WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol- 2(3H)-one]: A novel dopamine D2 receptor partial agonist/serotonin reuptake inhibitor with preclinical antipsychotic-like and antidepressant-like activity

Journal of Pharmacology and Experimental Therapeutics

Volumn 332, Issue 1, 2010, Pages 190-201

  Brennan, Julie Adams ^a   Graf, Radka ^a   Grauer, Steven M ^a   Navarra, Rachel L ^a   Pulicicchio, Claudine M ^a   Hughes, Zoë A ^a   Lin, Qian ^a   Wantuch, Caitlin ^a   Rosenzweig Lipson, Sharon ^a   Pruthi, Farhana ^a   Lai, Margaret ^a   Smith, Deborah ^a   Goutier, Wouter ^b   Van De Neut, Martina ^b   Robichaud, Albert J ^a   Rotella, David ^a   Feenstra, Rolf W ^b   Kruse, Chris ^b   Broqua, Pierre ^b   Beyer, Chad E ^a   McCreary, Andrew C ^b   Pausch, Mark H ^a   Marquis, Karen L ^a   more..

^a PFIZER INC   (United States)

^b Solvay Pharmaceuticals Inc   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

7 [4 [3 (1H INDEN 3 YL)PROPYL]PIPERAZIN 1 YL] 1,3 BENZOXAZOL 2(3H) ONE; APOMORPHINE; ARIPIPRAZOLE; DOPAMINE 2 RECEPTOR; DOPAMINE 2 RECEPTOR STIMULATING AGENT; OXIDOPAMINE; SEROTONIN; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; UNCLASSIFIED DRUG; WS 50030;

ANIMAL BEHAVIOR; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; AVOIDANCE BEHAVIOR; CATALEPSY; CLIMBING; CONTROLLED STUDY; DOSE RESPONSE; DRUG ACTIVITY; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; EMBRYO; HUMAN; HUMAN CELL; HYPERACTIVITY; IN VITRO STUDY; MALE; MOUSE; NONHUMAN; OLFACTORY BULBECTOMY; PREDICTION; PREFRONTAL CORTEX; PRIORITY JOURNAL; ROTATION; SINGLE DRUG DOSE; SUBSTANTIA NIGRA;

ANIMALS; ANTIDEPRESSIVE AGENTS; ANTIPSYCHOTIC AGENTS; AVOIDANCE LEARNING; BEHAVIOR, ANIMAL; BENZOXAZOLES; BRAIN; CHO CELLS; CRICETINAE; CRICETULUS; DOPAMINE; DOPAMINE AGONISTS; DRUG EVALUATION, PRECLINICAL; HUMANS; INDENES; MALE; MICE; MICE, INBRED STRAINS; MICRODIALYSIS; MOTOR ACTIVITY; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; RECEPTOR, SEROTONIN, 5-HT1A; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTOR, SEROTONIN, 5-HT2B; RECEPTORS, DOPAMINE D2; SEROTONIN; SEROTONIN UPTAKE INHIBITORS; TRANSFECTION;

EID: 73949093734     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.109.157388     Document Type: Article

References (42)

