In vivo visualization of a-synuclein deposition by [11C]BF-227 PET in Parkinson's disease and Parkinsonian syndrome - In vivo visualization of a-synuclein deposition by [11C]BF-227 PET in Parkinson's disease and Parkinsonian syndrome

开始日期2012-09-01

申办/合作机构

Tohoku University

100 项与 11C-BF-227 相关的临床结果

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100 项与 11C-BF-227 相关的转化医学

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100 项与 11C-BF-227 相关的专利（医药）

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项与 11C-BF-227 相关的文献（医药）

2007-08-01·Current Opinion in Neurology

Amyloid imaging in Alzheimer??s disease

Review

作者: Nordberg, Agneta

PURPOSE OF REVIEWThis paper reviews the progress in developing amyloid imaging ligands to be used to measure amyloid in vivo in the brain of patients with Alzheimer's disease.RECENT FINDINGSFour radioligands, [18F] 1,1-dicyano-2-[6-(dimethylamino)-2-naphtalenyl] propene or 18F-FDDNP, N-methyl [11C] 2-(4'-methylaminophenyl)-6-hydroxy-benzothiasole or 11C-PIB, 4-N-methylamino-4'-hydroxystilbene [11C] or SB13 and 2-(2-[2-dimethylaminothiazol-5-yl]ethenyl)-6-(2-[fluoro]ethoxy)benzoxazole or 11C-BF-227, have so far been studied in Alzheimer's disease patients and age-matched healthy controls by PET. A robust difference was observed between PIB retention in mild patients and controls. A 2-year follow-up study in mild patients showed a stable level of PIB retention and a decrease in cerebral glucose metabolism and cognition. 18F-FDDNP showed less difference between Alzheimer's disease patients and controls compared with PIB. Both ligands have detected increases in amyloid in the brain of patients with mild cognitive impairment.SUMMARYThe new PET amyloid imaging technique is a breakthrough in understanding the pathophysiological mechanisms and time course in amyloid deposits in the brain. The technique will enable early detection of Alzheimer's disease. PET amyloid imaging should be used in the evaluation of new antiamyloid therapies.

2007-03-01·Brain and nerve = Shinkei kenkyu no shinpo

[Introduction to and general remarks on molecular imaging].

Review

作者: Okamura, Nobuyuki ; Fukuda, Hiroshi

Molecular imaging is a visualization of quantity and dynamics of molecules to understand the process of gene regulation and physiological function of the proteins in living tissue or cells. Examples of the research include the development and application of fluorescent proteins, quantum dots, nanoparticles for optical imaging, micro bubbles for ultrasound, ferromagnetic compounds for MRI and radiopharmaceuticals for positron emission tomography (PET). PET is most promising in this field, because of its high sensitivity of the measurement and easy applicability to humans. In this general remark, the topics will be concentrated on molecular imaging with PET for the diagnosis of Alzheimer's disease (AD) in early stage. 11C-MP4P (N-methlpiperidyl-4-propionate), is a probe for the measurement of acetylcholine esterase (AchE) activity in the human brain by PET. The AchE activities (k3) in early onset AD measured with PET was low in hippocampus, amygdale and wide spread neocortex including parietal and temporal cortex compared to those in age-matched control. The results indicated that the decrease of AchE activities is preceded by the decrease of blood flow. One of the topics in this research field is an imaging of aggregated amyloid Abeta in the AD brain. Kudo et al, screened more than 2,600 compounds and found several good probes for amyloid Abeta imaging, including BF-168 and BF-227. Okamura demonstrated that BF-168 specifically bind to the amyloid plaques in the brain of a transgenic mouse (PS1/APPsw). Furumoto et al successfully labeled BF-227 with C-11, and clinical PET studies using 11C-BF-227 is now ongoing at Tohoku University. Preliminary clinical study revealed that the compound accumulated in the tempo-parietal region of the brain in AD patient, although non-specific accumulation in the thalamus, basal ganglia and white matter was observed. The goal of this project is to detect AD at pre-clinical stage.

2006-01-01·Minimally Invasive Therapy & Allied Technologies4区 · 医学

Development of amyloid imaging PET probes for an early diagnosis of Alzheimer's disease

4区 · 医学

Article

作者: Kudo, Yukitsuka

Progressive accumulation of senile plaques (SPs) is one of the major neuropathological features of Alzheimer's Disease (AD) that precedes cognitive decline. Noninvasive detection of SPs could, therefore, be a potential diagnostic test for early or presymptomatic detection of AD patients. For this purpose, many attempts have been made to visualize AD-specific pathological changes in the living brain. Currently, a most practical method for the in vivo measurement of SP depositions is using positron emission tomography (PET) and contrast agent that specifically label SPs. We have developed a novel compound 2-[2-(2-dimethylaminothiazol-5-yl) ethenyl]-6-[2-(fluoro)ethoxy] benzoxazole (BF-227) as a candidate for an amyloid imaging probe for PET. BF-227 displayed high affinity to synthetic amyloid beta fibrils and clearly stained both SPs and diffuse plaques in AD brain sections. Intravenous administration of [11C]BF-227 into normal mice indicated that this labeled tracer readily penetrated the blood brain barrier (BBB) and was washed out quickly from brain tissue. Currently, we have investigated the clinical trial of [11C]BF-227 in healthy subjects and AD patients.

100 项与 11C-BF-227 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
诊断试剂	临床2期	-	Tohoku University	-
多系统萎缩	药物发现	日本	Tohoku University	2015-06-15

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


J-ADNI (AAIC2013)	N/A	-	-	[C-11]BF-227 (Patients with mild cognitive impairment (MCI))	製遞獵衊蓋廠壓蓋簾襯(膚蓋鏇膚醖鏇觸繭顧窪) = 鑰簾鬱網醖憲襯範觸網鹹鬱願願觸齋壓衊艱簾 (鹽鏇襯鏇壓鹽夢齋築繭 )	-	2013-07-01
				[C-11]BF-227 (Patients with Alzheimer's disease (AD))	製遞獵衊蓋廠壓蓋簾襯(膚蓋鏇膚醖鏇觸繭顧窪) = 夢廠鹹遞構獵衊壓膚網鹹鬱願願觸齋壓衊艱簾 (鹽鏇襯鏇壓鹽夢齋築繭 )