Mark John Millan

Summary

Affiliation: Institut de Recherches Servier
Country: France

Publications

  1. ncbi request reprint S33138 [N-[4-[2-[(3aS,9bR)-8-cyano-1,3a,4,9b-tetrahydro[1]-benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenylacetamide], a preferential dopamine D3 versus D2 receptor antagonist and potential antipsychotic agent. II. A neurochemical, electrophysiological and
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    J Pharmacol Exp Ther 324:600-11. 2008
  2. ncbi request reprint Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization
    M J Millan
    Psychopharmacology Department, Centre de Recherches de Croissy, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Pharmacol Biochem Behav 71:589-98. 2002
  3. ncbi request reprint Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade
    Mark J Millan
    Department of Psychopharmacology, Centre de Recherches de Croissy, Institut de Recherches Servier, 125 Chemin de Ronde, Croissy Seine, 78290 Paris, France
    Psychopharmacology (Berl) 177:448-58. 2005
  4. ncbi request reprint The role of monoamines in the actions of established and "novel" antidepressant agents: a critical review
    Mark J Millan
    Psychopharmacology Department, IDR Servier, 125 Chemin de Ronde, Croissy Seine, Paris 78290, France
    Eur J Pharmacol 500:371-84. 2004
  5. ncbi request reprint Activation of dopamine D1 receptors enhances cholinergic transmission and social cognition: a parallel dialysis and behavioural study in rats
    Benjamin Di Cara
    Institut de Recherches Servier, Department of Psychopharmacology, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Int J Neuropsychopharmacol 10:383-99. 2007
  6. doi request reprint An epigenetic framework for neurodevelopmental disorders: from pathogenesis to potential therapy
    Mark J Millan
    Unit for Research and Discovery in Neuroscience, IDR Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
    Neuropharmacology 68:2-82. 2013
  7. doi request reprint Cognitive dysfunction in psychiatric disorders: characteristics, causes and the quest for improved therapy
    Mark J Millan
    Institut de Recherche Servier, 78290 Croissy Seine, France
    Nat Rev Drug Discov 11:141-68. 2012
  8. doi request reprint S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, neurochemical, and electrophysiological characterization
    Anne Dekeyne
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy Seine, France
    J Pharmacol Exp Ther 340:765-80. 2012
  9. doi request reprint S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy Seine, France
    J Pharmacol Exp Ther 340:750-64. 2012
  10. ncbi request reprint Multi-target strategies for the improved treatment of depressive states: Conceptual foundations and neuronal substrates, drug discovery and therapeutic application
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125, Chemin de Ronde, 78290 Croissy Seine, France
    Pharmacol Ther 110:135-370. 2006

Detail Information

Publications75

  1. ncbi request reprint S33138 [N-[4-[2-[(3aS,9bR)-8-cyano-1,3a,4,9b-tetrahydro[1]-benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenylacetamide], a preferential dopamine D3 versus D2 receptor antagonist and potential antipsychotic agent. II. A neurochemical, electrophysiological and
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    J Pharmacol Exp Ther 324:600-11. 2008
    ..Furthermore, in line with its in vitro actions, it more potently blocks cerebral populations of D(3) versus D(2) receptors...
  2. ncbi request reprint Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization
    M J Millan
    Psychopharmacology Department, Centre de Recherches de Croissy, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Pharmacol Biochem Behav 71:589-98. 2002
    ..In conclusion, [3H]GR125,743 is an appropriate tool for the radiolabelling of native, rat 5-HT(1B) receptors and permitted determination of the affinities of an extensive series of ligands at these sites...
  3. ncbi request reprint Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade
    Mark J Millan
    Department of Psychopharmacology, Centre de Recherches de Croissy, Institut de Recherches Servier, 125 Chemin de Ronde, Croissy Seine, 78290 Paris, France
    Psychopharmacology (Berl) 177:448-58. 2005
    ..The novel antidepressant agent, agomelatine, behaves as an agonist at melatonin receptors and as an antagonist at serotonin (5-HT)(2C) receptors...
  4. ncbi request reprint The role of monoamines in the actions of established and "novel" antidepressant agents: a critical review
    Mark J Millan
    Psychopharmacology Department, IDR Servier, 125 Chemin de Ronde, Croissy Seine, Paris 78290, France
    Eur J Pharmacol 500:371-84. 2004
    ....
