A PET study of 5-HT2 and D2 dopamine receptor occupancy induced by olanzapine in healthy subjects

Neuropsychopharmacology

Volumn 16, Issue 1, 1997, Pages 1-7

  Nyberg, Svante ^a   Farde, Lars ^a   Halldin, Christer ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

5 HT2 receptors; Antipsychotic drugs; Atypical; D2 dopamine receptors; Human; Olanzapine; Positron emission tomography

Indexed keywords

DOPAMINE 2 RECEPTOR; MUSCARINIC RECEPTOR; OLANZAPINE; RACLOPRIDE; SEROTONIN RECEPTOR;

ADULT; ARTICLE; DOSE RESPONSE; DRUG BLOOD LEVEL; HUMAN; HUMAN EXPERIMENT; ISOTOPE LABELING; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHARMACODYNAMICS; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RECEPTOR BINDING;

EID: 0031014718     PISSN: 0893133X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0893-133X(96)00218-7     Document Type: Article

References (37)

1. Alván G, Bechtel P, Iselius L, Gundert-Remy U (1990): Hydroxylation polymorphisms of debrisoquine and mephenytoin in European populations. Eur J Clin Pharmacol 39:533-537
2. Barnes TRE (1989): A rating scale for drug-induced akathisia. Br J Psychiatry 154:672-676
3. Beasley C, Jr, Tollefson G, Tran P, Satterlee W, Sanger T, Hamilton S, The Olanzapine HGAD Study Group (1996): Olanzapine versus placebo and haloperidol: Acute phase results of the North American double-blind olanzapine trial. Neuropsychopharmacology 14:111-123
4. Bergström M, Boëthius J, Eriksson L, Greitz T, Ribbe T, Widén L (1981): Head fixation device for reproducible position alignment in transmission CT and positron emission tomography. J Comput Assist Tomogr 5:136-141
5. Bymaster FP, Calligaro DO, Falcone JF, Marsh RD, Moore NA, Tye NC, Seeman P, Wong DT (1996): Radioreceptor binding profile of the atypical antipsychotic olanzapine. Neuropsychopharmacology 14:87-96
6. Catlow JT, Barton RD, Clemens M, Gillespie TA, Goodwin M, Swanson SP (1995): Analysis of olanzapine in human plasma utilizing reversed-phase high-performance liquid chromatography with electrochemical detection. Journal of Chromatography B: Biomedical Applications 668:85-90
7. Dahl M-L, Bertilsson L (1993): Genetically variable metabolism of antidepressants and neuroleptic drugs in man. Pharmacogenetics 3:61-70
8. 11C]Methyl)spiperone. Int J Rad Appl Instrum [A] 37:433-434
9. 2-dopamine receptors studied by PET-A comparison to the equilibrium analysis. J Cereb Blood Flow Metab 9:696-708
10. 2-dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine - relation to extrapyramidal side effects. Arch Gen Psychiatry 49:538-544
11. 2 receptor binding in risperidonetreated patients. J Clin Psychopharmacol 15 (suppl 1): 19S-23S
12. 2dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs. Arch Gen Psychiatry 45:71-76
13. 2 dopamine receptors in neuroleptic-naive schizophrenic patients. Arch Gen Psychiatry 47:213-219
14. Fuller RW, Snoddy HD (1992): Neuroendocrine evidence for antagonism of serotonin and dopamine receptors by olanzapine (LY170053), an antipsychotic drug candidate. Res Commun Chem Pathol Pharmacol 77:87-93
15. Gerlach J (1991): New antipsychotics: classification, efficacy, and adverse effects. Schizophr Bull 17:289-309
16. 3H-raclopride. J Neural Transm 73:7-21
17. Halldin C, Farde L, Högberg T, Hall H, Sedvall G (1990): C-11 labelling of eticlopride in two different positions - a selective high-affinity ligand for the study of dopamine D-2 receptors using PET. Appl Radiat Isot 41:669-674
