PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635

Richard E. Carson; Lixin Lang; Hiroshi Watabe; Margaret G. Der; H. Richard Adams; Elaine Jagoda; Peter Herscovitch; William C. Eckelman

doi:10.1016/S0969-8051(00)00118-9

PET evaluation of [¹⁸F]FCWAY, an analog of the 5-HT_1A receptor antagonist, WAY-100635

Richard E. Carson, Lixin Lang, Hiroshi Watabe, Margaret G. Der, H. Richard Adams, Elaine Jagoda, Peter Herscovitch, William C. Eckelman

Cyclotron and Radioisotope Center (CYRIC)

National Institutes of Health

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

65 Citations (Scopus)

Abstract

We synthesized [¹⁸F]FCWAY, an analog of [carbonyl-¹¹C]WAY-100635 ([¹¹C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2- (pyridinyl))cyclohexanecarboxamide), by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [¹⁸F]FC and [¹⁸F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [¹⁸F]FCWAY has very similar kinetic characteristics to [¹¹C]WAY-100635.

Original language	English
Pages (from-to)	493-497
Number of pages	5
Journal	Nuclear Medicine and Biology
Volume	27
Issue number	5
DOIs	https://doi.org/10.1016/S0969-8051(00)00118-9
Publication status	Published - 2000 Jul

Keywords

5-HT receptors
FCWAY
Modeling
Volume of distribution

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/S0969-8051(00)00118-9

Cite this

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title = "PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635",

abstract = "We synthesized [18F]FCWAY, an analog of [carbonyl-11C]WAY-100635 ([11C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2- (pyridinyl))cyclohexanecarboxamide), by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [18F]FC and [18F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [18F]FCWAY has very similar kinetic characteristics to [11C]WAY-100635.",

keywords = "5-HT receptors, FCWAY, Modeling, Volume of distribution",

author = "Carson, {Richard E.} and Lixin Lang and Hiroshi Watabe and Der, {Margaret G.} and Adams, {H. Richard} and Elaine Jagoda and Peter Herscovitch and Eckelman, {William C.}",

year = "2000",

month = jul,

doi = "10.1016/S0969-8051(00)00118-9",

language = "English",

volume = "27",

pages = "493--497",

journal = "Nuclear Medicine and Biology",

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T1 - PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635

AU - Carson, Richard E.

AU - Lang, Lixin

AU - Watabe, Hiroshi

AU - Der, Margaret G.

AU - Adams, H. Richard

AU - Jagoda, Elaine

AU - Herscovitch, Peter

AU - Eckelman, William C.

PY - 2000/7

Y1 - 2000/7

N2 - We synthesized [18F]FCWAY, an analog of [carbonyl-11C]WAY-100635 ([11C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2- (pyridinyl))cyclohexanecarboxamide), by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [18F]FC and [18F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [18F]FCWAY has very similar kinetic characteristics to [11C]WAY-100635.

AB - We synthesized [18F]FCWAY, an analog of [carbonyl-11C]WAY-100635 ([11C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2- (pyridinyl))cyclohexanecarboxamide), by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [18F]FC and [18F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [18F]FCWAY has very similar kinetic characteristics to [11C]WAY-100635.

KW - 5-HT receptors

KW - FCWAY

KW - Modeling

KW - Volume of distribution

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