Central Nervous System Drug Evaluation Using Positron Emission Tomography
1
조회
0
다운로드
0
인용
0
참고문헌
키워드
초록
In conventional pharmacological research in the field of mental disorders, pharmacological effect and dose have been estimated by ethological approach and in vitro data of affinity to the site of action. In addition, the frequency of administration has been estimated from drug kinetics in blood. However, there is a problem regarding an objective index of drug effects in the living body. Furthermore, the possibility that the concentration of drug in blood does not necessarily reflect the drug kinetics in target organs has been pointed out. Positron emission tomography (PET) techniques have made progress for more than 20 years,and made it possible to measure the distribution and kinetics of small molecule components in living brain. In this article, we focused on rational drug dosing using receptor occupancy and proof-of-concept of drugs in the drug development process using PET.
Abstract
In conventional pharmacological research in the field of mental disorders, pharmacological effect and dose have been estimated by ethological approach and in vitro data of affinity to the site of action. In addition, the frequency of administration has been estimated from drug kinetics in blood. However, there is a problem regarding an objective index of drug effects in the living body. Furthermore, the possibility that the concentration of drug in blood does not necessarily reflect the drug kinetics in target organs has been pointed out. Positron emission tomography (PET) techniques have made progress for more than 20 years,and made it possible to measure the distribution and kinetics of small molecule components in living brain. In this article, we focused on rational drug dosing using receptor occupancy and proof-of-concept of drugs in the drug development process using PET.
참고문헌 (50)
- Wong DF, "Proof of concept: functional models for drug development in humans, In Neuropsychopharmacology: The Fifth Generation of Progress", pp.457~473 (2002), Lippincott Williams & Wilkins
- Seeman P, "Antipsychotic drugs: direct correlation between clinical potency and presynaptic action ondopamine neurons", Science, 188, pp.1217~1219 (1975)
- Farde L, "Quantitative analysis of D2 dopamine receptor binding in the living human brain by PET", Science, 231, pp.258~261 (1986)
- Farde L, "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, 49, pp.538~544 (1992)
- Nordström AL, "Central D2-dopamine receptor occupancy in relation to antipsychotic drug effects: a double-blind PET study of schizophrenic patients", Biol Psychiatry, 33, pp.227~235 (1993)
- Kapur S, "Relationship between dopamine D(2) occupancy, clinical response, and side effects: a double-blind PET study of first-episode schizophrenia", Am J Psychiatry, 157, pp.514~520 (2000)
- Nyberg S, "Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients", Am J Psychiatry, 156, pp.869~875 (1999)
- Yasuno F, "Dose relationship of limbic-cortical D2-dopamine receptor occupancy with risperidone", Psychopharmacology (Berl), 154, pp.112~114 (2001)
- Arakawa R, "Extrastriatal dopamine D(2) receptor occupancy in olanzapine-treated patients with schizophrenia", Eur Arch Psychiatry Clin Neurosci, 260, pp.345~350 (2010)
- Kapur S, "5-HT2 and D2 receptor occupancy of olanzapine in schizophrenia: a PET investigation", Am J Psychiatry, 155, pp.921~928 (1998)
- Arakawa R, "Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia", Psychopharmacology (Berl), 197, pp.229~235 (2008)
- 강원준, "Modeling of brain D2 receptor occupancy-plasma concentration relationships with a novel antipsychotic, YKP1358, using serial PET scans in healthy volunteers", CLINICAL PHARMACOLOGY & THERAPEUTICS, 81(2), pp.252~258
- Takano A, "The antipsychotic sultopride is overdosed--a PET study of drug-induced receptor occupancy in comparison with sulpiride", Int J Neuropsychopharmacol, 9, pp.539~545 (2006)
- raclopride, "Neuropsychopharmacology", 2002, 248~259
- Grunder G, "Mechanism of new antipsychotic medications: occupancy is not just antagonism", Arch Gen Psychiatry, 60, pp.974~977 (2003)
- Gründer G, "The striatal and extrastriatal D2", D3 receptor-binding profile of clozapine in patients with schizophrenia, 2006, pp.31, 1027~1035
- Takano A, "Estimation of the time-course of dopamine D2 receptor occupancy in living human brain from plasma pharmacokinetics of antipsychotics", Int J Neuropsychopharmacol, 7, pp.19~26 (2004)
- Pilowsky LS, "Limbic selectivity of clozapine", Lancet, 350, pp.490~491 (1997)