1. Arnt J (1982) Pharmacological specificity of conditioned avoidance response inhibition in rats: inhibition by neuroleptics and correlation to dopamine receptor blockade. Acta Pharmacol Toxicol (Copenh) 51:321-329.
2. Beyer CE, Boikess S, Luo B, and Dawson LA (2002) Comparison of the effects of antidepressants on norepinephrine and serotonin concentrations in the rat frontal cortex: an in-vivo microdialysis study. J Psychopharmacol 16:297-304.
3. Bressan RA and Crippa JA (2005) The role of dopamine in reward and pleasure behavior-review of data from preclinical research. Acta Psychiatr Scand Suppl (427):14-21.
4. Bunzow JR, Van Tol HH, Grandy DK, Albert P, Salon J, Christie M, Machida CA, Neve KA, and Civelli O (1988) Cloning and expression of a rat D2 dopamine receptor cDNA. Nature 336:783-787.
5. Cassano GB, Fagiolini A, Lattanzi L, Monteleone P, Niolu C, Sacchetti E, Siracusano A, and Vita A (2007) Aripiprazole in the treatment of schizophrenia: a consensus report produced by schizophrenia experts in Italy. Clin Drug Investig 27:1-13.
6. Cheng Y and Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
7. Dawson LA, Nguyen HQ, Smith DI, and Schechter LE (2000) Effects of chronic fluoxetine treatment in the presence and absence of (±)pindolol: a microdialysis study. Br J Pharmacol 130:797-804.
8. Deecher DC, Beyer CE, Johnston G, Bray J, Shah S, Abou-Gharbia M, and Andree TH (2006) Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther 318:657-665.
9. Dunlop J, Sabb AL, Mazandarani H, Zhang J, Kalgaonker S, Shukhina E, Sukoff S, Vogel RL, Stack G, Schechter L, et al. (2005) WAY-163909 [(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activity. J Pharmacol Exp Ther 313:862-869.
10. Dunlop J, Zhang Y, Smith DL, and Schechter LE (1998) Characterization of 5-HT1A receptor functional coupling in cells expressing the human 5-HT1A receptor as assessed with the cytosensor microphysiometer. J Pharmacol Toxicol Methods 40:47-55.
11. Emilien G, Septien L, Brisard C, Corruble E, and Bourin M (2007) Bipolar disorder: how far are we from a rigorous definition and effective management? Prog Neuropsychopharmacol Biol Psychiatry 31:975-996.
12. Hirst WD, Andree TH, Aschmies S, Childers WE, Comery TA, Dawson LA, Day M, Feingold IB, Grauer SM, Harrison BL, et al. (2008) Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1a receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)- N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405). J Pharmacol Exp Ther 325:134-145.
13. Huang XP, Setola V, Yadav PN, Allen JA, Rogan SC, Hanson BJ, Revankar C, Robers M, Doucette C, and Roth BL (2009) Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine2B receptor agonists: implications for drug safety assessment. Mol Pharmacol 76:710-722.
14. Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals, 7th ed. Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington DC.
15. Jerman JC, Brough SJ, Gager T, Wood M, Coldwell MC, Smart D, and Middlemiss DN (2001) Pharmacological characterisation of human 5-HT2 receptor subtypes. Eur J Pharmacol 414:23-30.
16. Jordan S, Koprivica V, Dunn R, Tottori K, Kikuchi T, and Altar CA (2004) In vivo effects of aripiprazole on cortical and striatal dopaminergic and serotonergic function. Eur J Pharmacol 483:45-53.
17. Kane JM, Carson WH, Saha AR, McQuade RD, Ingenito GG, Zimbroff DL, and Ali MW (2002) Efficacy and safety of aripiprazole and haloperidol versus placebo in patients with schizophrenia and schizoaffective disorder. J Clin Psychiatry 63: 763-771.
18. Kapur S, Zipursky R, Jones C, Remington G, and Houle S (2000) Relationship between dopamine D2 occupancy, clinical response, and side effects: a double-blind PET study of first episode schizophrenia. Am J Psychiatry 157:514-520.
19. Kelly JP, Wrynn AS, and Leonard BE (1997) The olfactory bulbectomized rat as a model of depression: an update. Pharmacol Ther 74:299-316.
