In vivo biodistribution of two [18F]-labelled muscarinic cholinergic receptor ligands: 2-[18F]- and 4-[18F]-fluorodexetimide

Alan A. Wilson; Ursula A. Scheffel; Robert F. Dannals; Marigo Stathis; Hayden T. Ravert; Henry N. Wagner

doi:10.1016/0024-3205(91)90435-E

In vivo biodistribution of two [¹⁸F]-labelled muscarinic cholinergic receptor ligands: 2-[¹⁸F]- and 4-[¹⁸F]-fluorodexetimide

Alan A. Wilson, Ursula A. Scheffel, Robert F. Dannals, Marigo Stathis, Hayden T. Ravert, Henry N. Wagner

School of Medicine

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

16 Scopus citations

Abstract

Two [¹⁸F]-labelled analogues of the potent muscarinic cholinergic receptor (m-AChR) antagonist, dexetimide, were evaluated as potential ligands for imaging m-AChR by positron emission tomography (PET). Intravenous administration of both 2-[¹⁸F]- or 4-[¹⁸F]- fluorodexetimide resulted in high brain uptake of radioactivity in mice. High binding levels were observed in m-AChR rich areas, such as cortex and striatum, with low levels in the receptor-poor cerebellum. Uptake of radioactivity was saturable and could be blocked by pre-administration of dexetimide or atropine. Drugs with different sites of action were ineffective at blocking receptor binding. The results indicate that both radiotracers are promising candidates for use in PET studies.

Original language	English (US)
Pages (from-to)	1385-1394
Number of pages	10
Journal	Life Sciences
Volume	48
Issue number	14
DOIs	https://doi.org/10.1016/0024-3205(91)90435-E
State	Published - 1991

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

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@article{724d907323284b4f8e6354e2098a8f94,

title = "In vivo biodistribution of two [18F]-labelled muscarinic cholinergic receptor ligands: 2-[18F]- and 4-[18F]-fluorodexetimide",

abstract = "Two [18F]-labelled analogues of the potent muscarinic cholinergic receptor (m-AChR) antagonist, dexetimide, were evaluated as potential ligands for imaging m-AChR by positron emission tomography (PET). Intravenous administration of both 2-[18F]- or 4-[18F]- fluorodexetimide resulted in high brain uptake of radioactivity in mice. High binding levels were observed in m-AChR rich areas, such as cortex and striatum, with low levels in the receptor-poor cerebellum. Uptake of radioactivity was saturable and could be blocked by pre-administration of dexetimide or atropine. Drugs with different sites of action were ineffective at blocking receptor binding. The results indicate that both radiotracers are promising candidates for use in PET studies.",

author = "Wilson, {Alan A.} and Scheffel, {Ursula A.} and Dannals, {Robert F.} and Marigo Stathis and Ravert, {Hayden T.} and Wagner, {Henry N.}",

note = "Funding Information: Christina Cromwell for her help with fluorolevetimide biodistribution studies. This work was supported in part by grant numbers CA-32845 and NS-15080 from the U.S. Public Health Service.",

year = "1991",

doi = "10.1016/0024-3205(91)90435-E",

language = "English (US)",

volume = "48",

pages = "1385--1394",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier Inc.",

number = "14",

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T1 - In vivo biodistribution of two [18F]-labelled muscarinic cholinergic receptor ligands

T2 - 2-[18F]- and 4-[18F]-fluorodexetimide

AU - Wilson, Alan A.

AU - Scheffel, Ursula A.

AU - Dannals, Robert F.

AU - Stathis, Marigo

AU - Ravert, Hayden T.

AU - Wagner, Henry N.

N1 - Funding Information: Christina Cromwell for her help with fluorolevetimide biodistribution studies. This work was supported in part by grant numbers CA-32845 and NS-15080 from the U.S. Public Health Service.

PY - 1991

Y1 - 1991

N2 - Two [18F]-labelled analogues of the potent muscarinic cholinergic receptor (m-AChR) antagonist, dexetimide, were evaluated as potential ligands for imaging m-AChR by positron emission tomography (PET). Intravenous administration of both 2-[18F]- or 4-[18F]- fluorodexetimide resulted in high brain uptake of radioactivity in mice. High binding levels were observed in m-AChR rich areas, such as cortex and striatum, with low levels in the receptor-poor cerebellum. Uptake of radioactivity was saturable and could be blocked by pre-administration of dexetimide or atropine. Drugs with different sites of action were ineffective at blocking receptor binding. The results indicate that both radiotracers are promising candidates for use in PET studies.

AB - Two [18F]-labelled analogues of the potent muscarinic cholinergic receptor (m-AChR) antagonist, dexetimide, were evaluated as potential ligands for imaging m-AChR by positron emission tomography (PET). Intravenous administration of both 2-[18F]- or 4-[18F]- fluorodexetimide resulted in high brain uptake of radioactivity in mice. High binding levels were observed in m-AChR rich areas, such as cortex and striatum, with low levels in the receptor-poor cerebellum. Uptake of radioactivity was saturable and could be blocked by pre-administration of dexetimide or atropine. Drugs with different sites of action were ineffective at blocking receptor binding. The results indicate that both radiotracers are promising candidates for use in PET studies.

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JO - Life Sciences

JF - Life Sciences

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ER -

In vivo biodistribution of two [¹⁸F]-labelled muscarinic cholinergic receptor ligands: 2-[¹⁸F]- and 4-[¹⁸F]-fluorodexetimide

Abstract

ASJC Scopus subject areas

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