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

European Neuropsychopharmacology

Volumn 20, Issue 9, 2010, Pages 599-621

  Millan, Mark J ^a   Dekeyne, Anne ^a   Gobert, Alain ^a   Mannoury la Cour, Clotilde ^a   Brocco, Mauricette ^a   Rivet, Jean Michel ^a   Di Cara, Benjamin ^a   Lejeune, Françoise ^a   Cremers, Thomas I ^b   Flik, Gunnar ^b   de Jong, Trynke R ^c   Olivier, Berend ^c   de Nanteuil, Guillaume ^a  

^a INSTITUT DE RECHERCHES SERVIER   (France)

^b CHARLES RIVER LABORATORIES   (United States)

^c UTRECHT UNIVERSITY   (Netherlands)

Author keywords

Antidepressant; ; Aprepitant; ; Paroxetine; Serotonin transporter; ; Substance P;

Indexed keywords

2 PIPERAZIN 1 YL INDAN 2 CARBOXYLIC ACID (3 CHLORO 5 FLUOROBENZYL)METHYLAMIDE; 5 AMINOVALERYLSUBSTANCE P [7-11][9 PROLINE 10 (N METHYLLEUCINE)]; APREPITANT; MITOGEN ACTIVATED PROTEIN KINASE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; NEUROKININ 1 RECEPTOR; NEUROKININ 1 RECEPTOR ANTAGONIST; PAROXETINE; S 41744; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; SUBSTANCE P; UNCLASSIFIED DRUG; VOFOPITANT;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; CORPUS STRIATUM; DEPRESSION; DRUG DOSE COMPARISON; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; FEAR; FORCED SWIMMING TEST; FRONTAL CORTEX; GERBIL; GUINEA PIG; HIPPOCAMPUS; HUMAN; HUMAN CELL; LICKING; MALE; MOUSE; NEUROMODULATION; NONHUMAN; PRIORITY JOURNAL; RAT; ROTAROD TEST; SOCIAL INTERACTION; STRESS; VOCALIZATION;

EID: 77955092308     PISSN: 0924977X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.euroneuro.2010.04.003     Document Type: Article

References (115)

