Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor

Albert D. Windhorst; Henk Timmerman; Rob P. Klok; Wiro M.P.B. Menge; Rob Leurs; Jacobus D.M. Herscheid

doi:10.1016/S0968-0896(99)00108-X

Evaluation of [¹⁸F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H₃ receptor

Albert D. Windhorst^*, Henk Timmerman, Rob P. Klok, Wiro M.P.B. Menge, Rob Leurs, Jacobus D.M. Herscheid

^*Corresponding author for this work

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

Abstract

[¹⁸F]VUF 5000 was evaluated as a potential PET ligand for the histamine H₃ receptor. In the rat a high uptake of [¹⁸F]VUF 5000 was observed in liver, lung and kidney and a low uptake in the brain. In order to explain these findings we determined the LogD(oct,7.2) of [¹⁸F]VUF 5000, studied the biodistribution in the presence of carrier VUF 5000, modified [¹⁸F]VUF 5000 chemically and studied the binding of [¹⁸F]VUF 5000 to human serum albumin. From the results of these experiments it was concluded that [¹⁸F]VUF 5000 is not suitable as a PET ligand for brain imaging of the histamine H₃ receptor, since [¹⁸F]VUF 5000 hardly penetrates into the brain.

Original language	English
Pages (from-to)	1761-1767
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry
Volume	7
Issue number	9
DOIs	https://doi.org/10.1016/S0968-0896(99)00108-X
Publication status	Published - 1 Sep 1999

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10.1016/S0968-0896(99)00108-X

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title = "Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor",

abstract = "[18F]VUF 5000 was evaluated as a potential PET ligand for the histamine H3 receptor. In the rat a high uptake of [18F]VUF 5000 was observed in liver, lung and kidney and a low uptake in the brain. In order to explain these findings we determined the LogD(oct,7.2) of [18F]VUF 5000, studied the biodistribution in the presence of carrier VUF 5000, modified [18F]VUF 5000 chemically and studied the binding of [18F]VUF 5000 to human serum albumin. From the results of these experiments it was concluded that [18F]VUF 5000 is not suitable as a PET ligand for brain imaging of the histamine H3 receptor, since [18F]VUF 5000 hardly penetrates into the brain.",

keywords = "F, Biodistribution, Histamine H receptor, Positron emission tomography, Thioperamide, VUF 5000",

author = "Windhorst, {Albert D.} and Henk Timmerman and Klok, {Rob P.} and Menge, {Wiro M.P.B.} and Rob Leurs and Herscheid, {Jacobus D.M.}",

year = "1999",

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doi = "10.1016/S0968-0896(99)00108-X",

language = "English",

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T1 - Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor

AU - Windhorst, Albert D.

AU - Timmerman, Henk

AU - Klok, Rob P.

AU - Menge, Wiro M.P.B.

AU - Leurs, Rob

AU - Herscheid, Jacobus D.M.

PY - 1999/9/1

Y1 - 1999/9/1

N2 - [18F]VUF 5000 was evaluated as a potential PET ligand for the histamine H3 receptor. In the rat a high uptake of [18F]VUF 5000 was observed in liver, lung and kidney and a low uptake in the brain. In order to explain these findings we determined the LogD(oct,7.2) of [18F]VUF 5000, studied the biodistribution in the presence of carrier VUF 5000, modified [18F]VUF 5000 chemically and studied the binding of [18F]VUF 5000 to human serum albumin. From the results of these experiments it was concluded that [18F]VUF 5000 is not suitable as a PET ligand for brain imaging of the histamine H3 receptor, since [18F]VUF 5000 hardly penetrates into the brain.

AB - [18F]VUF 5000 was evaluated as a potential PET ligand for the histamine H3 receptor. In the rat a high uptake of [18F]VUF 5000 was observed in liver, lung and kidney and a low uptake in the brain. In order to explain these findings we determined the LogD(oct,7.2) of [18F]VUF 5000, studied the biodistribution in the presence of carrier VUF 5000, modified [18F]VUF 5000 chemically and studied the binding of [18F]VUF 5000 to human serum albumin. From the results of these experiments it was concluded that [18F]VUF 5000 is not suitable as a PET ligand for brain imaging of the histamine H3 receptor, since [18F]VUF 5000 hardly penetrates into the brain.

KW - F

KW - Biodistribution

KW - Histamine H receptor

KW - Positron emission tomography

KW - Thioperamide

KW - VUF 5000

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U2 - 10.1016/S0968-0896(99)00108-X

DO - 10.1016/S0968-0896(99)00108-X

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AN - SCOPUS:0032589505

VL - 7

SP - 1761

EP - 1767

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

SN - 0968-0896

IS - 9

ER -

Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor

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Evaluation of [¹⁸F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H₃ receptor