A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain.

Mathis CA; Bacskai BJ; Kajdasz ST; McLellan ME; Frosch MP; Hyman BT; Holt DP; Wang Y; Huang GF; Debnath ML; Klunk WE

doi:10.1016/s0960-894x(01)00734-x

A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain.

Wang Y ,

Affiliations

1. PET Facility, Department of Radiology, University of Pittsburgh, PA 15213, USA.
Authors
Mathis CA¹
(1 author)

ORCIDs linked to this article

Bioorganic & Medicinal Chemistry Letters, 01 Feb 2002, 12(3):295-298
https://doi.org/10.1016/s0960-894x(01)00734-x PMID: 11814781

Abstract

The synthesis of a new lipophilic thioflavin-T analogue (2-[4' -(methylamino)phenyl]benzothiazole, 6) with high affinity for amyloid is reported. Intravenous injection of [(11)C]-labeled 6 in control mice resulted in high brain uptake. Amyloid deposits were imaged with multiphoton microscopy in the brains of living transgenic mice following the systemic injection of unlabeled 6. [(11)C]6 is a promising amyloid imaging agent for Alzheimer's disease.

Full text links

Read article at publisher's site: https://doi.org/10.1016/s0960-894x(01)00734-x

References

Articles referenced by this article (25)

Biological markers of Alzheimer's disease.
Klunk WE
Neurobiol Aging, (2):145-147 1998
MED: 9558151
Title not supplied
Cutler
Prog. Neuro-Psychopharm. Biolog. Psych. 2001
Imaging Alzheimer's amyloid.
Selkoe DJ
Nat Biotechnol, (8):823-824 2000
MED: 10932146
Development of small molecule probes for the beta-amyloid protein of Alzheimer's disease.
Klunk WE, Debnath ML, Pettegrew JW
Neurobiol Aging, (6):691-698 1994
MED: 7891823
Title not supplied
Mathis
J. Labelled Compd. Radiopharm. 1997
Synthesis and amyloid binding properties of rhenium complexes: preliminary progress toward a reagent for SPECT imaging of Alzheimer's disease brain.
Zhen W, Han H, Anguiano M, Lemere CA, Cho CG, Lansbury PT Jr
J Med Chem, (15):2805-2815 1999
MED: 10425090
99mTc-MAMA-chrysamine G, a probe for beta-amyloid protein of Alzheimer's disease.
Dezutter NA, Dom RJ, de Groot TJ, Bormans GM, Verbruggen AM
Eur J Nucl Med, (11):1392-1399 1999
MED: 10552079
In vivo detection of amyloid plaques in a mouse model of Alzheimer's disease.
Skovronsky DM, Zhang B, Kung MP, Kung HF, Trojanowski JQ, Lee VM
Proc Natl Acad Sci U S A, (13):7609-7614 2000
MED: 10861023
Title not supplied
Agdeppa
J. Labelled Compd. Radiopharm., S242- 2001
Uncharged thioflavin-T derivatives bind to amyloid-beta protein with high affinity and readily enter the brain.
Klunk WE, Wang Y, Huang GF, Debnath ML, Holt DP, Mathis CA
Life Sci, (13):1471-1484 2001
MED: 11554609

Show 10 more references (10 of 25)

Citations & impact

Impact metrics

177

Citations

Jump to Citations

Data citations

Jump to Data

Citations of article over time

Alternative metrics

Altmetric item for https://www.altmetric.com/details/3131878

Altmetric
Discover the attention surrounding your research
https://www.altmetric.com/details/3131878