18. Halldin C, Farde L, Högberg T, Hall H, Ström P, Ohlberger A, Solin O (1991) : A comparative PET-study of five carbon-11 or fluorine-18 labelled salicylamides. Preparation and in vitro dopamine D-2 binding. Int J Rad Appl Instrum [B] 18:871-881
19. Kane JM, Honigfeld G, Singer J, Meltzer H (1988): Clozapine for the treatment-resistant schizophrenic. Arch Gen Psychiatry 45:789-796
20. 1-dopamine receptor occupancy and pharmacodynamics in man. Psychopharmacology 119:1-8
21. Lieberman JA (1994): Understanding the mechanism of action of atypical antipsychotic drugs. A review of compounds in use and development. Br J Psychiatry 163 (suppl 22):7-18
22. Litton JE, Holte S, Eriksson L (1990): Evaluation of the Karolinska new positron camera system; the Scanditronix PC2048-15B. IEEE Trans Nucl Sci 37:743-748
23. Marder SR, Meilbach RC (1994): Risperidone in the treatment of schizophrenia. Am J Psychiatry 151:825-835
24. Metzer HY (1991): The mechanism of action of novel antipsychotic drugs. Schizophr Bull 17:263-287
25. 2 affinities differentiate atypical and typical antipsychotic drugs. Psychopharmacol Bull 25:390-392
26. Moore NA, Rees G, Sanger G, Tye NC (1994): Effect of olanzapine and other antipsychotic agents on responding maintained by a conflict schedule. Behavioural Pharmacol 5:196-202
27. Moore NA, Tye NC, Axton MS, Risius FC (1992): The behavioral pharmacology of olanzapine, a novel "atypical" antipsychotic agent. J Pharmacol Exp Ther 262:545-551
28. Nordström A-L, Farde L, Eriksson L, Halldin C (1995a): No elevated D2 dopamine receptors in neuroleptic-naive schizophrenic patients revealed by positron emission tomography and [11C]N-methylspiperone. Psychiatry Res: Neuroimaging 61:67-83
29. Nordström A-L, Farde L; Nyberg S, Karlsson P, Halldin C, Sedvall G (1995b): Dl-, D2-and 5-HT2 receptor occupancy in relation to clozapine serum concentration-a PET study in schizophrenic patients. Am J Psychiatry 152:1444-1449
30. Nordström A-L, Farde L, Wiesel F-A, Forslund K, Pauli S, Halldin C, Uppfeldt G (1993): Central D2-dopamine receptor occupance in relation to antipsychotic drug effects - a double blind PET study of schizophrenic patients. Biol Psychiatry 33:227-235
31. 2 dopamine receptor occupancy in the living human brain. A PET study with risperidone. Psychopharmacology 110:265-272
32. Nyberg S, Nordström A-L, Halldin C, Farde L (1995): PET studies on D2 dopamine receptor occupancy and antipsychotic drug plasma levels in man. Int Clin Psychopharmacology 10, Suppl. 3:81-85
33. Nyhart E, Jr, Cerimele B, Kassahun K, Callaghan J, Bergstrom R, Radtke D (1995): An initial assessment of the bioequivalence of capsule and tablet formulations of olanzapine. (Poster). Proceedings from: Annual meeting of the American Association of Pharmaceutical Sciences, Miami, Fl, USA
34. Pazos A, Probst A, Palacios J (1987): Serotonin receptors in the human brain. IV: Autoradiographic mapping of serotonin-2 receptors. Neuroscience 21:123-139
35. Sanz E, Villén T, Alm C, Bertilsson L (1989): S-mephenytoin hydroxylation phenotypes in a Swedish population determined after coadministration with debrisoquin. Clin Pharmacol Ther 45:495-499
36. Schotte A, Maloteaux JM, Laduron PM (1983): Characterization and regional distribution of serotonin S2-receptors in human brain. Brain Res 276:232-235
37. Simpson GM, Angus JWS (1970): A rating scale for extrapyramidal side effects. Acta Psychiatr Scand 212:11-19