Change search
ReferencesLink to record
Permanent link

Direct link
Radiosynthesis and evaluation of [C-11-Carbonyl]-labeled carbamates as fatty acid amide hydrolase radiotracers for positron emission tomography
Show others and affiliations
2013 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 56, no 1, 201-209 p.Article in journal (Refereed) Published
Abstract [en]

Fatty acid amide hydrolase (FAAH) plays a key role in regulating the tone of the endocannabinoid system. Radiotracers are required to image and quantify FAAH activity in vivo. We have synthesized a series of potent FAAH inhibitors encompassing two classes of N-alkyl-O-arylcarbamates and radiolabeled eight of them with carbon-11. The [C-11-carbonyl]-radiotracers were evaluated in vitro and ex vivo in rats as potential FAAH imaging agents for positron emission tomography (PET). Both sets of [C-11] O-arylcarbamates showed good to excellent brain penetration and an appropriate regional distribution. Pretreatments with a FAAH inhibitor demonstrated that 80-95% of brain uptake of radioactivity constituted binding of the radiotracers to FAAH. Brain extraction measurements showed that binding to FAAH was irreversible and kinetically different for the two classes of carbamates. These promising results are discussed in terms of the requirements of a suitable radiotracer for the in vivo imaging of FAAH using PET.

Place, publisher, year, edition, pages
2013. Vol. 56, no 1, 201-209 p.
National Category
Pharmacology and Toxicology
URN: urn:nbn:se:umu:diva-65908DOI: 10.1021/jm301492yISI: 000313221600017OAI: diva2:612252
Available from: 2013-03-20 Created: 2013-02-13 Last updated: 2013-03-20Bibliographically approved

Open Access in DiVA

No full text

Other links

Publisher's full text

Search in DiVA

By author/editor
Fowler, Christopher J
By organisation
In the same journal
Journal of Medicinal Chemistry
Pharmacology and Toxicology

Search outside of DiVA

GoogleGoogle Scholar
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

Altmetric score

Total: 28 hits
ReferencesLink to record
Permanent link

Direct link