Article citations

Crystal Violet Selectively Detects Aβ Oligomers but Not Fibrils In Vitro and in Alzheimer's Disease Brain Tissue.
Karunarathne K, Kee TR, Jeon H, Cazzaro S, Gamage YI, Pan J, Woo JA, Kang DE, Muschol M
Biomolecules, 14(6):615, 23 May 2024
Cited by: 0 articles | PMID: 38927020
Multicenter Experience with Good Manufacturing Practice Production of [¹¹C]PiB for Amyloid Positron Emission Tomography Imaging.
Andersen ABA, Lehel S, Grove EK, Langkjaer N, Fuglø D, Huynh THV
Pharmaceuticals (Basel), 17(2):217, 07 Feb 2024
Cited by: 0 articles | PMID: 38399432 | PMCID: PMC10892710
This article is in the Europe PMC Open access subset. Refer to the copyright information in the article for licensing details.
Free full text in Europe PMC
Automated Synthesis of [¹¹C]PiB via [¹¹CH₃OTf]-as Methylating Agent for PET Imaging of β-Amyloid.
Singh AK, Gambhir S, Dixit M
Curr Radiopharm, 17(3):302-311, 01 Jan 2024
Cited by: 0 articles | PMID: 38454773
Repurposing of the PET Probe Prototype PiB for Label and Radiation-Free CEST MRI Molecular Imaging of Amyloid.
Zhuang C, Chen B, Wu S, Xu L, Zhang X, Zheng X, Chen Y, Geng Y, Guan J, Lin Y, Wilman AH, Wu R
ACS Chem Neurosci, 14(24):4344-4351, 07 Dec 2023
Cited by: 1 article | PMID: 38061891
Protein and Gene Delivery Systems for Neurodegenerative Disorders: Where Do We Stand Today?
Siafaka PI, Okur ME, Erim PD, Çağlar EŞ, Özgenç E, Gündoğdu E, Köprülü REP, Karantas ID, Üstündağ Okur N
Pharmaceutics, 14(11):2425, 10 Nov 2022
Cited by: 6 articles | PMID: 36365243 | PMCID: PMC9698227
Review
This article is in the Europe PMC Open access subset. Refer to the copyright information in the article for licensing details.
Free full text in Europe PMC

Go to all (177) article citations

Other citations

Wikipedia

https://en.wikipedia.org/wiki/Positron_emission_tomography

Data

Data that cites the article

This data has been provided by curated databases and other sources that have cited the article.

Small molecules (chemicals) in ChEMBL (Showing 10 of 10)

Mus musculus(CHEMBL - CHEMBL375)
2-(4-Dimethylamino-phenyl)-3,6-dimethyl-benzothiazol-3-ium(CHEMBL - CHEMBL57267)
Octanol-water partition at pH 7.4(CHEMBL - CHEMBL636384)
In vitro binding using synthetic aggregated Abeta(1-40) fibrils(CHEMBL - CHEMBL636886)
Compound was tested in vivo for mouse brain uptake after 2 min; Mouse brain uptake per g(CHEMBL - CHEMBL721009)
Compound was tested in vivo for mouse brain uptake after 30 min; Mouse brain uptake per g(CHEMBL - CHEMBL721010)
Ratio of 2-30 min mouse brain uptakes per g was determined(CHEMBL - CHEMBL849031)
(4-Benzothiazol-2-yl-phenyl)-methyl-amine(CHEMBL - CHEMBL93334)
Methyl-[4-(6-methyl-benzothiazol-2-yl)-phenyl]-amine(CHEMBL - CHEMBL330529)
In vitro binding using synthetic aggregated Abeta(1-40) fibrils(CHEMBL - CHEMBL636887)

Show less

Funding

Funders who supported this work.

NIA NIH HHS (3)

Grant ID: AG08487
135 publications
Grant ID: AG18402
9 publications
Grant ID: AG15379
50 publications

Search life-sciences literature (45,103,589 articles, preprints and more)

A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain.

Author information

Affiliations

Authors

ORCIDs linked to this article

Abstract

Full text links

References

Title not supplied

Title not supplied

Title not supplied

Citations & impact

Impact metrics

Citations of article over time

Alternative metrics

Article citations

Other citations

Wikipedia

Data

Data that cites the article

Small molecules (chemicals) in ChEMBL (Showing 10 of 10)

Similar Articles

Funding

NIA NIH HHS (3)﻿

Partnerships & funding

NIA NIH HHS (3)