  5. ncbi request reprint Activation of dopamine D1 receptors enhances cholinergic transmission and social cognition: a parallel dialysis and behavioural study in rats
    Benjamin Di Cara
    Institut de Recherches Servier, Department of Psychopharmacology, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Int J Neuropsychopharmacol 10:383-99. 2007
    ..Although the relationship between these actions awaits further clarification, these data underpin the relevance of D1 receptors to CNS disorders in which cholinergic transmission and social cognition are disrupted...
  6. doi request reprint An epigenetic framework for neurodevelopmental disorders: from pathogenesis to potential therapy
    Mark J Millan
    Unit for Research and Discovery in Neuroscience, IDR Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
    Neuropharmacology 68:2-82. 2013
    ..This article is part of the Special Issue entitled 'Neurodevelopmental Disorders'...
  7. doi request reprint Cognitive dysfunction in psychiatric disorders: characteristics, causes and the quest for improved therapy
    Mark J Millan
    Institut de Recherche Servier, 78290 Croissy Seine, France
    Nat Rev Drug Discov 11:141-68. 2012
    ..This article critically discusses these issues, highlighting the challenges and opportunities for improving cognition in individuals suffering from psychiatric disorders...
  8. doi request reprint S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, neurochemical, and electrophysiological characterization
    Anne Dekeyne
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy Seine, France
    J Pharmacol Exp Ther 340:765-80. 2012
    ..In conclusion, S32212 displays a functional profile consistent with improved mood and cognitive performance, together with satisfactory tolerance...
  9. doi request reprint S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy Seine, France
    J Pharmacol Exp Ther 340:750-64. 2012
    ..Its promising profile in preclinical models potentially relevant to the treatment of depression is described in J Pharmacol Exp Ther 340:765-780, 2012...
  10. ncbi request reprint Multi-target strategies for the improved treatment of depressive states: Conceptual foundations and neuronal substrates, drug discovery and therapeutic application
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125, Chemin de Ronde, 78290 Croissy Seine, France
    Pharmacol Ther 110:135-370. 2006
    ..Finally, a diversity of multi-target strategies is proposed for the more efficacious and rapid control of core and co-morbid symptoms of depression, together with improved tolerance relative to currently available agents...
  11. ncbi request reprint Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies
    Mark John Millan
    Institut de Recherches Servier, Croissy sur Seine, France
    Therapie 60:441-60. 2005
    ....
  12. ncbi request reprint N-Methyl-D-aspartate receptors as a target for improved antipsychotic agents: novel insights and clinical perspectives
    Mark J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 78290 Croissy Seine, Paris, France
    Psychopharmacology (Berl) 179:30-53. 2005
    ..Activation of "co-agonist" N-methyl-D-aspartate (NMDA) and Glycine(B) sites is mandatory for the operation of NMDA receptors, which play an important role in the control of mood, cognition and motor function...
  13. ncbi request reprint Discriminative stimulus properties of the selective norepinephrine reuptake inhibitor, reboxetine, in rats: a characterization with alpha/beta-adrenoceptor subtype selective ligands, antidepressants, and antagonists at neuropeptide receptors
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, Croissy sur Seine, Paris, France
    Int J Neuropsychopharmacol 10:579-93. 2007
    ..The neurokinin-1 antagonist, GR205,171, mimics the interoceptive properties of reboxetine, possibly reflecting its elevation of extracellular levels of NE in corticolimbic structures...
  14. ncbi request reprint The serotonin1A receptor partial agonist S15535 [4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine] enhances cholinergic transmission and cognitive function in rodents: a combined neurochemical and behavioral analysis
    Mark J Millan
    Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 chemin de Ronde 78290 Croissy Seine, France
    J Pharmacol Exp Ther 311:190-203. 2004
    ..Its actions involve both blockade of postsynaptic 5-HT(1A) receptors and engagement of 5-HT(1A) autoreceptors...
