva Endocrinol 28:313-20. 2003
    ..Both, the MT1 and MT2 subtypes appear to be involved. The respective contribution of central and peripheral effects of melatonin on energy homeostasis in vivo must be established in future studies...
  11. ncbi request reprint Design and synthesis of 3-phenyl tetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands
    Said Yous
    Laboratoire de Chimie Therapeutique, Faculte des Sciences Pharmaceutiques et Biologiques, Universite de Lille 2, BP 83, 59006 Lille Cedex, France
    Bioorg Med Chem 11:753-9. 2003
    ..The (+)-(RR)-cis enantiomer of the N-[2-(7-methoxy-3-phenyl-1,2,3,4-tetrahydro-naphthalen-1-yl)ethyl]cyclobutyl carboxamide (14) is one of the most MT(2) selective ligands described until now and behaves as an antagonist...
  12. ncbi request reprint First evidence of melatonin receptors distribution in the suprachiasmatic nucleus of tree shrew brain
    Celine Legros
    INRA, UMR85 Physiologie de Reproduction et des Comportements, F 37380 Nouzilly, France
    Neuro Endocrinol Lett 28:267-73. 2007
    ..In this study we investigated the distribution of melatonergic receptors in the tree shrew brain. The psychosocial stress in the tree shrew is a validated model of depression with disturbance of circadian rhythms...
  13. ncbi request reprint Organs from mice deleted for NRH:quinone oxidoreductase 2 are deprived of the melatonin binding site MT3
    François Mailliet
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    FEBS Lett 578:116-20. 2004
    ..These data establish NQO2 as part of the MT3 binding sites in vivo and resolve the matter of the nature of the third melatonin binding site...
  14. ncbi request reprint Molecular tools to study melatonin pathways and actions
    Jean A Boutin
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125, chemin de Ronde 78290 Croissy sur Seine, France
    Trends Pharmacol Sci 26:412-9. 2005
    ..Furthermore, various compounds, mainly inhibitors and antagonists, that can be used to dissect these functions and pathways are presented...
  15. ncbi request reprint NRH:quinone reductase 2: an enzyme of surprises and mysteries
    Fanny Vella
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125, chemin de Ronde 78290 Croissy sur Seine, France
    Biochem Pharmacol 71:1-12. 2005
    ..Finally QR2 might be implicated in the toxicity, in vivo, of quinones such as menadione. The present commentary attempts to summarize this information and discusses a series of hypotheses...
  16. ncbi request reprint Characterization of the melatoninergic MT3 binding site on the NRH:quinone oxidoreductase 2 enzyme
    François Mailliet
    Division de Pharmacologie Moleculaire et Cellulaire, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Biochem Pharmacol 71:74-88. 2005
    ..The compounds described in the present paper are new tools for such a task...
  17. ncbi request reprint New ligands at the melatonin binding site MT(3)
    Marie Françoise Boussard
    Division de Chimie médicinale E, Institut de Recherches Servier, Suresnes, France
    Eur J Med Chem 41:306-20. 2006
    ....
  18. ncbi request reprint Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3)
    Véronique Leclerc
    Institut de Chimie Pharmaceutique Albert Lespagnol, 3 rue du Professeur Laguesse, BP83, 59006 Lille Cedex, France
    J Med Chem 45:1853-9. 2002
    ..The 2-iodo derivatives (12 and 10) of compounds 5 and 17 have also been synthesized to evaluate their binding profile with a view to further develop MT(3) selective radioligands...
  19. ncbi request reprint Are G protein-coupled receptor heterodimers of physiological relevance?--Focus on melatonin receptors
    Angelique Levoye
    Department of Cell Biology, Institut Cochin, Universite Paris Descartes, Faculte de Medecine, France
    Chronobiol Int 23:419-26. 2006
    ....
  20. doi request reprint Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3
    Mohamed Ettaoussi
    Laboratoire de Chimie Thérapeutique EA 1043, Faculte des Sciences Pharmaceutiques et Biologiques, Universite de Lille, 3, rue du Professeur Laguesse, 2, BP 83, 59006 Lille Cedex, France
    Bioorg Med Chem 16:4954-62. 2008
    ..This selectivity can be modulated with suitable variations of the C-5 position and the acyl group on the C-3 side chain...
  21. doi request reprint Molecular cloning and pharmacological characterization of rat melatonin MT1 and MT2 receptors
    Valérie Audinot
    Division de Pharmacologie Moleculaire et Cellulaire, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Biochem Pharmacol 75:2007-19. 2008
    ..These in vitro results obtained with the rat melatonin receptors are thus of importance to understand the physiological roles of each subtype in animal models...
  22. doi request reprint Studies of the melatonin binding site location onto quinone reductase 2 by directed mutagenesis
    Jean A Boutin
    Division de Pharmacologie Moleculaire et Cellulaire, Institut de Recherches Servier, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    Arch Biochem Biophys 477:12-9. 2008
    ....
