Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase …

…, GG Muccioli, S De Bruyne, L Moerman…

Index: Wyffels, Leonie; Muccioli, Giulio G.; De Bruyne, Sylvie; Moerman, Lieselotte; Sambre, Johan; Lambert, Didier M.; De Vos, Filip Journal of Medicinal Chemistry, 2009 , vol. 52, # 15 p. 4613 - 4622

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Citation Number: 24

Abstract

Fatty acid amide hydrolyase (FAAH) is one of the main enzymes responsible for terminating the signaling of endocannabinoids in the brain. Imaging FAAH in vivo using PET or SPECT is important to deeper understanding of its role in neuropsychiatric disorders. However, at present, no radioligand is available for mapping the enzyme in vivo. Here, we synthesized 18 aryl analogues of anandamide, FAAH's endogenous substrate, and in vitro evaluated ...