1. 1 receptor-mediated apoptosis in glioblastomas. J. Neurochem. 2009, 109:1079-1086.
2. Amadoro G., Pieri M., Ciotti M.T., Carunchi I., Canu N., Calissano P., Zona C., Severini C. Substance P provides neuroprotection in cerebellar granule cells through Akt and MAPK/Erk activation: evidence for the involvement of the delayed rectifier potassium current. Neuropharmacology 2007, 52:1366-1377.
3. 1 receptor antagonist. Eur. J. Pharmacol. 2001, 412:255-264.
4. Bassi G.S., Nobre M.J., Carvalho M.C., Brandão M.L. Substance P injected into the dorsal periaqueductal gray causes anxiogenic effects similar to long-term isolation as assessed by ultrasound vocalizations measurements. Behav. Brain Res. 2007, 182:301-307.
5. Bilkei-Gorzo A., Racz I., Michel K., Zimmer A. Diminished anxiety- and depression-related behaviours in mice with selective deletion of the Tac1 gene. J. Neurosci. 2002, 22:10046-10052.
6. Blier P., Gobbi G., Haddjeri N., Santarelli L., Mathew G., Hen R. Impact of substance P receptor antagonism on the serotonin and norepinephrine systems: relevance to the antidepressant/anxiolytic response. J. Psychiatry Neurosci. 2004, 29:208-218.
7. Bourin M., Chue P., Guillon Y. Paroxetine: a review. CNS Drug Rev. 2001, 7:25-47.
8. 1 imidazoline receptors involved in cardiovascular regulation: where are we and where are we going? Ann. N.Y. Acad. Sci. 2003, 1009:228-233.
9. 1 receptor) antagonist L-760735 inhibits neonatal vocalisations in guinea-pigs. Neuropharmacology 2001, 41:130-137.
10. 1 receptor antagonist, vestipitant: a comparison to other agents. Eur. Neuropsychopharmacol. 2008, 18:729-750.
11. 2C receptor antagonist. Biol. Psychiatry 2007, 62:1111-1118.
12. Castagliuolo I., Valenick L., Liu J., Pothoulaki C. Epidermal growth factor receptor transactivation mediates substance P-induced mitogenic responses in U373MG cells. J. Biol. Chem. 2000, 275:26545-26550.
13. 1A agonist 8-OH-DPAT in the social interaction test in gerbils. Brain Res. 2001, 915:170-175.
14. 1 receptor antagonist in the mouse forced swimming test. Behav. Brain Res. 2006, 172:256-263.
15. Commons, K.G., 2010. Neuronal pathways linking substance P to drug addiction and stress. Brain Res. 1314, 175-182.
16. Commons K.G., Valentino R.J. Cellular basis for the effects of substance P in the periaqueductal gray and dorsal raphe nucleus. J. Comp. Neurol. 2002, 447:82-97.
17. Cremers T.I., Dremencov E., Bosker F.J., Westerink B.H. Oxazepam and temazepam attenuate paroxetine-induced elevation of serotonin levels in guinea-pig hippocampus. Int. J. Neuropsychopharmacol. 2010, 13(6):807-811.
18. 2C antagonists: mechanistic studies. Neuropsychopharmacology 2007, 32:1550-1557.
19. Cryan J.F., Valentino R.J., Lucki I. Assessing substrates underlying the behavioral effects of antidepressants using the modified rat forced swimming test. Neurosci. Biobehav. Rev. 2005, 29:547-569.
20. Curran M.P., Robinson D.M. Aprepitant: a review of its use in the prevention of nausea and vomiting. Drugs 2009, 69:1853-1878.
21. 1 receptor antagonists under investigation for the treatment of affective disorders. Expert Opin. Investig. Drugs 2006, 15:479-486.
22. Dableh L.J., Yashpal K., Rochford J., Henry J.L. Antidepressant-like effects of neurokinin receptor antagonists in the forced swim test in the rat. Eur. J. Pharmacol. 2005, 507:99-105.
23. 2C receptors. Neuropharmacology 2000, 39:114-1117.
24. 1 antagonists. J. Pharmacol. Exp. Ther. 2002, 301:536-542.
25. Ebner K., Rupniak N.M., Saria A., Singewald N. Substance P in the medial amygdala: emotional stress-sensitive release and modulation of anxiety-related behavior in rats. Proc. Natl. Acad. Sci. USA 2004, 101:4280-4285.