  15. ncbi request reprint The role of dopamine D3 compared with D2 receptors in the control of locomotor activity: a combined behavioural and neurochemical analysis with novel, selective antagonists in rats
    Mark J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Psychopharmacology (Berl) 174:341-57. 2004
    ..The role of dopamine D(3)/D(2) receptors in the control of locomotion is poorly understood...
  16. ncbi request reprint S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: III. Actions in models of potential antidepressive and anxiolytic activity in comparison with ropinirole
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, Paris, France
    J Pharmacol Exp Ther 309:936-50. 2004
    ..Its actions are more pronounced than those of ropinirole and principally involve engagement of D(2) receptors...
  17. ncbi request reprint S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: II. Actions in rodent, primate, and cellular models of antiparkinsonian activity in comparison to ropinirole
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, Paris, France
    J Pharmacol Exp Ther 309:921-35. 2004
    ..Although activation of D(2) receptors is crucial to the motor actions of S32504, engagement of D(3) receptors contributes to its neuroprotective properties...
  18. ncbi request reprint Discriminative stimulus properties of S32504, a novel D3/D2 receptor agonist and antiparkinson agent, in rats: attenuation by the antipsychotics, aripiprazole, bifeprunox, N-desmethylclozapine, and by selective antagonists at dopamine D2 but not D3 recept
    Mark J Millan
    Department of Neuropharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290, Croissy sur Seine, Paris, France
    Psychopharmacology (Berl) 191:767-82. 2007
    ..J Pharmacol Exp Ther 309:936-950, 2004a; Millan et al., J Pharmacol Exp Ther 309:903-920, 2004b; Millan et al., J Pharmacol Exp Ther 309:921-935, 2004c)...
  19. ncbi request reprint Selective blockade of dopamine D(3) versus D(2) receptors enhances frontocortical cholinergic transmission and social memory in rats: a parallel neurochemical and behavioural analysis
    Mark J Millan
    Department of Psychopharmacology, Institut de Recherches Servier, Croissy Seine, France
    J Neurochem 100:1047-61. 2007
    ..These data support the pertinence of D(3) receptors as a target for treatment of disorders in which cognitive function is compromised...
  20. doi request reprint MicroRNA in the regulation and expression of serotonergic transmission in the brain and other tissues
    Mark J Millan
    IDR Servier, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Curr Opin Pharmacol 11:11-22. 2011
    ..The present article discusses the functionally and clinically important interplay amongst miRNAs and serotoninergic mechanisms in the brain, peripheral organs and cancerous tissue...
  21. doi request reprint The melatonergic agonist and clinically active antidepressant, agomelatine, is a neutral antagonist at 5-HT(2C) receptors
    Mark J Millan
    Department of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine, France
    Int J Neuropsychopharmacol 14:768-83. 2011
    ..It will be of interest to determine whether the neutral antagonist properties of agomelatine are related to its favourable clinical profile of antidepressant properties with few side-effects and no discontinuation syndrome...
  22. doi request reprint The dopamine D3 receptor antagonist, S33138, counters cognitive impairment in a range of rodent and primate procedures
    Mark J Millan
    Institut de Recherches Servier, Croissy sur Seine, France
    Int J Neuropsychopharmacol 13:1035-51. 2010
    ..These data underpin interest in D(3) receptor blockade as a strategy for improving cognitive performance in CNS disorders like schizophrenia and Parkinson's disease...
  23. doi request reprint From the cell to the clinic: a comparative review of the partial D₂/D₃receptor agonist and α2-adrenoceptor antagonist, piribedil, in the treatment of Parkinson's disease
    Mark J Millan
    Dept of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy Seine Paris, France
    Pharmacol Ther 128:229-73. 2010
    ..The article concludes by highlighting perspectives for clarifying the mechanisms of action of piribedil and other antiparkinson agents, and for optimizing their clinical exploitation...
  24. doi request reprint Dual- and triple-acting agents for treating core and co-morbid symptoms of major depression: novel concepts, new drugs
    Mark J Millan
    Psychopharmacology Department, Institut du Recherches Servier, Centre de Recherches de Croissy, Paris, France
    Neurotherapeutics 6:53-77. 2009
    ..This review discusses the discovery and development of dual- and triple-acting antidepressants, focusing on novel concepts and new drugs disclosed over the last 2 to 3 years...
