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Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles

Patent ·
OSTI ID:1174615
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A method for labeling .beta.-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I): ##STR1## with mammalian tissue. In formula (I), R.sub.1 is selected from the group consisting of --C(O)-alkyl, --C(O)-alkylenyl-R.sub.4, --C(O)O-alkyl, --C(O)O-alkylenyl-R.sub.4, --C.dbd.C(CN).sub.2 -alkyl, --C.dbd.C(CN).sub.2 -alkylenyl-R.sub.4, ##STR2## R.sub.4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R.sub.5 is a radical selected from the group consisting of --NH.sub.2, --OH, --SH, --NH-alkyl, --NHR.sub.4, --NH-alkylenyl-R.sub.4, --O-alkyl, --O-alkylenyl-R.sub.4, --S-alkyl, and --S-alkylenyl-R.sub.4 ; R.sub.6 is a radical selected from the group consisting of --CN, --COOH, --C(O)O-alkyl, --C(O)O-alkylenyl-R.sub.4, --C(O)-alkyl, --C(O)-alkylenyl-R.sub.4, --C(O)-halogen, --C(O)NH, --C(O)NH-alkyl, --C(O)NH-alkylenyl-R.sub.4 ; R.sub.7 is a radical selected from the group consisting of O, NH, and S; and R.sub.8 is N, O or S. R.sub.2 and R.sub.3 are each independently selected from the group consisting of alkyl and alkylenyl-R.sub.10, wherein R.sub.10 is selected from the group consisting of --OH, --OTs, halogen, spiperone, spiperone ketal and spiperone-3-yl. Alternatively, R.sub.2 and R.sub.3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkylenyl-R.sub.10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl. In the compounds of formula (I), one or more of the hydrogen, halogen or carbon atoms can, optionally, be replaced with a radiolabel.
Research Organization:
The Regents of the University of California, Oakland, CA (United States)
Sponsoring Organization:
USDOE
DOE Contract Number:
FC03-87ER60615
Assignee:
The Regents of the University of California (Oakland, CA)
Patent Number(s):
6,660,530
Application Number:
09/891,883
OSTI ID:
1174615
Country of Publication:
United States
Language:
English

References (14)

Interaction of the anthracycline 4'-iodo-4'-deoxydoxorubicin with amyloid fibrils: inhibition of amyloidogenesis. journal March 1995
Regional cerebral glucose metabolism in dementia with Lewy bodies and Alzheimer's disease: a comparative study using positron emission tomography journal October 1997
Application of PRODAN fluorescent probe to measure surface hydrophobicity of proteins interacting with κ-carrageenan journal May 2001
The Preparation and Use of Radioiodinated Congo Red in Detecting Amyloidosis**Received August 21, 1959, from the Radioisotope Service, Veietatis Administration Center, Los Angeles, and the Departments of Radiology and Medicine, University of California Medical Center, Los Angeles, Calif. journal July 1960
Vector-mediated delivery of 125I-labeled beta-amyloid peptide A beta 1-40 through the blood-brain barrier and binding to Alzheimer disease amyloid of the A beta 1-40/vector complex. journal October 1995
1,1-Dicyano-2-[6-(dimethylamino)naphthalen-2-yl]propene (DDNP):  A Solvent Polarity and Viscosity Sensitive Fluorophore for Fluorescence Microscopy ⊥ journal January 1996
Neuroreceptor Assay with Positron Emission Tomography: Equilibrium versus Dynamic Approaches journal October 1986
Fluorometric determination of amyloid fibrils in vitro using the fluorescent dye, thioflavine T journal March 1989
Development of small molecule probes for the Beta-amyloid protein of Alzheimer's Disease journal November 1994
Regional cerebral glucose metabolism and postmortem pathology in Alzheimer’s disease journal February 1996
Technetium Complexes for the Quantitation of Brain Amyloid journal January 1996
Receptor Changes in the Neocortex of Post-Mortem Tissue in Parkinson's Disease and Alzheimer's Disease journal January 1992
Chrysamine-G binding to Alzheimer and control brain: Autopsy study of a new amyloid probe journal August 1995
Tangles and plaques in nondemented aging and ?preclinical? Alzheimer's disease journal March 1999

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