Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor.
[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.
Windhorst
A D
AD
Radionuclide Center, Vrije Universiteit, Amsterdam, The Netherlands. bwindhorst@rnc.vu.nl
Timmerman
H
H
Klok
R P
RP
Menge
W M
WM
Leurs
R
R
Herscheid
J D
JD
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D005069:Evaluation Studies as Topic; D005462:Fluorine Radioisotopes; D006801:Humans; D008297:Male; D010880:Piperidines / Q000378:metabolism* / Q000493:pharmacokinetics; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D012709:Serum Albumin / Q000378:metabolism; D013890:Thiourea / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
D005462:Fluorine Radioisotopes; D010880:Piperidines; D018100:Receptors, Histamine H3; D012709:Serum Albumin; C122192:VUF 5182; D013890:Thiourea