  25. doi request reprint Cognitive impairment in schizophrenia: a review of developmental and genetic models, and pro-cognitive profile of the optimised D(3) > D(2) antagonist, S33138
    Mark J Millan
    Institut de Recherches Servier, Croissy sur Seine, France
    Therapie 63:187-229. 2008
    ..It also reviews developmental and genetic risk factors for schizophrenia and their experimental modeling in rodents, with a particular emphasis on sensorimotor gating and cognitive deficits...
  26. doi request reprint Signaling at G-protein-coupled serotonin receptors: recent advances and future research directions
    Mark J Millan
    Institut de Recherche Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
    Trends Pharmacol Sci 29:454-64. 2008
    ..In view of the diversity of transduction mechanisms engaged by 5-HT, much of this discussion is relevant to other classes of G-protein-coupled receptors...
  27. doi request reprint The melanin-concentrating hormone1 receptor antagonists, SNAP-7941 and GW3430, enhance social recognition and dialysate levels of acetylcholine in the frontal cortex of rats
    Mark J Millan
    Division of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine, France
    Int J Neuropsychopharmacol 11:1105-22. 2008
    ..This profile differentiates MCH1 receptor antagonists from conventional anxiolytic and antidepressant agents...
  28. ncbi request reprint S33138 (N-[4-[2-[(3aS,9bR)-8-cyano-1,3a,4,9b-tetrahydro[1] benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenyl-acetamide), a preferential dopamine D3 versus D2 receptor antagonist and potential antipsychotic agent: III. Actions in models of therapeutic activi
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    J Pharmacol Exp Ther 324:1212-26. 2008
    ..In comparison with clinically available agents, S33138 displays, thus, a distinctive and promising profile of potential antipsychotic properties...
  29. ncbi request reprint S33138 [N-[4-[2-[(3aS,9bR)-8-cyano-1,3a,4,9b-tetrahydro[1]-benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenylacetamide], a preferential dopamine D3 versus D2 receptor antagonist and potential antipsychotic agent: I. Receptor-binding profile and functional ac
    Mark J Millan
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    J Pharmacol Exp Ther 324:587-99. 2008
    ..In conclusion, S33138 possesses a distinctive receptor-binding profile and behaves, in contrast to clinically available antipsychotics, as a preferential antagonist at hD(3) versus hD(2) receptors...
  30. ncbi request reprint S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole
    Mark J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Paris, France
    J Pharmacol Exp Ther 309:903-20. 2004
    ..Although the D(3)/D(2) agonist and antiparkinsonian agent ropinirole mimicked the profile of S32504, it was less potent. In conclusion, S32504 is a potent and selective agonist at dopamine D(3) and D(2) receptors...
  31. ncbi request reprint The neurobiology and control of anxious states
    Mark J Millan
    Psychopharmacology Department, Centre de Rescherches de Croissy, Institut de Recherches IDR Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
    Prog Neurobiol 70:83-244. 2003
    ....
  32. ncbi request reprint Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization
    M J Millan
    Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France
    J Pharmacol Exp Ther 297:876-87. 2001
    ..6). In conclusion, piribedil displays essentially antagonist properties at cloned, human and cerebral, rat alpha(2)-ARs. Blockade of alpha(2)-ARs may, thus, contribute to its clinical antiparkinsonian profile...
  33. ncbi request reprint S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine
    M J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France
    J Pharmacol Exp Ther 298:565-80. 2001
    ..It enhances extracellular levels of 5-HT and NE throughout corticolimbic structures and selectively elevates dialysis levels of DA in frontal cortex versus subcortical regions...
  34. ncbi request reprint S33005, a novel ligand at both serotonin and norepinephrine transporters: II. Behavioral profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine
    M J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France
    J Pharmacol Exp Ther 298:581-91. 2001
    ..It exerts its actions more potently than venlafaxine and clomipramine, and its overall profile is distinct from those of citalopram and reboxetine...
  35. ncbi request reprint Selective blockade of neurokinin (NK)(1) receptors facilitates the activity of adrenergic pathways projecting to frontal cortex and dorsal hippocampus in rats
    M J Millan
    Institut de Recherches Servier, Psychopharmacology Department, Croissy sur Seine, Paris, France
    J Neurochem 76:1949-54. 2001
    ..Adrenergic mechanisms may, thus, be involved in the potential antidepressant and other functional properties of NK(1) receptor antagonists...
