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

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

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Abstract

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),more »« less

Inventors:

Barrio, Jorge R ^[1]; Petric, Andrej ^[2]; Satyamurthy, Nagichettiar ^[3]; Small, Gary W ^[3]; Cole, Gregory M ^[4]; Huang, Sung-Cheng ^[5]

Agoura Hills, CA
Ljubljana, SI
Los Angeles, CA
Santa Monica, CA
Sherman Oaks, CA

Publication Date:: 2001-01-01

Research Org.:: Univ. of California (United States)

OSTI Identifier:: 873929

Patent Number(s):: US 6274119

Assignee:: Regents of Univ. of California (Oakland, CA)

DOE Contract Number:: FC03-87ER60615

Resource Type:: Patent

Country of Publication:: United States

Language:: English

Subject:: methods; labeling; beta; -amyloid; plaques; neurofibrillary; tangles; method; vivo; vitro; comprises; contacting; compound; formula; str1; mammalian; tissue; selected; consisting; -c; -alkyl; -alkylenyl-r; o-alkyl; o-alkylenyl-r; dbd; cn; str2; radical; alkyl; substituted; aryl; -nh; -oh; -sh; -nh-alkyl; -nhr; -nh-alkylenyl-r; -o-alkyl; -o-alkylenyl-r; -s-alkyl; -s-alkylenyl-r; -cn; -cooh; -halogen; nh; nh-alkyl; nh-alkylenyl-r; independently; alkylenyl-r; 10; -ots; halogen; spiperone; ketal; spiperone-3-yl; alternatively; form; heterocyclic; optionally; alkoxy; oh; ots; carbonyl; compounds; hydrogen; carbon; atoms; replaced; radiolabel; radical selected; independently selected; comprises contacting; carbon atoms; carbon atom; mammalian tissue; optionally substituted; neurofibrillary tangles; substituted alkyl; -amyloid plaques; /424/

Citation Formats


                    Barrio, Jorge R, Petric, Andrej, Satyamurthy, Nagichettiar, Small, Gary W, Cole, Gregory M, and Huang, Sung-Cheng. Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles.  United States: N. p., 2001. 
        Web.

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                    Barrio, Jorge R, Petric, Andrej, Satyamurthy, Nagichettiar, Small, Gary W, Cole, Gregory M, & Huang, Sung-Cheng. Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles.  United States.

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                    Barrio, Jorge R, Petric, Andrej, Satyamurthy, Nagichettiar, Small, Gary W, Cole, Gregory M, and Huang, Sung-Cheng. Mon .  
        "Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles".  United States.  https://www.osti.gov/servlets/purl/873929.

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@article{osti_873929,

  title        = {Methods for labeling .beta.-amyloid plaques and neurofibrillary tangles},

  author       = {Barrio, Jorge R and Petric, Andrej and Satyamurthy, Nagichettiar and Small, Gary W and Cole, Gregory M and Huang, Sung-Cheng},

  abstractNote = {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.},

  doi          = {},

  url          = {https://www.osti.gov/biblio/873929},
  journal      = {},
number       = ,

  volume       = ,

  place        = {United States},

  year         = {2001},

  month        = {1}

}

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