867252-29-7Relevant articles and documents
Synthesis of [11C]FEDAA1106 as a new PET imaging probe of peripheral benzodiazepine receptor expression
Wang, Min,Gao, Mingzhang,Hutchins, Gary D.,Zheng, Qi-Huang
experimental part, p. 2748 - 2753 (2009/09/25)
Peripheral benzodiazepine receptor (PBR) is associated with neuroinflammation and tumor progression. [11C]DAA1106 and [18F]FEDAA1106 are two promising radioligands for positron emission tomography (PET) imaging of PBR. This study was
Design, synthesis and structure-affinity relationships of aryloxyanilide derivatives as novel peripheral benzodiazepine receptor ligands
Okubo, Taketoshi,Yoshikawa, Ryoko,Chaki, Shigeyuki,Okuyama, Shigeru,Nakazato, Atsuro
, p. 423 - 438 (2007/10/03)
Since the peripheral benzodiazepine receptor (PBR) has been primarily found as a high-affinity binding site for diazepam in rat kidney, numerous studies of it have been performed. However, the physiological role and functions of PBR have not been fully elucidated. Currently, we presented the pharmacological profile of two high and selective PBR ligands, N-(2,5-dimethoxybenzyl)-N-(4-fluoro-2-phenoxyphenyl)acetamide (7-096, DAA1106) (PBR: IC50=0.28 nM) and N-(4-chloro-2-phenoxyphenyl)-N-(2- isopropoxybenzyl)acetamide (7-099, DAA1097) (PBR: IC50=0.92 nM). The compounds are aryloxyanilide derivatives, and identified with known PBR ligands such as benzodiazepine (1, Ro5-4864), isoquinoline (2, PK11195), imidazopyridine (3, Alpidem), and indole (5, FGIN-1-27) derivatives. The aryloxyanilide derivatives, which have been derived by opening the diazepine ring of 1, are a novel class as PBR ligands and have exhibited high and selective affinity for peripheral benzodiazepine receptors (PBRs). These novel derivatives would be useful for exploring the functions of PBR. In this paper, the design, synthesis and structure-affinity relationships of aryloxyanilide derivatives are described.