  36. ncbi request reprint Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes
    Mark J Millan
    Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    J Pharmacol Exp Ther 303:791-804. 2002
    ..In conclusion, an innovative multivariate analysis revealed marked heterogeneity in binding profiles of antiparkinson agents. Actions at sites other than hD(2) receptors likely participate in their (contrasting) functional profiles...
  37. ncbi request reprint Improving the treatment of schizophrenia: focus on serotonin (5-HT)(1A) receptors
    M J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, Croissy Seine, Paris, France
    J Pharmacol Exp Ther 295:853-61. 2000
    ....
  38. ncbi request reprint Anxiolytic properties of the selective, non-peptidergic CRF(1) antagonists, CP154,526 and DMP695: a comparison to other classes of anxiolytic agent
    M J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France
    Neuropsychopharmacology 25:585-600. 2001
    ..In conclusion, CP154,526 and DMP695 possess a common and distinctive profile of anxiolytic action expressed in the absence of an intrinsic influence upon monoamine release...
  39. ncbi request reprint The Vogel conflict test: procedural aspects, gamma-aminobutyric acid, glutamate and monoamines
    Mark J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Eur J Pharmacol 463:67-96. 2003
    ..Indeed, in view of its clinical relevance, broader exploitation of the Vogel conflict test in the identification of novel classes of anxiolytic agents, and in the determination of their mechanisms of action, would prove instructive...
  40. ncbi request reprint Descending control of pain
    Mark J Millan
    Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Prog Neurobiol 66:355-474. 2002
    ..Knowledge of descending pathways has increased exponentially in recent years, so this is an opportune moment to survey their operation and therapeutic relevance to the improved management of pain...
  41. doi request reprint S41744, a dual neurokinin (NK)1 receptor antagonist and serotonin (5-HT) reuptake inhibitor with potential antidepressant properties: a comparison to aprepitant (MK869) and paroxetine
    Mark J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Eur Neuropsychopharmacol 20:599-621. 2010
    ..In conclusion, S41744 is an innovative NK(1) antagonist/5-HT reuptake inhibitor justifying further evaluation for treatment of stress-related disorders...
  42. ncbi request reprint Blockade of serotonin 5-HT1B and 5-HT2A receptors suppresses the induction of locomotor activity by 5-HT reuptake inhibitors, citalopram and fluvoxamine, in NMRI mice exposed to a novel environment: a comparison to other 5-HT receptor subtypes
    Mark J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, France
    Psychopharmacology (Berl) 168:397-409. 2003
    ..Recently, we demonstrated that SSRIs, such as citalopram, enhance LA in mice exposed to a novel environment...
  43. ncbi request reprint The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways
    M J Millan
    Department of Psychopharmacology, Institut de Recherches Servier, Croissy Seine, France
    J Pharmacol Exp Ther 306:954-64. 2003
    ..In conclusion, in contrast to melatonin, agomelatine behaves as an antagonist at 5-HT2B and 5-HT2C receptors: blockade of the latter reinforces frontocortical adrenergic and dopaminergic transmission...
  44. ncbi request reprint N-methyl-D-aspartate receptor-coupled glycineB receptors in the pathogenesis and treatment of schizophrenia: a critical review
    M J Millan
    Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Curr Drug Targets CNS Neurol Disord 1:191-213. 2002
    ..This article reviews the complex role of GLY(B) sites/NMDA receptors and their endogenous ligands in the pathogenesis and treatment of psychotic states...
  45. ncbi request reprint Stereospecific blockade of marble-burying behaviour in mice by selective, non-peptidergic neurokinin1 (NK1) receptor antagonists
    M J Millan
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Sein, Paris, France
    Neuropharmacology 42:677-84. 2002
    ..Although the biological bases of this behaviour remain unclear, these observations underpin the contention that NK(1) receptors may be implicated in affective disorders...
  46. doi request reprint Neurokinin1 antagonists potentiate antidepressant properties of serotonin reuptake inhibitors, yet blunt their anxiogenic actions: a neurochemical, electrophysiological, and behavioral characterization
    Alain Gobert
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France
    Neuropsychopharmacology 34:1039-56. 2009
    ..Combined NK(1) receptor antagonism/5-HT reuptake inhibition may offer advantages in the management of depressed and anxious states...