20. Kikuchi T, Tottori K, Uwahodo Y, Hirose T, Miwa T, Oshiro Y, and Morita S (1995) 7-{4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy}-3,4-dihydro- 2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity. J Pharmacol Exp Ther 274:329-336.
21. Mazeh D, Shahal B, Saraf R, and Melamed Y (2004) Venlafaxine for the treatment of depressive episode during the course of schizophrenia. J Clin Pharmacol 24: 653-655.
22. Meltzer HY (1999) The role of serotonin in antipsychotic drug action. Neuropsychopharmacology 21 (2 Suppl):106S-115S.
23. Millan MJ, Brocco M, Papp M, Serres F, La Rochelle CD, Sharp T, Peglion JL, and Dekeyne A (2004) S32504, a novel naphthoxazine agonist at dopamine D3/D2 receptors: III. Actions in models of potential antidepressive and anxiolytic activity in comparison with ropinirole. J Pharmacol Exp Ther 309:936-950.
24. Oak JN, Lavine N, and Van Tol HH (2001) Dopamine D(4) and D(2L) receptor stimulation of the mitogen-activated protein kinase pathway is dependent on trans-activation of the platelet-derived growth factor receptor. Mol Pharmacol 60:92-103.
25. Paxinos G and Watson C (1986) The Rat Brain in Stereotaxic Coordinates, 2nd ed. Academic Press, New York.
26. Pae CU, Serretti A, Patkar AA, and Masand PS (2008) Aripiprazole in the treatment of depressive and anxiety disorders: a review of current evidence. CNS Drugs 22:367-388.
27. Pistovcakova J and Sulcova A (2008) Effect of aripiprazole on behaviour and leukocyte phagocytosis in the olfactory bulbectomy model of depression in rats. Eur Neuropsychopharmacol 18 (Suppl 4):S258.
28. 3H]L-657,743 (MK-912): a new, high affinity, selective radioligand for brain alpha 2-adrenoceptors. Life Sci 44:459-467.
29. 2C receptor agonist WAY-161503. Brain Res 1073:240-251.
30. Sanberg PR (1980) Haloperidol-induced catalepsy is mediated by postsynaptic dopamine receptors. Nature 284:472-473.
31. Seeman P, Lee T, Chau-Wong M, and Wong K (1976) Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature 261:717-719.
32. Shapiro DA, Renock S, Arrington E, Chiodo LA, Liu LX, Sibley DR, Roth BL, and Mailman R (2003) Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology. Neuropsychopharmacology 28:1400-1411.
33. Silver H (2003) Selective serotonin reuptake inhibitor augmentation in the treatment of negative symptoms of schizophrenia. Int Clin Psychopharmacol 18:305-313.
34. Siris SG, Addington D, Azorin J, Falloon IRH, Gerlach J, and Hirsch SR (2001) Depression in schizophrenia: recognition and management in the USA. Schizophr Res 47:185-197.
35. Stahl SM (2001) Dopamine system stabilizers, aripiprazole, and the next generation of antipsychotics, part 2: illustrating their mechanism of action. J Clin Psychiatry 62:923-924.
36. Stark AD, Jordan S, Allers KA, Bertekap RL, Chen R, Mistry Kannan T, Molski TF, Yocca FD, Sharp T, Kikuchi T, et al. (2007) Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT2A receptors: functional receptor-binding and in vivo electrophysiological studies. Psychopharmacology 190:373-382.
37. Swainston HT and Perry CM (2004) Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs 64:1715-1736.
38. Tamminga CA (2002) Partial dopamine agonists in the treatment of psychosis. J Neural Transm 109:411-420.
39. Tamminga CA and Carlsson A (2002) Partial dopamine agonists and dopaminergic stabilizers in the treatment of psychosis. Curr Drug Targets CNS Neurol Disord 1:141-147.
40. U'Prichard DC and Snyder SH (1980) Interactions of divalent cations and guanine nucleotides at alpha 2-noradrenergic receptor binding sites in bovine brain mechanisms. J Neurochem 34:385-394.
41. Weinberger DR and Lipska BK (1995) Cortical maldevelopment, antipsychotic drugs and schizophrenia: a search for common ground. Schizophr Res 16:87-110.
42. Zocchi A, Fabbri D, and Heidbreder CA (2005) Aripiprazole increases dopamine but not noradrenaline and serotonin levels in the mouse prefrontal cortex. Neurosci Lett 387:157-161.