| Literature DB >> 10530922 |
A D Windhorst1, H Timmerman, R P Klok, W M Menge, R Leurs, J D Herscheid.
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.Entities:
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Year: 1999 PMID： 10530922 DOI： 10.1016/s0968-0896(99)00108-x
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641