- Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein - Potential novel positron emitting tomography imaging agents
-
A series of novel ligands based on the diaryl anilide (DAA) class of translocator protein (TSPO) ligands was synthesised and evaluated as potential positron emitting tomography (PET) ligands for imaging TPSO in vivo. Fluorine-18 labelling of the molecules was achieved using direct radiolabelling or synthon based labelling approaches. Several of the ligands prepared have promising profiles as potential TSPO PET imaging ligands and will be evaluated further as potential clinical imaging agents.
- Wadsworth, Harry,Jones, Paul A.,Chau, Wai-Fung,Durrant, Clare,Morisson-Iveson, Veronique,Passmore, Joanna,O'Shea, Dennis,Wynn, Duncan,Khan, Imtiaz,Black, Andrew,Avory, Michelle,Trigg, William
-
p. 5795 - 5800,6
(2020/07/30)
-
- Synthesis of [11C]FEDAA1106 as a new PET imaging probe of peripheral benzodiazepine receptor expression
-
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
- Wang, Min,Gao, Mingzhang,Hutchins, Gary D.,Zheng, Qi-Huang
-
experimental part
p. 2748 - 2753
(2009/09/25)
-
- Phenyloxyaniline derivatives
-
The present invention relates to phenyloxyaniline derivatives, to methods of their production and to uses thereof.
- -
-
Page/Page column 24
(2008/06/13)
-
- N-(5-fluoro-2-phenoxyphenyl)-N-(2-[131I]iodo-5-methoxybenzyl) acetamide: A potent iodinated radioligand for the peripheral-type benzodiazepine receptor in brain
-
To image the peripheral-type benzodiazepine receptor (PBR) in vivo, we previously developed two positron emission tomography (PET) ligands, N-(2-[ 11C],5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide ([ 11C]1a) and its [sup
- Zhang, Ming-Rong,Kumata, Katsushi,Maeda, Jun,Haradahira, Terushi,Noguchi, Junko,Suhara, Tetsuya,Halldin, Christer,Suzuki, Kazutoshi
-
p. 848 - 855
(2007/10/03)
-
- Synthesis of N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)[carbonyl- 11C]acetamide ([carbonyl- 11C]DAA1106) and analogues using [11C]carbon monoxide and palladium(0) complex
-
N-(2,5-Dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetomide (DAA1106), a potent and selective ligand for peripheral benzodiazepine receptor, and eight structurally related analogues were labelled with 11C at the carbonyl position using a low
- Rahman, Obaidur,Langstroem, Bengt
-
p. 1192 - 1199
(2008/04/05)
-
- CARBON-ISOTOPE MONOXIDE LABELING OF DAA1106 AND ITS ANALOGUES TO BE USED AS TRACERS FOR A PERIPHERAL TYPE BENZODIAZEPINE BINDING SITE
-
A potent and selective ligand for peripheral benzodiazepine receptor (PBR), N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide or DAA1106 and eight structurally related analogues were labelled with 11C at carbonyl position of the mol
- -
-
Page/Page column 42-43
(2010/11/26)
-
- Design, synthesis and structure-affinity relationships of aryloxyanilide derivatives as novel peripheral benzodiazepine receptor ligands
-
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.
- Okubo, Taketoshi,Yoshikawa, Ryoko,Chaki, Shigeyuki,Okuyama, Shigeru,Nakazato, Atsuro
-
p. 423 - 438
(2007/10/03)
-
- NON-STEROIDAL PROGESTERONE RECEPTOR MODULATORS
-
The present invention provides compounds according to general Formula (I), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a prodrug thereof. More particularly, the present invention provides high affinity non-steroidal compounds which are agonists, partial agonists or antagonists of the progesterone receptor.
- -
-
Page/Page column 23-24
(2010/02/07)
-