In vivo quantification of striatal dopamine D2 receptor occupancy by JNJ-37822681 using [11C]raclopride and positron emission tomography

Journal of Psychopharmacology

Volumn 26, Issue 8, 2012, Pages 1128-1135

  Te Beek, Erik T ^a   De Boer, Peter ^b   Moerland, Matthijs ^a   Schmidt, Mark E ^b   Hoetjes, Nikie J ^c   Windhorst, Albert D ^c   Van Berckel, Bart N M ^c   Cohen, Adam Fa ^a   Van Gerven, Joop M A ^a   Lammertsma, Adriaan A ^c  

^a CENTRE FOR HUMAN DRUG RESEARCH   (Netherlands)

^b JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^c VU UNIVERSITY MEDICAL CENTER   (Netherlands)

Author keywords

11C raclopride; antipsychotic drug; Dopamine D2 receptor; JNJ 37822681; occupancy; PET

Indexed keywords

DOPAMINE 2 RECEPTOR; DOPAMINE 2 RECEPTOR BLOCKING AGENT; JNJ 37822681; RACLOPRIDE C 11; UNCLASSIFIED DRUG;

ADULT; ARTICLE; BLOOD CHEMISTRY; BLOOD PRESSURE; CAUDATE NUCLEUS; CEREBELLUM; CLINICAL TRIAL; CORPUS STRIATUM; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG RECEPTOR BINDING; ECG ABNORMALITY; HEART RATE; HEMATOLOGY; HUMAN; HUMAN EXPERIMENT; MALE; NEUROIMAGING; NORMAL HUMAN; OPEN STUDY; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PUTAMEN; RECEPTOR OCCUPANCY; RESTLESSNESS; SIDE EFFECT; SOMNOLENCE;

ADOLESCENT; ADULT; CORPUS STRIATUM; DOPAMINE ANTAGONISTS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MALE; PIPERIDINES; POSITRON-EMISSION TOMOGRAPHY; PYRIDAZINES; RACLOPRIDE; RADIOLIGAND ASSAY; RECEPTORS, DOPAMINE D2;

EID: 84864126110     PISSN: 02698811     EISSN: 14617285     Source Type: Journal    
DOI: 10.1177/0269881111435251     Document Type: Article

References (70)