26. Ebner K., Sartori S.B., Singewald N. Tachykinin receptors as therapeutic targets in stress-related disorders. Curr. Pharmacol. Design 2009, 15:1647-1674.
27. Ebner K., Singewald G.M. Stress-induced release of substance P in the locus coeruleus modulates cortical noradrenaline release. Naunyn-Schmiedeberg's Arch. Pharmacol. 2007, 376:73-82.
28. 1 receptors. Biochem. Pharmacol. 2007, 73:259-269.
29. Feuring M., Lee Y., Orlowski L.H., Michiels N., De Smet M., Majumdar A.K., Petty K.J., Goldberg M.R., Murphy M.G., Gottesdiener K.M., Hesney M., Brackett L.E., Wehling M. Lack of effect of aprepitant on digoxin pharmacokinetics in healthy subjects. J. Clin. Pharmacol. 2003, 43:912-917.
30. Fineberg N.A., Gale T.M. Evidence-based pharmacotherapy of obsessive-compulsive disorder. Int. J. Neuropsychopharmacol. 2005, 8:107-129.
31. 1) receptor knock-out mice mimic antidepressant-induced desensitization. Neuroscience 2001, 15:8188-8197.
32. 18F]SPA-RQ. Biol. Psychiatry 2009, 66:94-97.
33. Furmark T., Appel L., Michelgård A., Wahlstedt K., Ahs F., Zancan S., Jacobsson E., Flyckt K., Grohp M., Bergström M., Pich E.M., Nilsson L.G., Bani M., Långström B., Fredrikson M. Cerebral flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram or placebo. Biol. Psychiatry 2005, 58:132-142.
34. 1 receptor antagonism as a possible therapy for alcoholism. Science 2008, 319:1536-1539.
35. Gether U., Andersen P.H., Larsson O.M., Schousboe A. Neurotransmitter transporters: molecular function of important drug targets. Trends Pharmacol. Sci. 2008, 27:375-383.
36. 1 receptor antagonism requires norepinephrine to increase serotonin function. Eur. Neuropsychopharmacology 2007, 17:328-338.
37. 1 antagonists potentiate antidepressant properties of serotonin reuptake inhibitors, yet blunt their anxiogenic actions: a neurochemical, electrophysiological and behavioural characterization. Neuropsychopharmacology 2009, 34:1039-1056.
38. 1A receptor agonists and antagonists: A comparison to adrenergic and dopaminergic neurones in individual rats. J. Pharmacol. Exp. Ther. 1995, 273:1032-1046.
39. 1 receptor binding profile in gerbil and human brain. Br. J. Pharmacol. 2006, 148:39-45.
40. 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice. J. Neurochem. 2004, 89:54-63.
41. 1A autoreceptors in mice. J. Neurochem. 2005, 95:1713-1723.
42. 1 receptor activation within the dorsal raphe nucleus controls serotonin release in the mouse frontal cortex. Mol. Pharmacol. 2007, 72:1411-1418.
43. 1) receptor antagonist administration: a review. Curr. Drug Targets 2006, 7:187-201.
44. 1 receptors enhances serotonin neurotransmission. Biol. Psychiatry 2001, 50:191-199.
45. Haddjeri N., Blier P. Neurokinin-1 receptor antagonists modulate brain noradrenaline and serotonin interactions. Eur. J. Pharmacol. 2008, 600:64-70.
46. Halaris A., Piletz J.E. Relevance of imidazoline receptors and agmatine to psychiatry: a decade of progress. Ann. N. Y. Acad. Sci. 2003, 1009:1-20.
47. Heldt S.A., Davis M., Ratti E., Corsi M., Trist D., Ressler K.J. Anxiolytic-like effects of the neurokinin1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils. Behav. Pharmacol. 2009, 20:584-595.
48. 1-/-) and wildtype mice: exploratory behaviour and extracellular noradrenaline concentration in the cerebral cortex of anaesthetised subjects. Neuropharmacology 2005, 48:706-719.
49. Keith C.T., Borisy A.A., Stockwell B.R. Multicomponent therapeutics for networked systems. Nat. Rev. Drug Discov. 2005, 4:71-78.