  23. ncbi request reprint New selective ligands of human cloned melatonin MT1 and MT2 receptors
    Valérie Audinot
    Division de Pharmacologie Moleculaire et Cellulaire, Institut de Recherches Servier, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    Naunyn Schmiedebergs Arch Pharmacol 367:553-61. 2003
    ..Finally, we also discovered S 25150, the most potent melatonin receptor agonist, so far reported in the literature...
  24. pmc Melatonin inhibits nitrate tolerance in isolated coronary arteries
    STEPHEN T O'ROURKE
    Department of Pharmaceutical Sciences, North Dakota State University, Fargo, ND 58105, USA
    Br J Pharmacol 139:1326-32. 2003
    ..5) The results demonstrate that melatonin, acting via specific melatonin receptors, inhibits nitrate tolerance in coronary arteries and that this effect is dependent on the presence of the vascular endothelium...
  25. ncbi request reprint Synthesis of 5-substituted-2,3-dihydro-1,4-benzoxathiins: biological evaluation as melatonin receptors ligands
    Isabelle Charton
    Institut de Chimie Organique et Analytique, UMR CNRS 6005, Universite d Orleans, rue de Chartres, BP 6759, 45067 Orleans Cedex 02, France
    J Enzyme Inhib Med Chem 18:187-93. 2003
    ..These new melatonin analogues were evaluated on human receptors MT1 and MT2 and have a similar affinity to that of melatonin itself...
  26. ncbi request reprint New substrate analogues of human serotonin N-acetyltransferase produce in situ specific and potent inhibitors
    Gilles Ferry
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, Croissy sur Seine, France
    Eur J Biochem 271:418-28. 2004
    ..Nevertheless, these inhibitors form a series of pharmacological tools that could be used to understand more closely the inhibition of pineal melatonin production in vivo...
  27. ncbi request reprint Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands
    Carole Descamps-François
    Faculte de Pharmacie, Laboratoire de Chimie Therapeutique, Universite de Lille 2, 3 rue du Professeur Laguesse, BP 83, 59006 Lille Cedex, France
    J Med Chem 46:1127-9. 2003
    ..Some of these compounds behave as MT(1)-selective ligands. The most selective one (5) behaves as an antagonist...
  28. ncbi request reprint Differential coupling of the extreme C-terminus of G protein alpha subunits to the G protein-coupled melatonin receptors
    Janice E Drew
    Phytochemicals and Genomic Stability, Rowett Research Institute, Greenburn Road, Bucksburn, Aberdeen AB21 9SB, Scotland, UK
    Biochim Biophys Acta 1592:185-92. 2002
    ..Recognition of the C-terminal five amino acids of the Galpha subunit is a requisite for coupling to a receptor, but it is not the sole determinant...
  29. ncbi request reprint Molecular pharmacology of the ovine melatonin receptor: comparison with recombinant human MT1 and MT2 receptors
    François Mailliet
    UMR INRA CNRS Université de Tours 6073, Physiologie de la Reproduction et des Comportements, Nouzilly 37380, France
    Biochem Pharmacol 67:667-77. 2004
    ..Furthermore, some compounds showed marked different functional activities at oMT1 vs. hMT1 receptors. Our findings demonstrated differences in the pharmacological properties of melatonin receptors in ovine and human species...
  30. ncbi request reprint Synthesis of new arylalkoxy amido derivatives as melatoninergic ligands
    Cecile Pegurier
    CNRS BIOCIS UPRES A 8076, Universite de Paris Sud, Faculte de Pharmacie, 5 Rue Jean Baptiste Clement, 92296, Chatenay Malabry, France
    Bioorg Med Chem 11:789-800. 2003
    ..The compounds were found to be full agonists and compound 17a was 20-fold more potent than melatonin in this bioassay...
  31. ncbi request reprint Synthesis and structure-affinity-activity relationships of novel benzofuran derivatives as MT(2) melatonin receptor selective ligands
    Valérie Wallez
    Institut de Chimie Pharmaceutique Albert Lespagnol, 3 rue du Professeur Laguesse, BP 83, 59006 Lille Cedex, France
    J Med Chem 45:2788-800. 2002
    ..1 nM). Nevertheless, 10c acts as an MT(1) and MT(2) antagonist, whereas 19 is a partial agonist...
  32. ncbi request reprint Cellular knock-down of quinone reductase 2: a laborious road to successful inhibition by RNA interference
    Pascale Chomarat
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Biochimie 89:1264-75. 2007
    ..Although becoming widespread and in some cases effective, siRNA-mediated cellular knock-down proves in the present work to be of marginal efficiency. Much development is required for this technique to be of general application...