  47. ncbi request reprint The selective neurokinin (NK)(1) antagonist, GR205,171, stereospecifically enhances mesocortical dopaminergic transmission in the rat: a combined dialysis and electrophysiological study
    Françoise Lejeune
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
    Brain Res 935:134-9. 2002
    ..Activation of mesocortical dopaminergic pathways may be involved in the influence of NK(1) antagonists upon mood...
  48. doi request reprint Cellular and behavioural profile of the novel, selective neurokinin1 receptor antagonist, vestipitant: a comparison to other agents
    Mauricette Brocco
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, Croissy Seine, Paris, France
    Eur Neuropsychopharmacol 18:729-50. 2008
    ..In conclusion, vestipitant is a potent NK(1) receptor antagonist: its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression...
  49. ncbi request reprint Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex
    Florence Loiseau
    Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290, Croissy sur Seine, Paris, France
    Psychopharmacology (Berl) 196:93-104. 2008
    ..5-HT6 receptor antagonists improve cognitive processes in rodents. However, their site(s) of action remains unexplored and their influence upon social memory has been little investigated...
  50. ncbi request reprint Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes
    Adrian Newman-Tancredi
    Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    J Pharmacol Exp Ther 303:815-22. 2002
    ..Although all show modest (agonist) activity at 5-HT(1A) sites, their contrasting actions at 5-HT(2A) and 5-HT(2C) sites may be of particular significance to their functional profiles in vivo...
  51. ncbi request reprint Differential modulation of efficiency in a food-rewarded "differential reinforcement of low-rate" 72-s schedule in rats by norepinephrine and serotonin reuptake inhibitors
    Anne Dekeyne
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Psychopharmacology (Berl) 162:156-67. 2002
    ..Indeed, several antidepressants have been shown to improve efficiency (ratio of reinforcement rate to response rate) in this model, either by decreasing response rates and/or by increasing reinforcement rates...
  52. pmc h5-HT(1B) receptor-mediated constitutive Galphai3-protein activation in stably transfected Chinese hamster ovary cells: an antibody capture assay reveals protean efficacy of 5-HT
    Adrian Newman-Tancredi
    Department of Psychopharmacology, Institut de Recherches Servier, 125, Chemin de Ronde, Croissy sur Seine, Paris 78290, France
    Br J Pharmacol 138:1077-84. 2003
    ....
  53. ncbi request reprint Antibody capture assay reveals bell-shaped concentration-response isotherms for h5-HT(1A) receptor-mediated Galpha(i3) activation: conformational selection by high-efficacy agonists, and relationship to trafficking of receptor signaling
    Adrian Newman-Tancredi
    Department of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine, France
    Mol Pharmacol 62:590-601. 2002
    ..In contrast, partial agonists favor h5-HT(1A) receptor signaling to Galpha(i3) over a wide concentration range, whereas inverse agonists inhibit constitutive Galpha(i3) activation...
  54. ncbi request reprint Stimulation by antipsychotic agents of mitogen-activated protein kinase (MAPK) coupled to cloned, human (h)serotonin (5-HT)(1A) receptors
    Didier Cussac
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Psychopharmacology (Berl) 162:168-77. 2002
    ..There is evidence that serotonergic mechanisms contribute to the functional profiles of antipsychotic drugs, several of which display affinity for human (h)5-HT(1A) receptors...
  55. ncbi request reprint Induction of hyperlocomotion in mice exposed to a novel environment by inhibition of serotonin reuptake. A pharmacological characterization of diverse classes of antidepressant agents
    Mauricette Brocco
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Pharmacol Biochem Behav 71:667-80. 2002
    ..Although an influence upon arousal and/or anxiety is likely related to the increase in LA, the functional significance of this response requires additional elucidation...
  56. ncbi request reprint Characterisation of Gs activation by dopamine D1 receptors using an antibody capture assay: antagonist properties of clozapine
    Didier Cussac
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    Eur J Pharmacol 485:111-7. 2004
    ..Employing this novel technique, the typical and atypical antipsychotics, clozapine and haloperidol, respectively, both exhibited antagonist properties at dopamine D1 receptors...