1. Agid O, Mamo D, Ginovart N, et al. Striatal vs. extrastriatal dopamine D2 receptors in antipsychotic response-a double-blind PET study in schizophrenia. Neuropsychopharmacology. 2007 ; 32: 1209-1215
2. Arakawa R, Okumura M, Ito H, et al. Positron emission tomography measurement of dopamine D2 receptor occupancy in the pituitary and cerebral cortex: relation to antipsychotic-induced hyperprolactinemia. J Clin Psychiatry. 2010 ; 71: 1131-1137
3. Barnes TR. A rating scale for drug-induced akathisia. Br J Psychiatry. 1989 ; 154: 672-676
4. Bench CJ, Lammertsma AA, Dolan RJ, et al. Dose-dependent occupancy of central dopamine D2 receptors by the novel neuroleptic CP-88,059-01: a study using positron emission tomography and 11 C-raclopride. Psychopharmacology (Berl). 1993 ; 112: 308-314
5. Bigliani V, Mulligan RS, Acton PD, et al. Striatal and temporal cortical D2/D3 receptor occupancy by olanzapine and sertindole in vivo: a [123 I]epidepride single photon emission tomography (SPET) study. Psychopharmacology (Berl). 2000 ; 150: 132-140
6. Bressan RA, Erlandsson K, Jones HM, Mulligan RS, Ell PJ, Pilowsky LS. Optimizing limbic selective D2/D3 receptor occupancy by risperidone: a [123 I]-epidepride SPET study. J Clin Psychopharmacol. 2003 ; 23: 5-14
7. Brix G, Zaers J, Adam LE, et al. Performance evaluation of a whole-body PET scanner using the NEMA protocol. J Nucl Med. 1997 ; 38: 1614-1623
8. Ehrin E, Gawell L, Hogberg T, de Paulis T, Strom P. Synthesis of [methoxy-3H]- and [methoxy-11C]-labelled raclopride. Specific dopamine-D2 receptor ligands. J Labelled Compd Radiopharm. 1987 ; 24: 931-940
9. Erlandsson K, Bressan RA, Mulligan RS, Ell PJ, Cunningham VJ, Pilowsky LS. Analysis of D2 dopamine receptor occupancy with quantitative SPET using the high-affinity ligand [123I]epidepride: resolving conflicting findings. Neuroimage. 2003 ; 19: 1205-1214
10. Farde L, Nordström AL, Wiesel FA, Pauli S, Halldin C, Sedvall G. Positron emission tomographic analysis of central D1 and D2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. Relation to extrapyramidal side effects. Arch Gen Psychiatry. 1992 ; 49: 538-544
11. Farde L, Suhara T, Nyberg S, et al. A PET study of [11C]FLB 457 binding to extrastriatal D2-dopamine receptors in healthy subjects and antipsychotic drug-treated patients. Psychopharmacology (Berl). 1997 ; 133: 396-404
12. Farde L, Wiesel FA, Halldin C, Sedvall G. Central D2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs. Arch Gen Psychiatry. 1988 ; 45: 71-76
13. Farde L, Wiesel FA, Nordström AL, Sedvall G. D1- and D2-dopamine receptor occupancy during treatment with conventional and atypical neuroleptics. Psychopharmacology (Berl). 1989 ; 99: S28 - S31
14. Gefvert O, Lundberg T, Wieselgren IM, et al. D2 and 5HT2A receptor occupancy of different doses of quetiapine in schizophrenia: a PET study. Eur Neuropsychopharmacol. 2001 ; 11: 105-110
15. Grunder G, Landvogt C, Vernaleken I, et al. The striatal and extrastriatal D2/D3 receptor-binding profile of clozapine in patients with schizophrenia. Neuropsychopharmacology. 2006 ; 31: 1027-1035
16. Gunn RN, Lammertsma AA, Hume SP, Cunningham VJ. Parametric imaging of ligand-receptor binding in PET using a simplified reference region model. Neuroimage. 1997 ; 6: 279-287
17. Innis RB, Cunningham VJ, Delforge J, et al. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab. 2007 ; 27: 1533-1539
18. Ito H, Arakawa R, Takahashi H, et al. No regional difference in dopamine D2 receptor occupancy by the second-generation antipsychotic drug risperidone in humans: a positron emission tomography study. Int J Neuropsychopharmacol. 2009 ; 12: 667-675
19. Kapur S, Seeman P. Antipsychotic agents differ in how fast they come off the dopamine D2 receptors. Implications for atypical antipsychotic action. J Psychiatry Neurosci. 2000 ; 25: 161-166
20. Kapur S, Seeman P. Does fast dissociation from the dopamine D2 receptor explain the action of atypical antipsychotics?: A new hypothesis. Am J Psychiatry. 2001 ; 158: 360-369
21. Kapur S, Remington G, Zipursky RB, Wilson AA, Houle S. The D2 dopamine receptor occupancy of risperidone and its relationship to extrapyramidal symptoms: a PET study. Life Sci. 1995 ; 57: L103 - L107
22. Kapur S, Zipursky R, Jones C, Remington G, Houle S. Relationship between dopamine D2 occupancy, clinical response, and side effects: a double-blind PET study of first-episode schizophrenia. Am J Psychiatry. 2000a ; 157: 514-520