50. Keller M., Montgomery S., Ball W., Morrison M., Snavely D., Liu G., Hargreaves R., Hietala J., Lines C., Beebe K., Reines S. Lack of efficacy of the substance P (neurokinin1) receptor antagonist aprepitant in the treatment of major depressive disorder. Biol. Psychiatry 2006, 59:216-223.
51. Kramer M.S., Cutler N., Feighner J., Shrivastava R., Carman J., Sramek J.J., Reines S.A., Liu G., Snavely D., Wyatt-Knowles E., Hale J.J., Mills S.G., MacCoss M., Swain C.J., Harrison T., Hill R.G., Hefti F., Scolnick E.M., Casieri M.A., Chicchi G.G., Sadowski S., Williams A.R., Hewson L., Smith D., Carlson E.J., Hargreaves R.J., Rupniak N.M. Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science 1998, 281:1640-1645.
52. 1) receptor antagonist in major depression. Neuropsychopharmacology 2004, 29:385-392.
53. Lacoste B., Riad M., Ratté M.O., Boye S.M., Lévesque D., Descarries L. Trafficking of neurokinin-1 receptors in serotonin neurons is controlled by substance P within the rat dorsal raphe nucleus. Eur. J. Neurosci. 2009, 29:2303-2314.
54. Leffler A., Ahlstedt I., Engberg S., Svensson A., Billger M., Oberg L., Bjursell M.K., Lindstöm E., von Mentzer B. Characterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3. Biochemical Pharmacol. 2009, 77:1522-1530.
55. Lejeune F., Gobert A., Millan M.J. The selective NK1 antagonist, GR205, 171, stereospecifically enhances mesocortical dopaminergic transmission in the rat: a combined dialysis and electrophysiological study. Brain Res. 2002, 935:134-139.
56. Lessard A., Pickel V.M. Subcellular distribution and plasticity of neurokinin-1 receptors in the rat substantia nigra and ventral tegmental area. Neuroscience 2005, 135:1309-1323.
57. 1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy. J. Pharmacol. Exp. Ther. 2007, 322:1286-1293.
58. 1 receptor antagonists in two conflict procedures in rats. Behav. Pharmacol. 2003, 14:447-455.
59. 1 receptor antagonist GR205171 in impulsive-related behaviour in rats. Psychopharmacology 2005, 182:24-32.
60. 1 receptors in rats. Neuroreport 2002, 13:1809-1813.
61. Maggi C.A. The mammalian tachykinin receptors. Gen. Pharmacol. 1995, 26:911-944.
62. 1 receptor antagonism and the neural processing of emotional information in healthy volunteers. Int. J. Neuropsychopharmacol. 2009, 12:1261-1274.
63. McIntyre M., Moral M.A. Augmentation in treatment-resistant depression. Drugs Fut. 2006, 31:1069-1081.
64. Mico J.A., Ardid D., Berrocoso E., Eschalier A. Antidepressants and pain. Trends Pharmacol. Sci. 2006, 27:348-354.
65. Millan M.J. The induction of pain: an integrative review. Prog. Neurobiol. 1999, 57:1-164.
66. Millan M.J. The neurobiology and control of anxious states. Prog. Neurobiol. 2003, 70:83-244.
67. Millan M.J. Multi-target strategies for the improved treatment of depressive states: conceptual foundations and neuronal substrates, drug discovery and therapeutic application. Pharmacol. Ther. 2006, 110:135-370.
68. Millan M.J., Gobert A., Lejeune F., Newman-Tancredi A., Rivet J.-M., Bosc C., Auclair A., Peglion J.-L. S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptorial, electrophysiological and neurochemical profile in comparison to venlafaxine, reboxetine, citalopram and clomipramine. J. Pharmacol. Exp. Ther. 2001, 298:565-580.
69. 1) receptor antagonists. Neuropharmacology 2002, 42:677-684.
70. 1 receptors facilitates the activity of adrenergic pathways projecting to frontal cortex and dorsal hippocampus in rats. J. Neurochem. 2001, 76:1949-1954.
71. Millan M.J., Lejeune F., Gobert A. Reciprocal autoreceptor and heteroceptor control of serotonergic, dopaminergic and adrenergic transmission in frontal cortex: a review, and relevance to the actions of antidepressant agents. J. Psychopharmacol. 2000, 14:114-138.
