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

Volumn 27, Issue 2, 2002, Pages 248-259

  Yokoi, Fuji ^a,b   Gründer, Gerhard ^a,b   Biziere, Kathleen ^a,b   Stephane, Massoud ^a,b   Dogan, Ahmet S ^a,b   Dannals, Robert F ^a,b   Ravert, Hayden ^a,b   Suri, Ajit ^a,b   Bramer, Steven ^a,b   Wong, Dean F ^a,b  

^a DEPARTMENT OF PATHOLOGY   (United States)

^b OTSUKA PHARMACEUTICAL DEVELOPMENT AND COMMERCIALIZATION INC   (United States)

Author keywords

11C raclopride; Aripiprazole; D2 dopamine receptor; Dopamine agonist; Positron Emission Tomography (PET); Receptor occupancy; Schizophrenia

Indexed keywords

ARIPIPRAZOLE; DOPAMINE 2 RECEPTOR; DOPAMINE 3 RECEPTOR; RACLOPRIDE; DIAGNOSTIC AGENT; DOPAMINE RECEPTOR BLOCKING AGENT; DRD3 PROTEIN, HUMAN; NEUROLEPTIC AGENT; PIPERAZINE DERIVATIVE; QUINOLONE DERIVATIVE;

ADULT; ARTICLE; BRAIN REGION; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG MECHANISM; HUMAN; KINETICS; MALE; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RADIOACTIVITY; RECEPTOR OCCUPANCY; BINDING COMPETITION; BLOOD; BRAIN; CEREBELLUM; COMPUTER ASSISTED EMISSION TOMOGRAPHY; CORPUS STRIATUM; DRUG ADMINISTRATION; DRUG EFFECT; METABOLISM; NERVE CELL; ORAL DRUG ADMINISTRATION; PATHOPHYSIOLOGY; PHYSIOLOGY; RADIOASSAY; SCHIZOPHRENIA; SCINTISCANNING;

ADMINISTRATION, ORAL; ADULT; ANTIPSYCHOTIC AGENTS; BINDING, COMPETITIVE; BRAIN; CEREBELLUM; CORPUS STRIATUM; DOPAMINE ANTAGONISTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; HUMANS; MALE; NEURONS; PIPERAZINES; QUINOLONES; RACLOPRIDE; RADIOLIGAND ASSAY; RECEPTORS, DOPAMINE D2; RECEPTORS, DOPAMINE D3; SCHIZOPHRENIA; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0035983682     PISSN: 0893133X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0893-133X(02)00304-4     Document Type: Article

References (59)

1. Pergolide binds tightly to dopamine D2 short receptors and induces receptor sequestration
2. 2 dopamine receptors in human Y-79 retinoblastoma cells
3. Dose dependent occupancy of central dopamine D2 receptors by the novel neuroleptic CP-88,059-01: A study using positron emission tomography and 11C-raclopride
4. Correction for scattered radiation in a ring detector positron camera by integral transformation of the projections
5. Aripiprazole is a high affinity partial agonist at human D2 dopamine receptors
6. Antischizophrenic drugs: Chronic treatment elevates dopamine receptor binding in brain
7. Efficacy of aripiprazole in psychotic disorders: Comparison with haloperidol and placebo
8. In vivo [3H]spiperone binding: Evidence for accumulation in corpus striatum by agonist-mediated receptor internalization
9. Striatal dopamine receptors become supersensitive while rats are given trifluoperazine for six months
10. Changes in rat striatal dopamine turnover and receptor activity during one year's neuroleptic administration
11. Cerebral dopamine function in rats following withdrawal from one year of continuous neuroleptic administration
12. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs
13. Aripiprazole, a novel antipsychotic: Overview of a phase II study result
14. Concept of reaction volume in the in vivo ligand-receptor model
15. Preparation of 11C-labelled Raclopride, a new potent dopamine receptor antagonist: Preliminary PET studies of cerebral dopamine receptors in the monkey
16. Central D2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs
17. 2-dopamine receptors studied by PET: A comparison to the equilibrium analysis
18. 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
19. Roxindole, a dopamine autoreceptor agonist, in the treatment of major depression
20. The neuroendocrinological profile of roxindole, a dopamine autoreceptor agonist, in schizophrenic patients
21. 2-like dopamine receptors after treatment with the sigma ligand EMD 57445, a putative atypical antipsychotic
22. Effect of endogenous dopamine on in vivo binding of dopamine D1 and D2 radiotracers
23. SPECT studies of D2 occupancy in low-dose haloperidol treatment
24. Noninvasive quantification of dopamine D2 receptors with iodine-123-IBF SPECT
25. Effects of the novel antipsychotic agent 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy}-3,4-dihydro-2(1H)- quinolinone (OPC-14597) on prolactin release from the rat anterior pituitary gland
26. Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum
27. Sequestration of dopamine D2 receptors depends on coexpression of G-protein-coupled receptor kinases 2 or 5
28. Efficacy of aripiprazole in psychotic disorders: Comparison with haloperidol and placebo
29. High levels of dopamine D2 receptor occupancy with low-dose haloperidol treatment: A PET study
30. 2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia
31. A positron emission tomography study of quetiapine in schizophrenia: A preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy
32. Does fast dissociation from the dopamine D2 receptor explain the action of atypical antipsychotics? A new hypothesis
33. Dopamine autoreceptor and postsynaptic receptor blocking potency of neuroleptics
34. 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
35. Comparison of methods for analysis of clinical [11C]raclopride studies
36. Simplified reference tissue model for PET receptor studies
37. Imaging D2 receptor occupancy by endogenous dopamine in humans
38. Imaging synaptic neurotransmission with in vivo binding competition techniques: A critical review
39. Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes
40. Trapping of labelled ligands in intact cells: A pitfall in binding studies
41. Agonist-induced muscarinic cholinergic receptor internalization, recycling and degradation in cultured neuronal cells. Cellular mechanisms and role in desensitization
42. Effects of discontinuous drug administration on the development of dopamine receptor supersensitivity during chronic trifluoperazine or cis-flupenthixol administration to rats
43. Time course of D2-dopamine receptor occupancy examined by PET after single oral doses of haloperidol
44. 2-dopamine receptor occupancy in relation to antipsychotic drug effects: A double-blind PET study of schizophrenic patients
45. Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency
46. Aripiprazole, A new atypical antipsychotic: Phase 2 clinical trial result
47. Biochemical pharmacology of midbrain dopamine neurons
48. Discriminative stimulus effects of apomorphine and 7-OH-DPAT: A potential role for dopamine D3 receptors
49. Antipsychotic drug doses and neuroleptic/dopamine receptors
50. Serial [18F]N-methylspiroperidol PET studies to measure changes in antipsychotic drug D-2 receptor occupancy in schizophrenic patients
51. Role of agonist-dependent receptor internalization in the regulation of mu opioid receptors
52. Chronic neuroleptic treatment specifically alters the number of dopamine receptors in rat brain
53. Distinct dynamin-dependent and -independent mechanisms target structurally homologous dopamine receptors to different endocytic membranes
54. Roxindole, a dopamine autoreceptor agonist, in the treatment of positive and negative schizophrenia
55. Dopamine blockade and clinical response: Evidence for two biological subgroups of schizophrenia
56. Compartments and reaction volumes of brain fluid spaces: Shaken, not stirred
57. A quantification of extracellular dopamine release in schizophrenia and cocaine use by means of tremble
58. 2 dopamine receptors in schizophrenia: The ups and downs of neuroimaging research, commentary
59. 3H]raclopride binding in the rat brain