  57. doi request reprint Inhibitory and facilitory actions of isocyanine derivatives at human and rat organic cation transporters 1, 2 and 3: a comparison to human alpha 1- and alpha 2-adrenoceptor subtypes
    Anne Amphoux
    INSERM U952, 75005, Paris, France
    Eur J Pharmacol 634:1-9. 2010
    ....
  58. ncbi request reprint The selective serotonin(2A) receptor antagonist, MDL100,907, elicits a specific interoceptive cue in rats
    Anne Dekeyne
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Neuropsychopharmacology 26:552-6. 2002
    ..In conclusion, selective blockade of 5-HT(2A) receptors by MDL100,907 elicits a discriminative stimulus in rats which appears to be specifically mediated via 5-HT(2A) as compared with 5-HT(2B) and 5-HT(2C) receptors...
  59. ncbi request reprint The CRF1 receptor antagonist, DMP695, abolishes activation of locus coeruleus noradrenergic neurones by CRF in anesthetized rats
    Françoise Lejeune
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    Eur J Pharmacol 464:127-33. 2003
    ..These data demonstrate antagonist properties of DMP695 at central CRF(1) receptors excitatory to ascending noradrenergic neurones, an action which may contribute to its distinctive profile of anxiolytic properties...
  60. ncbi request reprint Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor
    Adrian Newman-Tancredi
    Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
    J Pharmacol Exp Ther 303:805-14. 2002
    ..In conclusion, antiparkinson agents display diverse agonist and antagonist properties at multiple subtypes of D(2)-like receptor and alpha(1)/alpha(2)-AR, actions, which likely contribute to their contrasting functional profiles...
  61. ncbi request reprint Differential activation of Gq/11 and Gi(3) proteins at 5-hydroxytryptamine(2C) receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonist-directed trafficking
    Didier Cussac
    Institut de Recherches Servier, Psychopharmacology Department, Chemin de Ronde, Croissy Seine, Paris, France
    Mol Pharmacol 62:578-89. 2002
    ..In conclusion, h5-HT(2C) receptors couple to both Gq/11 and Gi(3) in CHO cells, and efficacy for G protein subtype activation is both ligand- and receptor reserve-dependent...
  62. ncbi request reprint Discriminative stimulus properties of the selective and highly potent alpha2-adrenoceptor agonist, S18616, in rats: mediation by the alpha2A subtype, and blockade by the atypical antidepressants, mirtazapine and mianserin
    Anne Dekeyne
    Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125, Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
    Neuropharmacology 51:718-26. 2006
    ..In conclusion, S18616 elicits a robust DS in rats that principally reflects engagement of alpha2A-ARs. This novel procedure should prove useful in the characterisation of psychoactive drugs which interact with alpha2-ARs...
  63. ncbi request reprint Antidepressant-like properties of the anti-Parkinson agent, piribedil, in rodents: mediation by dopamine D2 receptors
    Mauricette Brocco
    Psychopharmacology Department, Servier Research Institute, Croissy Research Center, Paris, France
    Behav Pharmacol 17:559-72. 2006
    ..In conclusion, principally via recruitment of D2 receptors, piribedil exerts robust and specific antidepressant-like actions in diverse rodent models...
  64. ncbi request reprint Ligand modulation of [35S]GTPgammaS binding at human alpha(2A), alpha(2B) and alpha(2C) adrenoceptors
    Valérie Audinot
    Département de Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    Cell Signal 14:829-37. 2002
    ..Moreover, they emphasize the continuing need for alpha(2)-AR subtype-selective antagonists in order to define further the roles and therapeutic relevance of halpha(2A)-, halpha(2B)-, and halpha(2C)-AR...
  65. ncbi request reprint Quantification and pharmacological characterization of dialysate levels of noradrenaline in the striatum of freely-moving rats: release from adrenergic terminals and modulation by alpha2-autoreceptors
    Alain Gobert
    Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, Croissy Seine 78290, France
    J Neurosci Methods 140:141-52. 2004
    ..A role of dopaminergic terminals in the reuptake of NA likely explains the elevation in its levels elicited by DA reuptake-inhibitors and D3/D2 receptor antagonists...