- -epidepride SPET study, "J Clin Psychopharmacol", 2003, 5~14
- Xiberas X, "Extrastriatal and striatal D(2) dopamine receptor blockade with haloperidol or new antipsychotic drugs in patients with schizophrenia", Br J Psychiatry, 179, pp.503~508 (2001)
- Ito H, "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, 12, pp.667~675 (2009)
- Nordström AL, "Plasma prolactin and central D2 receptor occupancy in antipsychotic drug-treated patients", J Clin Psychopharmacol, 18, pp.305~310 (1998)
- Bressan RA, "Prolactinemia is uncoupled from central D2", D3 dopamine receptor occupancy in amisulpride treated patients, 2004, pp.175, 367~373
- Arakawa R, "PET measurement of dopamine D2 receptor occupancy in the pituitary and cerebral cortex: relation to antipsychotic-induced hyperprolactinemia", J Clin Psychiatry, 71, pp.1131~1137 (2010)
- DASB positron emission tomography study, "Am J Psychiatry", 2004, 826~835
- Suhara T, "High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography", Arch Gen Psychiatry, 60, pp.386~391 (2003)
- Takano A, "A dose-finding study of duloxetine based on serotonin transporter occupancy", Psychopharmacology (Berl), 185, pp.395~399 (2006)
- Martin AJ, "Affective disorders in general practice. Treatment of 6000 patients with fluvoxamine", Pharmatherapeutica, 5, pp.40~49 (1987)
- Stokes PE, "Fluoxetine: a five-year review", Clin Ther, 15, pp.216~243 (1993)
- Papakostas GI, "Are antidepressant drugs that combine serotonergic and noradrenergic mechanisms of action more effective than the selective serotonin reuptake inhibitors in treating major depressive disorder? A meta-analysis of studies of newer agents", Biol Psychiatry, 62, pp.1217~1227 (2007)
- Thase ME, "Efficacy of duloxetine and selective serotonin reuptake inhibitors: comparisons as assessed by remission rates in patients with major depressive disorder", J Clin Psychopharmacol, 27, pp.672~676 (2007)
- Schou M, "PET evaluation of novel radiofluorinated reboxetine analogs as norepinephrine transporter probes in the monkey brain", Synapse, 53, pp.57~67 (2004)
- Arakawa R, "Quantitative analysis of norepinephrine transporter in the human brain using PET with (S,S)-18F-FMeNER-D2", J Nucl Med, 49, pp.1270~1276 (2008)
- FMeNER-D2, "Eur J Nucl Med Mol Imaging", 2008, 153~157
- FMeNER-D2, "Neuroimage", 2008, 474~482
- FMeNER-D2, "Psychopharmacology (Berl)", 2010, 331~336
- Kudo Y, "Development of amyloid imaging PET probes for an early diagnosis of Alzheimer's disease", Minim Invasive Ther Allied Technol, 15, pp.209~213 (2006)
- ethoxy)benzoxazole: a novel PET agent for in vivo detection of dense amyloid plaques in Alzheimer's disease patients, "J Nucl Med", 2007, 553~561
- AZD2184, "Eur J Nucl Med Mol Imaging", 2009, 1859~1863
- Choi SR, "Preclinical properties of 18F-AV-45: a PET agent for Abeta plaques in the brain", J Nucl Med, 50, pp.1887~1894 (2009)
- F 18), "J Nucl Med", 2010, 913~920
- Rinne JO, "11C-PiB PET assessment of change in fibrillar amyloid-beta load in patients with Alzheimer's disease treated with bapineuzumab: a phase 2, double-blind, placebo-controlled, ascending-dose study", Lancet Neurol, 9, pp.363~372 (2010)
- Ota T, "Estimation of plasma IC50 of donepezil for cerebral acetylcholinesterase inhibition in patients with Alzheimer disease using positron emission tomography", Clin Neuropharmacol, 33, pp.74~78 (2010)
- Maeda J, "Longitudinal, quantitative assessment of amyloid, neuroinflammation, and anti-amyloid treatment in a living mouse model of Alzheimer's disease enabled by positron emission tomography", J Neurosci, 27, pp.10957~10968 (2007)
- Saijo T, "Utility of small-animal positron emission tomographic imaging of rats for preclinical development of drugs acting on the serotonin transporter", Int J Neuropsychopharmacol, 12, pp.1021~1032 (2009)
- Maeda J, "p.2.d.002 Wf-516, a novel antidepressant with dual serotonergic activity:Ⅱ. Pharmacological profiles ex vivo and in vivo to monoamine transporters in comparison with standard antidepressant", Eur Neuropsychopharmacol, 16, pp.333~334 (2006)
- Takano A, "Time course of in vivo 5-HTT transporter occupancy by fluvoxamine", J Clin Psychopharmacol, 26, pp.188~191 (2006)
- Tai YC, "Performance evaluation of the microPET focus: a third-generation microPET scanner dedicated to animal imaging", J Nucl Med, 46(46), pp.455~463 (2005)
- Hildebrandt IJ, "Anesthesia and other considerations for in vivo imaging of small animals", ILAR J, 49, pp.17~26 (2008)
- FPWAY in blood and brain of the rat with and without isoflurane anesthesia, "Eur J Nucl Med Mol Imaging", 2007, 259~266