  33. ncbi request reprint Prevention of apoptotic and necrotic cell death, caspase-3 activation, and renal dysfunction by melatonin after ischemia/reperfusion
    Oxana R Kunduzova
    INSERM U388, Institut Louis Bugnard, CHU Rangueil, Bat L3, 31403 Toulouse Cedex 4, France
    FASEB J 17:872-4. 2003
    ..The demonstration that melatonin prevents postreperfusion apoptotic and necrotic cell death and improves renal function suggests that melatonin may represent a novel therapeutic approach for prevention of I/R injury...
  34. ncbi request reprint Detection of the human GPR50 orphan seven transmembrane protein by polyclonal antibodies mapping different epitopes
    Hassina Ould Hamouda
    Institut Cochin, Department of Cell Biology, Paris, France
    J Pineal Res 43:10-5. 2007
    ..In conclusion, we successfully produced antibodies against the orphan GPR50 protein that will become valuable tools for functional studies of this protein...
  35. ncbi request reprint Concentrations of estradiol in ewe cerebrospinal fluid are modulated by photoperiod through pineal-dependent mechanisms
    Jean Claude Thiery
    UMR INRA CNRS Université de Tours, Physiologie de la Reproduction et des Comportements, Nouzilly, France
    J Pineal Res 41:306-12. 2006
    ..The results demonstrate that LD increases the E2 concentration in the CSF by a mechanism involving the pineal gland...
  36. pmc The orphan GPR50 receptor specifically inhibits MT1 melatonin receptor function through heterodimerization
    Angelique Levoye
    Department of Cell Biology, Institut Cochin, Paris, France
    EMBO J 25:3012-23. 2006
    ..Pairing orphan GPCRs to potential heterodimerization partners might be of clinical importance and may become a general strategy to better understand the function of orphan GPCRs...
  37. ncbi request reprint Preferential formation of MT1/MT2 melatonin receptor heterodimers with distinct ligand interaction properties compared with MT2 homodimers
    Mohammed A Ayoub
    Department of Cell Biology, Institut Cochin, Paris, France
    Mol Pharmacol 66:312-21. 2004
    ....
  38. ncbi request reprint Melatonin reduces body weight gain in Sprague Dawley rats with diet-induced obesity
    Bénédicte Prunet-Marcassus
    Unité Mixte de Recherche 5018 Centre National de la Recherche Scientifique, Universitaire Paul Sabatier, Institut Fédératif de Recherche 31, Toulouse Cedex 9, France
    Endocrinology 144:5347-52. 2003
    ..These data demonstrate that melatonin may act as a regulator of body weight in a model of obesity and may prevent some of the side effects on glucose homeostasis such as decreased insulin sensitivity...
  39. pmc Impact of treatment with melatonin on cerebral circulation in old rats
    François Dupuis
    Cardiovascular Research Group, EA 3448, Faculté de Pharmacie de l Université Henri Poincaré Nancy I, 5 rue Albert Lebrun, 54000 Nancy, France
    Br J Pharmacol 141:399-406. 2004
    ..British Journal of Pharmacology (2004) 141, 399-406. doi:10.1038/sj.bjp.0705629..
  40. ncbi request reprint Preparation of 4-azaindole and 7-azaindole dimers with a bisalkoxyalkyl spacer in order to preferentially target melatonin MT1 receptors over melatonin MT2 receptors
    Carlos Larraya
    EA 3247 GRCHT laboratoire de chimie organique, UFR des Sciences Pharmaceutiques, Universite de Tours, 31, avenue de Monge, 37200 Tours, France
    Eur J Med Chem 39:515-26. 2004
    ..Our results suggest the distance between indole ring seems to be an important parameter in determining the potency of binding with melatonin receptor site...
  41. ncbi request reprint Structural requirements of the N-terminal region of GLP-1-[7-37]-NH2 for receptor interaction and cAMP production
    Cyril Sarrauste de Menthiere
    Centre de Biochimie Structurale, CNRS UMR 5048 UM1 INSERM UMR 554, 29 rue de Navacelles, 34090 Montpellier Cedex, France
    Eur J Med Chem 39:473-80. 2004
    ..We also performed circular dichroism study and propose a hypothetical structural model explaining the most part of observed activities of GLP-1 analogs on RIN T3 cells...
  42. ncbi request reprint S 23521 decreases food intake and body weight gain in diet-induced obese rats
    Marc Claret
    Endocrinology and Nutrition Unit, Hospital Clinic de Barcelona, Villarroel 170, 08036 Barcelona, Spain
    Obes Res 12:1596-603. 2004
    ..To investigate the effect of S 23521, a new glucagon-like peptide-1-(7-36) amide analogue, on food intake and body weight gain in obese rats, as well as on gene expression of several proteins involved in energy homeostasis...