  66. ncbi request reprint Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols
    Jean Louis Peglion
    Institut de Recherches Servier, 11 rue des Moulineaux, 92150 Suresnes et 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    J Med Chem 45:165-76. 2002
    ....
  67. ncbi request reprint Influence of positive allosteric modulators on GABA(B) receptor coupling in rat brain: a scintillation proximity assay characterisation of G protein subtypes
    Clotilde Mannoury La Cour
    Psychopharmacology Department, Institut de Recherche Servier, Croissy sur Seine, France
    J Neurochem 105:308-23. 2008
    ..PAMs more markedly enhanced efficacy of coupling to Go versus Gi(1/3). It will be of interest to confirm these observations employing complementary techniques and to evaluate their potential therapeutic significance...
  68. doi request reprint Modulations of the amide function of the preferential dopamine D3 agonist (R,R)-S32504: improvements of affinity and selectivity for D3 versus D2 receptors
    Jean Louis Peglion
    Institut de Recherches Servier, Chemistry B Departement, Suresnes, France
    Bioorg Med Chem Lett 19:2133-8. 2009
    ..Conversely, when the primary amide function was integrated in a lactam ring, an enhancement of affinity and selectivity was attained for the five-membered ring lactam but also for its five-membered ring lactone analogue...
  69. ncbi request reprint Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols
    Didier Cussac
    Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy Sur Seine Paris, France
    Naunyn Schmiedebergs Arch Pharmacol 365:242-52. 2002
    ..Although several antagonists clearly differentiated h5-HT2C from h5-HT2B receptors under these conditions, highly selective agonists remain to be identified...
  70. doi request reprint Actions of novel agonists, antagonists and antipsychotic agents at recombinant rat 5-HT6 receptors: a comparative study of coupling to G alpha s
    Delphine S Dupuis
    Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Eur J Pharmacol 588:170-7. 2008
    ..Though 5-HT6 receptor blockade is not indispensable for therapeutic efficacy, it may well play a role in the functional actions of certain antipsychotic agents...
  71. doi request reprint Blockade of dopamine D(3) receptors in frontal cortex, but not in sub-cortical structures, enhances social recognition in rats: similar actions of D(1) receptor agonists, but not of D(2) antagonists
    Florence Loiseau
    Institut de Recherches Servier, Department of Psychopharmacology, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
    Eur Neuropsychopharmacol 19:23-33. 2009
    ..63), into the FCX though it was also active (0.63) in the nucleus accumbens. These data suggest that D(3) receptors modulating social recognition are localized in FCX, and underpin their pertinence as targets for antipsychotic agents...
  72. doi request reprint S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models
    Anne Dekeyne
    Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, 125 Chemin de Ronde, Croissy Seine, France
    Psychopharmacology (Berl) 199:549-68. 2008
    ..Serotonin (5-HT)(2C) receptors are implicated in the control of mood, and their blockade is of potential interest for the management of anxiodepressive states...
  73. doi request reprint Discriminative stimulus properties of the atypical antidepressant, mirtazapine, in rats: a pharmacological characterization
    Anne Dekeyne
    Department of Neuropharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy 125 Chemin de Ronde, 78290, Croissy sur Seine, Paris, France
    Psychopharmacology (Berl) 203:329-41. 2009
    ..Though interoceptive properties of antidepressants have been described, discriminative stimulus (DS) properties of mirtazapine, which does not affect monoamine reuptake, remain uncharacterized...
  74. doi request reprint Signaling pathways leading to phosphorylation of Akt and GSK-3β by activation of cloned human and rat cerebral D₂and D₃ receptors
    Clotilde Mannoury La Cour
    Institut de Recherches Servier, Psychopharmacology Department, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Mol Pharmacol 79:91-105. 2011
    ..However, significant differences were seen regarding the involvement of PLC, calmodulin, and ERK1/2...
  75. ncbi request reprint [Dopamine D3 receptors as a novel target for improving the treatment of schizophrenia]
    Mark J Millan
    IDR Servier, Department de Psychopharmacologie, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    Med Sci (Paris) 21:434-42. 2005
    ..The first clinical studies for the evaluation of this hypothesis have recently got underway...