23. Kapur S, Zipursky RB, Jones C, et al. The D2 receptor occupancy profile of loxapine determined using PET. Neuropsychopharmacology. 1996 ; 15: 562-566
24. Kapur S, Zipursky R, Jones C, Shammi CS, Remington G, Seeman P. A positron emission tomography study of quetiapine in schizophrenia: a preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch Gen Psychiatry. 2000b ; 57: 553-559
25. Kapur S, Zipursky RB, Remington G, et al. 5-HT2 and D2 receptor occupancy of olanzapine in schizophrenia: a PET investigation. Am J Psychiatry. 1998 ; 155: 921-928
26. Kapur S, Zipursky RB, Remington G. Clinical and theoretical implications of 5-HT2 and D2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia. Am J Psychiatry. 1999 ; 156: 286-293
27. Kapur S, Zipursky R, Roy P, et al. The relationship between D2 receptor occupancy and plasma levels on low-dose oral haloperidol: a PET study. Psychopharmacology (Berl). 1997 ; 131: 148-152
28. Kegeles LS, Slifstein M, Frankle WG, et al. Dose-occupancy study of striatal and extrastriatal dopamine D2 receptors by aripiprazole in schizophrenia with PET and [18F]fallypride. Neuropsychopharmacology. 2008 ; 33: 3111-3125
29. Kessler RM, Meltzer HY. Regional selectivity in clozapine treatment?. Am J Psychiatry. 2002 ; 159: 1064-1065
30. Kessler RM, Ansari MS, Riccardi P, et al. Occupancy of striatal and extrastriatal dopamine D2/D3 receptors by olanzapine and haloperidol. Neuropsychopharmacology. 2005 ; 30: 2283-2289
31. Kessler RM, Ansari MS, Riccardi P, et al. Occupancy of striatal and extrastriatal dopamine D2 receptors by clozapine and quetiapine. Neuropsychopharmacology. 2006 ; 31: 1991-2001
32. Kuroki T, Nagao N, Nakahara T. Neuropharmacology of second-generation antipsychotic drugs: a validity of the serotonin-dopamine hypothesis. Prog Brain Res. 2008 ; 172: 199-212
33. Lammertsma AA, Hume SP. Simplified reference tissue model for PET receptor studies. Neuroimage. 1996 ; 4: 153-158
34. Langlois X, Megens A, Lavreysen H, et al. Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. Eur Neuropsychopharmacol. 2010 ; 20: S502
35. Mamo D, Graff A, Mizrahi R, Shammi CM, Romeyer F, Kapur S. Differential effects of aripiprazole on D2, 5-HT2, and 5-HT1A receptor occupancy in patients with schizophrenia: a triple tracer PET study. Am J Psychiatry. 2007 ; 164: 1411-1417
36. Mamo D, Kapur S, Shammi CM, et al. A PET study of dopamine D2 and serotonin 5-HT2 receptor occupancy in patients with schizophrenia treated with therapeutic doses of ziprasidone. Am J Psychiatry. 2004 ; 161: 818-825
37. Meltzer HY. Action of atypical antipsychotics. Am J Psychiatry. 2002 ; 159: 153-154
38. Meltzer HY, Li Z, Kaneda Y, Ichikawa J. Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 2003 ; 27: 1159-1172
39. Miyamoto S, Duncan GE, Marx CE, Lieberman JA. Treatments for schizophrenia: a critical review of pharmacology and mechanisms of action of antipsychotic drugs. Mol Psychiatry. 2005 ; 10: 79-104
40. Nordström AL, Farde L, Halldin C. Time course of D2- dopamine receptor occupancy examined by PET after single oral doses of haloperidol. Psychopharmacology (Berl). 1992 ; 106: 433-438
41. Nyberg S, Eriksson B, Oxenstierna G, Halldin C, Farde L. Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients. Am J Psychiatry. 1999 ; 156: 869-875
42. Nyberg S, Farde L, Eriksson L, Halldin C, Eriksson B. 5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone. Psychopharmacology (Berl). 1993 ; 110: 265-272
43. Nyberg S, Farde L, Halldin C, Dahl ML, Bertilsson L. D2 dopamine receptor occupancy during low-dose treatment with haloperidol decanoate. Am J Psychiatry. 1995a ; 152: 173-178
44. Nyberg S, Farde L, Halldin C. A PET study of 5-HT2 and D2 dopamine receptor occupancy induced by olanzapine in healthy subjects. Neuropsychopharmacology. 1997 ; 16: 1-7
45. Nyberg S, Nordström AL, Halldin C, Farde L. Positron emission tomography studies on D2 dopamine receptor occupancy and plasma antipsychotic drug levels in man. Int Clin Psychopharmacol. 1995b ; 10: 81-85
46. Olsson H, Farde L. Potentials and pitfalls using high-affinity radioligands in PET and SPET determinations on regional drug-induced D2 receptor occupancy-a simulation study based on experimental data. Neuroimage. 2001 ; 14: 936-945
47. Pani L, Pira L, Marchese G. Antipsychotic efficacy: relationship to optimal D2-receptor occupancy.. Eur Psychiatry. 2007 ; 22: 267-275