72. 2 receptor antagonist and potential antipsychotic agent. I. Receptor-binding profile and functional actions at G-protein coupled receptors. J. Pharmacol. Exp. Ther. 2008, 324:587-599.
73. Millan M.J., Panayi F., Rivet J.-M., Di Cara B., Cistarelli L., Billiras R., Girardon S., Gobert A. The role of microdialysis in drug discovery: focus on antipsychotic agents. Handbook of Microdialysis 2007, 16:485-511. Academic Press, Amsterdam. B.H.C. Westerink, T.I.F.H. Cremers (Eds.).
74. 2A receptors mediate the induction of locomotor activity elicited by reuptake inhibitors in mice exposed to a novel environment: a pharmacological analysis. Psychopharmacology 2003, 68:397-409.
75. Molewijk H.E., Hartog K., van der Poel A.M., Mos J., Olivier B. Reduction of guinea pig pup isolation calls by anxiolytic and antidepressant drugs. Psychopharmacology 1996, 128:31-38.
76. Morcuande S., Gadd C.A., Peters M., Moss H., Harris E.A., Sheasby A., Fisher A.S., De Felipe C., Mantyh P.W., Rupniak N.M.J., Giese P.K., Hunt S.P. Increased neurogenesis and brain-derived neurotrophic factor in neurokinin-1 receptor gene knockout mice. Eur. J. Neurosci. 2003, 18:1828-1836.
77. Morphy R., Rankovic Z. Designing multiple ligands-medicinal chemistry strategies and challenges. Curr. Pharm. Des. 2010, 15:587-600.
78. 1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest. New Drugs 2010, 28:187-193.
79. Nicolas L., Kolb Y., Prinssen E. A combined marble burying-locomotor activity test in mice: a practical screening test with sensitivity to different classes of anxiolytics and antidepressants. Eur. J. Pharmacol. 2006, 547:106-115.
80. 1 receptors in the progression of human gliomas. Life Sci. 2000, 67:985-1001.
81. Partridge W.M. Blood-brain barrier drug targeting: the future of brain drug development. Mol. Interv. 2003, 3:90-105.
82. Placenza F.M., Fletcher P.J., Vaccarino F.J., Erb S. Effects of central neurokinin-1 receptor antagonism on cocaine- and opiate-induced locomotor activity and self-administration behaviour in rats. Pharmacol. Biochem. Behav. 2006, 84:94-101.
83. Quartara L., Altamura M., Evangelista S., Maggi C.A. Tachykinin receptor antagonists in clinical trials. Expert Opin. Investig. Drugs 2009, 18:1843-1864.
84. 1 receptors attenuates stress-induced rise of extracellular noradrenaline and dopamine in the rat and gerbil medial prefrontal cortex. J. Neurosci. Res. 2006, 84:961-968.
85. 1A or 5-HT re-uptake site blockade. Neuropharmacology 1999, 38:1409-1419.
86. 1A receptor antagonists in the dorsal raphe pathway: role of somatodendritic autoreceptors. J. Neurochem. 1997, 68:2593-2603.
87. Rupniak N.M., Carlson E., Boyce S., Webb J.K., Hill R.G. Enantioselective inhibition of the formalin paw late phase by the NK1 receptor antagonist L-733, 060 in gerbils. Pain 1996, 67:189-195.
88. 1) receptors attenuates neonatal vocalisation in guinea-pigs and mice. Neuropharmacology 2000, 39:1413-1421.
89. 1) receptors by GR205171, RP67580, SR140333 and NKP-608. Neuropharmacology 2003, 45:231-241.
90. 1) receptor in assays for antidepressant and anxiolytic drugs. Behav. Pharmacol. 2001, 12:497-508.
91. 1 receptor) antagonists SR140333 and GR205171: a comparative study using mdr1a-/-and mdr1a+/+ mice. Behav. Pharmacol. 2003, 14:457-463.
92. 1) receptor antagonist L-760735 inhibits fear conditioning in gerbils. Neuropharmacology 2003, 44:516-523.
93. 1 antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants. Bioog. Med. Chem. Lett. 2002, 12:261-264.
94. 1 antagonists-serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and Activity of benzoloxyphenethyl piperazine derivatives. Bioog. Med. Chem. Lett. 2002, 12:3195-3198.
