Synthesis and preliminary evaluation of [18F]FEtP4A, a promising PET tracer for mapping acetylcholinesterase in vivo

Nuclear Medicine and Biology

Volumn 29, Issue 4, 2002, Pages 463-468

  Zhang, Ming Rong ^a,b   Tsuchiyama, Akio ^a,c   Haradahira, Terushi ^a   Furutsuka, Kenji ^a,b   Yoshida, Yuichiro ^b,d   Junko Noguchi, Takayo Kida ^a,b   Irie, Toshiaki ^a   Suzuki, Kazutoshi ^a  

^a NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES   (Japan)

^b 141 0032   (Japan)

^c TOKYO UNIVERSITY OF SCIENCE   (Japan)

^d JAPAN SCIENCE AND TECHNOLOGY AGENCY   (Japan)

Author keywords

18F FEtBr; 18F FEtP4A; Acetylcholinesterase; Alzheimer's disease; PET

Indexed keywords

4 PIPERIDYLACETATE; ACETYLCHOLINESTERASE; FLUOROETHYL BROMIDE F 18; N FLUOROETHYL 4 PIPERIDINOL F 18; N FLUOROETHYL 4 PIPERIDYLACETATE F 18; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; ACETIC ACID DERIVATIVE; DIAGNOSTIC AGENT; FLUORINE; N FLUOROETHYL 4 PIPERIDYL ACETATE; N-FLUOROETHYL-4-PIPERIDYL ACETATE; PIPERIDINE DERIVATIVE;

ANIMAL TISSUE; ARTICLE; AUTOMATION; BRAIN CORTEX; CEREBELLUM; CHEMICAL ANALYSIS; CONTROLLED STUDY; CORPUS STRIATUM; DRUG DISTRIBUTION; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVITY; HYDROLYSIS; IN VIVO STUDY; MOUSE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RADIOACTIVITY; RESTRICTION MAPPING; ANIMAL; BRAIN; EVALUATION; METABOLISM; SCINTISCANNING; SENSITIVITY AND SPECIFICITY; SYNTHESIS; TISSUE DISTRIBUTION;

ACETATES; ACETYLCHOLINESTERASE; ANIMAL; BRAIN; CEREBELLUM; CEREBRAL CORTEX; CORPUS STRIATUM; FLUORINE RADIOISOTOPES; MICE; PIPERIDINES; SENSITIVITY AND SPECIFICITY; SUPPORT, NON-U.S. GOV'T; TISSUE DISTRIBUTION; ANIMALS;

EID: 0035988232     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(01)00315-8     Document Type: Article

References (25)

1. 18F]fluoro-1,2,3,4-tetrahydroacridine: A potential PET agent for evaluation acetylcholinesterase
2. 11C]physostigmine
3. 11C]methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1, 2-benzisoxazole as an in vivo radioligand for acetylcholinesterase
4. 18F]FP-TZTP: Control and competition studies
5. A rapid and efficient method for the fluoroalkylation of amines and amides. Development of a method suitable for incorporation of the short-lived positron emitting radionuclide fluorine-18
6. Selective loss of central cholinergic neurons in Alzheimer's diseases
7. Design and evaluation of radioactive acetylcholine analogues for mapping brain acetylcholineaterase (AchE) in vivo
8. Evaluation of phenylmethanesulfonyl fluoride as a tracer candidate mapping acetylcholinesterase (AchE) in vivo
9. Brain acetylcholinesterase activity: Validation of a PET tracer in a rat model of Alzheimer's Disease
10. Measurement of acetylocholinesterase by positron emission tomograph in the brains of health controls and patients with Alzheimer's disease
11. Simplified methods for in vivo measurement of acetylcholinesterase activity in rodent brain
12. 11C]PMP)
13. Shades of gray: Radiopharmaceutical chemistry in the 1990s and beyond
14. Limited donepezil inhibition of acetylcholinesterase measured with positron emission tomography in living Alzheimer cerebral cortex
15. Radiolabeling of an acetylcholinesterase inbibitor: P-[18F]fluorodonepezil
16. Simple preparation of a novol C-11 acetylcholinesterase inhibitor
17. In vivo measurement of acetylcholinesterase activity in the brain with a radioactive acetylcholine analog
18. Necropsy evidence of central cholinergic deficts in senile dementia
19. 11C]-sarin
20. Microchemical pathology of the cerebral cortex in pre-senile dementias
21. In vivo visulization of acetylcholinesterase with positron emission tomograph
22. Pyridostigmine, a carbamate acetylcholinesterase AchE inhibitor and reactivator, is used prophylactically against chemical warfare agents
23. 18F]fluoroethyl bromide
24. An automated synthesis of [18F]fluoroethyl bromide by distillation and its application to the synthesis of [18F]fluoroethyl-P4A, a PET tracer for measurement of acetylcholinesterase activity