48. Pilowsky LS, Mulligan RS, Acton PD, Ell PJ, Costa DC, Kerwin RW. Limbic selectivity of clozapine. Lancet. 1997 ; 350: 490-491
49. Remington G, Kapur S, Zipursky R. The relationship between risperidone plasma levels and dopamine D2 occupancy: a positron emission tomographic study. J Clin Psychopharmacol. 1998 ; 18: 82-83
50. Roth BL, Sheffler D, Potkin SG. Atypical antipsychotic drug actions: unitary or multiple mechanisms for 'atypicality'?. Clin Neurosci Res. 2003 ; 3: 108-117
51. Schmidt M, De Boer P, Mannaert E, Iersel T, Van Nueten L. Safety, tolerability and D2 occupancy of the fast-dissociating D2 antagonist JNJ-37822681 in healthy subjects. Eur Neuropsychopharmacol. 2010a ; 20: S444
52. Schmidt M, Janssens L, Kent J, et al. Efficacy and safety of JNJ-37822681, a fast-dissociating D2 receptor antagonist, in the treatment of schizophrenia. Eur Neuropsychopharmacol. 2010b ; 20: S484 - S485
53. Schmidt M, Mannaert E, De Boer P, et al. D2 receptor occupancy with 11C-raclopride PET following single and multiple dose: does steady state make a difference?. Eur Neuropsychopharmacol. 2009 ; 19: S314
54. Seeman P. Atypical antipsychotics: Mechanism of action. Can J Psychiatry. 2002 ; 47: 27-38
55. Seeman P. An update of fast-off dopamine D2 atypical antipsychotics. Am J Psychiatry. 2005 ; 162: 1984-1985
56. Seeman P, Tallerico T. Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. Mol Psychiatry. 1998 ; 3: 123-134
57. Seeman P, Tallerico T. Rapid release of antipsychotic drugs from dopamine D2 receptors: an explanation for low receptor occupancy and early clinical relapse upon withdrawal of clozapine or quetiapine. Am J Psychiatry. 1999 ; 156: 876-884
58. Simpson GM, Angus JW. A rating scale for extrapyramidal side effects. Acta Psychiatr Scand Suppl. 1970 ; 212: 11-19
59. Stone JM, Bressan RA, Erlandsson K, Ell PJ, Pilowsky LS. Non-uniform blockade of intrastriatal D2/D3 receptors by risperidone and amisulpride. Psychopharmacology (Berl). 2005 ; 180: 664-669
60. Stone JM, Davis JM, Leucht S, Pilowsky LS. Cortical dopamine D2/D3 receptors are a common site of action for antipsychotic drugs-an original patient data meta-analysis of the SPECT and PET in vivo receptor imaging literature. Schizophr Bull. 2009 ; 35: 789-797
61. Svarer C, Madsen K, Hasselbalch SG, et al. MR-based automatic delineation of volumes of interest in human brain PET images using probability maps. Neuroimage. 2005 ; 24: 969-979
62. Talvik M, Nordstrom AL, Nyberg S, Olsson H, Halldin C, Farde L. No support for regional selectivity in clozapine-treated patients: A PET study with [11C]raclopride and [11C]FLB 457. Am J Psychiatry. 2001 ; 158: 926-930
63. Tauscher-Wisniewski S, Kapur S, Tauscher J, et al. Quetiapine: an effective antipsychotic in first-episode schizophrenia despite only transiently high dopamine-2 receptor blockade. J Clin Psychiatry. 2002 ; 63: 992-997
64. Te Beek ET, Moerland M, De Boer P, et al. Pharmacokinetics and central nervous system effects of the novel dopamine D2 receptor antagonist JNJ-37822681. J Psychopharmacol. 2012 ; 26: 1119-1127
65. Uchida H, Mamo DC, Kapur S, et al. Monthly administration of long-acting injectable risperidone and striatal dopamine D2 receptor occupancy for the management of schizophrenia. J Clin Psychiatry. 2008 ; 69: 1281-1286
66. Vernaleken I, Fellows C, Janouschek H, et al. Striatal and extrastriatal D2/D3-receptor-binding properties of ziprasidone: a positron emission tomography study with [18F]Fallypride and [11C]raclopride (D2/D3-receptor occupancy of ziprasidone). J Clin Psychopharmacol. 2008 ; 28: 608-617
67. Vernaleken I, Janouschek H, Raptis M, et al. Dopamine D2/3 receptor occupancy by quetiapine in striatal and extrastriatal areas. Int J Neuropsychopharmacol. 2010 ; 13: 951-960
68. Xiberas X, Martinot JL, Mallet L, et al. Extrastriatal and striatal D2 dopamine receptor blockade with haloperidol or new antipsychotic drugs in patients with schizophrenia. Br J Psychiatry. 2001 ; 179: 503-508
69. Yokoi F, Grunder G, Biziere K, et al. Dopamine D2 and D3 receptor occupancy in normal humans treated with the antipsychotic drug aripiprazole (OPC 14597): a study using positron emission tomography and [11C]raclopride. Neuropsychopharmacology. 2002 ; 27: 248-259
70. Zipursky RB, Christensen BK, Daskalakis Z, et al. Treatment response to olanzapine and haloperidol and its association with dopamine D receptor occupancy in first-episode psychosis. Can J Psychiatry. 2005 ; 50: 462-469