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

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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). ",

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

language = "English (US)",

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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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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

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