Biodistribution of [18F] SR144385 and [18F] SR147963: Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors

William B. Mathews; Ursula Scheffel; Paige Finley; Hayden T. Ravert; Richard A. Frank; Murielle Rinaldi-Carmona; Francis Barth; Robert F. Dannals

doi:10.1016/S0969-8051(00)00152-9

Biodistribution of [¹⁸F] SR144385 and [¹⁸F] SR147963: Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors

William B. Mathews, Ursula Scheffel, Paige Finley, Hayden T. Ravert, Richard A. Frank, Murielle Rinaldi-Carmona, Francis Barth, Robert F. Dannals

School of Medicine

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

36 Scopus citations

Abstract

[¹⁸F] SR144385 and [¹⁸F] SR147963 were synthesized in a multistep reaction in which fluorine-18 was introduced by nucleophilic halogen displacement on a bromo precursor. The fluorine-18-labeled intermediate was deprotected and coupled with the appropriate alkyl amine to give the final products. Both radioligands had appropriate regional brain distribution for cannabinoid receptors with a target to nontarget ratio of 1.7 for [¹⁸F] SR147963 and 2.5 for [¹⁸F] SR144385 at 60 and 90 min postinjection, respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.

Original language	English (US)
Pages (from-to)	757-762
Number of pages	6
Journal	Nuclear Medicine and Biology
Volume	27
Issue number	8
DOIs	https://doi.org/10.1016/S0969-8051(00)00152-9
State	Published - 2000

Keywords

Cannabinoid antagonist
Fluorine-18
Mice
PET

ASJC Scopus subject areas

Molecular Medicine
Radiology Nuclear Medicine and imaging
Cancer Research

Access to Document

10.1016/S0969-8051(00)00152-9

Cite this

Mathews, W. B., Scheffel, U., Finley, P., Ravert, H. T., Frank, R. A., Rinaldi-Carmona, M., Barth, F., & Dannals, R. F. (2000). Biodistribution of [¹⁸F] SR144385 and [¹⁸F] SR147963: Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors. Nuclear Medicine and Biology, 27(8), 757-762. https://doi.org/10.1016/S0969-8051(00)00152-9

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title = "Biodistribution of [18F] SR144385 and [18F] SR147963: Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors",

abstract = "[18F] SR144385 and [18F] SR147963 were synthesized in a multistep reaction in which fluorine-18 was introduced by nucleophilic halogen displacement on a bromo precursor. The fluorine-18-labeled intermediate was deprotected and coupled with the appropriate alkyl amine to give the final products. Both radioligands had appropriate regional brain distribution for cannabinoid receptors with a target to nontarget ratio of 1.7 for [18F] SR147963 and 2.5 for [18F] SR144385 at 60 and 90 min postinjection, respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.",

keywords = "Cannabinoid antagonist, Fluorine-18, Mice, PET",

author = "Mathews, {William B.} and Ursula Scheffel and Paige Finley and Ravert, {Hayden T.} and Frank, {Richard A.} and Murielle Rinaldi-Carmona and Francis Barth and Dannals, {Robert F.}",

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T2 - Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors

AU - Mathews, William B.

AU - Scheffel, Ursula

AU - Finley, Paige

AU - Ravert, Hayden T.

AU - Frank, Richard A.

AU - Rinaldi-Carmona, Murielle

AU - Barth, Francis

AU - Dannals, Robert F.

PY - 2000

Y1 - 2000

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KW - Cannabinoid antagonist

KW - Fluorine-18

KW - Mice

KW - PET

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