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

Chester A. Mathis; Brian J. Bacskai; Stephen T. Kajdasz; Megan E. McLellan; Matthew P. Frosch; Bradley T. Hyman; Daniel P. Holt; Yanming Wang; Guo Feng Huang; Manik L. Debnath; William E. Klunk

doi:10.1016/S0960-894X(01)00734-X

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

Chester A. Mathis
, Brian J. Bacskai
, Stephen T. Kajdasz
, Megan E. McLellan
, Matthew P. Frosch
, Bradley T. Hyman
, Daniel P. Holt
, Yanming Wang
, Guo Feng Huang
, Manik L. Debnath
, William E. Klunk

Research output: Contribution to journal › Article › peer-review

302 Scopus citations

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 [¹¹C]-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. [¹¹C]6 is a promising amyloid imaging agent for Alzheimer's disease.

Original language	English (US)
Pages (from-to)	295-298
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	3
DOIs	https://doi.org/10.1016/S0960-894X(01)00734-X
State	Published - Feb 11 2002
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)00734-X

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Mathis, C. A., Bacskai, B. J., Kajdasz, S. T., McLellan, M. E., Frosch, M. P., Hyman, B. T., Holt, D. P., Wang, Y., Huang, G. F., Debnath, M. L., & Klunk, W. E. (2002). A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain. Bioorganic and Medicinal Chemistry Letters, 12(3), 295-298. https://doi.org/10.1016/S0960-894X(01)00734-X

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title = "A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain",

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 [11C]-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. [11C]6 is a promising amyloid imaging agent for Alzheimer's disease.",

author = "Mathis, \{Chester A.\} and Bacskai, \{Brian J.\} and Kajdasz, \{Stephen T.\} and McLellan, \{Megan E.\} and Frosch, \{Matthew P.\} and Hyman, \{Bradley T.\} and Holt, \{Daniel P.\} and Yanming Wang and Huang, \{Guo Feng\} and Debnath, \{Manik L.\} and Klunk, \{William E.\}",

note = "Funding Information: Financial support was provided in part by grants from the Alzheimer's Association (Pioneer Award to B.T.H. and NIRG-00-2335) and the National Institute on Aging (AG08487, AG15379, and AG18402). ",

year = "2002",

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day = "11",

doi = "10.1016/S0960-894X(01)00734-X",

language = "English (US)",

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pages = "295--298",

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T1 - A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain

AU - Mathis, Chester A.

AU - Bacskai, Brian J.

AU - Kajdasz, Stephen T.

AU - McLellan, Megan E.

AU - Frosch, Matthew P.

AU - Hyman, Bradley T.

AU - Holt, Daniel P.

AU - Wang, Yanming

AU - Huang, Guo Feng

AU - Debnath, Manik L.

AU - Klunk, William E.

N1 - Funding Information: Financial support was provided in part by grants from the Alzheimer's Association (Pioneer Award to B.T.H. and NIRG-00-2335) and the National Institute on Aging (AG08487, AG15379, and AG18402).

PY - 2002/2/11

Y1 - 2002/2/11

N2 - 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 [11C]-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. [11C]6 is a promising amyloid imaging agent for Alzheimer's disease.

AB - 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 [11C]-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. [11C]6 is a promising amyloid imaging agent for Alzheimer's disease.

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UR - https://www.scopus.com/pages/publications/0037059914#tab=citedBy

U2 - 10.1016/S0960-894X(01)00734-X

DO - 10.1016/S0960-894X(01)00734-X

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VL - 12

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 3

ER -

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

Abstract

ASJC Scopus subject areas

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