95. Saarto T., Wiffen P.J. Antidepressants for neuropathic pain. Cochrane Database Syst. Rev. 2007, 4. CD005454.
96. 3 binding sites. Neuroscience 2003, 116:761-773.
97. Santarelli L., Gobbi G., Debs P., Sibille E., Blier P., Hen R., Heath M.J.S. Genetic and pharmacological disruption of neurokinin 1 receptor function decreases anxiety-related behaviors and increases serotonergic function. Proc. Natl. Acad. Sci. USA 2001, 98:1912-1917.
98. 1 receptor in the brain: pharmacology and putative functions. Eur. J. Pharmacol. 1999, 375:51-60.
99. 1 receptor antagonist L-822429. J. Neurochem. 2008, 106:2476-2488.
100. Smith B.J., Doran A.C., McLean S., Tingley F.D., O'Neill B.T., Kajiji S.M. P-glycoprotein efflux at the blood-brain barrier mediates differences in brain disposition and pharmacodynamic between two structurally related neurokinin-1 receptor antagonists. J. Pharmacol. Exp. Ther. 2001, 298:1252-1259.
101. Smith D.W., Hewson L., Fuller P., Williams A.R., Wheeldon A., Rupniak N.M. The substance P antagonist L-760, 735 inhibits stress-induced NK1 receptor internalisation in the basolateral amygdala. Brain Res. 1999, 848:90-95.
102. Smith K.L., Jessop D.S., Finn D.P. Modulation of stress by imidazoline binding sites: implications for psychiatric disorders. Stress 2009, 12:97-114.
103. Sun J., Ramnath R.D., Tamizhselvi R., Bhatia M. Role of protein kinase C and phosphoinositide 3-kinase-Akt in substance P-induced proinflammatory pathways in mouse macrophages. FASEB J. 2009, 23:997-1010.
104. Tang S.W., Helmeste D. Paroxetine. Exp. Opin. Pharmacol. Ther. 2008, 9:787-794.
105. Tauscher J., Kielbasa W., Iyengar S., Vandenhende F., Peng X., Mozley D., Gehlert D.R., Marek G. Development of the 2nd generation neurokinin-1 receptor antagonist LY686017 for social anxiety disorder. Eur. Neuropsychopharmacol. 2010, 10:1016/j.euroneuro.2009.10.005.
106. Thomas A., Burant A., Bui N., Graham D., Yuva-Paylor L.A., Paylor R. Marble burying reflects a repetitive and perseverative behavior more than novelty-induced anxiety. Psychopharmacology 2009, 204:361-373.
107. Valentino R.J., Commons K.G. Peptides that fine-tune the serotonin system. Neuropeptides 2005, 39:1-8.
108. 1 receptor) antagonist L-760735 and clomipramine on endocrine and behavioral parameters. Psychopharmacology 2005, 181:207-216.
109. 1 receptor antagonists. Neuropsychopharmacology 2002, 27:371-379.
110. Wallace-Boone T.L., Newton A.E., Wright R.N., Lodge N.J., McElroy J.F. Behavioral and pharmacological validation of the gerbil forced-swim test: effects of neurokinin-1 receptor antagonists. Neuropsychopharmacology 2008, 33:1919-1928.
111. Wick K.M., Jongen-Relo A., Groth I., Gross G. The guinea pig forced swim test as a new behavioral despair model to characterize potential antidepressants. Psychopharmacology 2007, 195:95-102.
112. Wong E.H., Nikam S.S., Shahid M. Multi- and single-target agents for major psychiatric diseases: therapeutic opportunities and challenges. Curr. Opin. Investig. Drugs 2008, 9:28-36.
113. Yamaguchi K., Richardson M.D., Bigner D.D., Kwatra M.M. Signal transduction through substance P receptor in human glioblastoma cells: role for Src and PKCdelta. Cancer Chemother. Pharmacol. 2005, 56:585-593.
114. 1) receptors: a model of attention deficit hyperactivity disorder. Neuropharmacology 2009, 57:627-635.
115. Zhang M.Y., Hughes Z.A., Kerns E.H., Lin Q., Beyer C.E. Development of liquid chromatography/tandem mass spectrometry method for the quantitation of acetylcholine and related neurotransmitters in brain microdialysis samples. J. Pharm. Biomed. Anal. 2007, 44:586-593.