18F-labeled flavones for in vivo imaging of beta-amyloid plaques in Alzheimer's brains. 2009

Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
Graduate School of Biomedical Sciences, Nagasaki University, Nagasaki, Japan.

In vivo imaging of beta-amyloid (Abeta) aggregates in the brain may lead to early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of treatment. The purpose of this study was to develop novel (18)F-labeled amyloid-imaging probes based on flavones as a core structure. Fluoropegylated (FPEG) flavone derivatives were designed and synthesized. The affinity of the derivatives for Abeta aggregates varied from 5 to 321nM. In brain sections of AD model mice, FPEG flavones with the dimethylamino group intensely stained beta-amyloid plaques. In biodistrubution experiments using normal mice, they displayed high uptake in the brain ranging from 2.9 to 4.2%ID/g at 2 min postinjection. The radioactivity washed out from the brain rapidly (1.3-2.0%ID/g at 30 min), which is highly desirable for beta-amyloid imaging agents. FPEG flavones may be potential PET imaging agents for beta-amyloid plaques in Alzheimer's brains.

UI MeSH Term Description Entries
D007553 Isotope Labeling Techniques for labeling a substance with a stable or radioactive isotope. It is not used for articles involving labeled substances unless the methods of labeling are substantively discussed. Tracers that may be labeled include chemical substances, cells, or microorganisms. Isotope Labeling, Stable,Isotope-Coded Affinity Tagging,Isotopically-Coded Affinity Tagging,Affinity Tagging, Isotope-Coded,Affinity Tagging, Isotopically-Coded,Isotope Coded Affinity Tagging,Labeling, Isotope,Labeling, Stable Isotope,Stable Isotope Labeling,Tagging, Isotope-Coded Affinity,Tagging, Isotopically-Coded Affinity
D011092 Polyethylene Glycols Polymers of ETHYLENE OXIDE and water, and their ethers. They vary in consistency from liquid to solid depending on the molecular weight indicated by a number following the name. They are used as SURFACTANTS, dispersing agents, solvents, ointment and suppository bases, vehicles, and tablet excipients. Some specific groups are NONOXYNOLS, OCTOXYNOLS, and POLOXAMERS. Macrogols,Polyoxyethylenes,Carbowax,Macrogol,Polyethylene Glycol,Polyethylene Oxide,Polyethyleneoxide,Polyglycol,Glycol, Polyethylene,Glycols, Polyethylene,Oxide, Polyethylene,Oxides, Polyethylene,Polyethylene Oxides,Polyethyleneoxides,Polyglycols,Polyoxyethylene
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D005462 Fluorine Radioisotopes Unstable isotopes of fluorine that decay or disintegrate emitting radiation. F atoms with atomic weights 17, 18, and 20-22 are radioactive fluorine isotopes. Radioisotopes, Fluorine
D000544 Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57) Acute Confusional Senile Dementia,Alzheimer's Diseases,Dementia, Alzheimer Type,Dementia, Senile,Presenile Alzheimer Dementia,Senile Dementia, Alzheimer Type,Alzheimer Dementia,Alzheimer Disease, Early Onset,Alzheimer Disease, Late Onset,Alzheimer Sclerosis,Alzheimer Syndrome,Alzheimer Type Senile Dementia,Alzheimer's Disease,Alzheimer's Disease, Focal Onset,Alzheimer-Type Dementia (ATD),Dementia, Presenile,Dementia, Primary Senile Degenerative,Early Onset Alzheimer Disease,Familial Alzheimer Disease (FAD),Focal Onset Alzheimer's Disease,Late Onset Alzheimer Disease,Primary Senile Degenerative Dementia,Senile Dementia, Acute Confusional,Alzheimer Dementias,Alzheimer Disease, Familial (FAD),Alzheimer Diseases,Alzheimer Type Dementia,Alzheimer Type Dementia (ATD),Alzheimers Diseases,Dementia, Alzheimer,Dementia, Alzheimer-Type (ATD),Familial Alzheimer Diseases (FAD),Presenile Dementia,Sclerosis, Alzheimer,Senile Dementia
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D047309 Flavones A group of 4-keto-FLAVONOIDS. 2-Phenyl-2-Ene-Benzopyran-4-One Compounds
D049268 Positron-Emission Tomography An imaging technique using compounds labelled with short-lived positron-emitting radionuclides (such as carbon-11, nitrogen-13, oxygen-15 and fluorine-18) to measure cell metabolism. It has been useful in study of soft tissues such as CANCER; CARDIOVASCULAR SYSTEM; and brain. SINGLE-PHOTON EMISSION-COMPUTED TOMOGRAPHY is closely related to positron emission tomography, but uses isotopes with longer half-lives and resolution is lower. PET Imaging,PET Scan,Positron-Emission Tomography Imaging,Tomography, Positron-Emission,Imaging, PET,Imaging, Positron-Emission Tomography,PET Imagings,PET Scans,Positron Emission Tomography,Positron Emission Tomography Imaging,Positron-Emission Tomography Imagings,Scan, PET,Tomography Imaging, Positron-Emission,Tomography, Positron Emission
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus
D058225 Plaque, Amyloid Accumulations of extracellularly deposited AMYLOID FIBRILS within tissues. Amyloid Deposits,Plaques, Amyloid,Amyloid Plaques,Neuritic Plaques,Senile Plaques,Amyloid Deposit,Amyloid Plaque,Deposit, Amyloid,Deposits, Amyloid,Neuritic Plaque,Plaque, Neuritic,Plaque, Senile,Plaques, Neuritic,Plaques, Senile,Senile Plaque

Related Publications

Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
October 2010, Bioorganic & medicinal chemistry letters,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
November 2007, Bioorganic & medicinal chemistry,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
November 2005, Journal of medicinal chemistry,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
April 2011, Journal of medicinal chemistry,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
May 2006, Journal of medicinal chemistry,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
January 2018, American journal of nuclear medicine and molecular imaging,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
July 2021, Biosensors,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
October 2009, Chemical & pharmaceutical bulletin,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
June 2010, Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
Masahiro Ono, and Rumi Watanabe, and Hidekazu Kawashima, and Tomoki Kawai, and Hiroyuki Watanabe, and Mamoru Haratake, and Hideo Saji, and Morio Nakayama
October 2010, ACS medicinal chemistry letters,
Copied contents to your clipboard!