914394-64-2Relevant articles and documents
Synthesis and characterization of 18F-labeled hydrazinocurcumin derivatives for tumor imaging
Shin, Sarah,Koo, Hyun-Jung,Lee, Iljung,Choe, Yearn Seong,Choi, Joon Young,Lee, Kyung-Han,Kim, Byung-Tae
, p. 96733 - 96745 (2015/11/24)
Fluorine-substituted hydrazinocurcumin derivative 1 and its dimethyl-substituted form at the C2 and C6 positions (2) were synthesized and their radiolabeled forms, [18F]1 and [18F]2, were evaluated for tumor imaging. In vitro and in vivo metabolism studies showed that the two radioligands were resistant to reductive metabolism, probably due to the presence of a pyrazole ring. In cellular uptake studies, [18F]1 and [18F]2 exhibited comparable uptake by human umbilical vascular endothelial cells and rat C6 glioma cells. Inhibition of radioligand uptake to a similar extent by HC and curcumin suggests that these radioligands may share the same binding sites as those for HC and curcumin. Positron emission tomography imaging of C6 glioma xenografted mice acquired 30 and 60 min after radioligand injection showed that [18F]2 had markedly higher tumor uptake than [18F]1, which was consistent with biodistribution data (3.20 ± 0.35% ID per g vs. 0.98 ± 0.31% ID per g, respectively). However, the two radioligands showed similar levels of tumor-to-background uptake ratio, except for the significantly higher uptake of [18F]1 by the small intestine, indicating its more rapid clearance. The results of this study will guide further structural modifications of these radioligands to enhance tumor-to-background uptake ratios.
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A
Zhang, Zhanbin,Lu, Xiaoxia,Xu, Jinbin,Rothfuss, Justin,MacH, Robert H.,Tu, Zhude
experimental part, p. 3986 - 3995 (2011/10/31)
A series of analogues were synthesized by optimizing the structure of papaverine. The in vitro PDE10A binding affinity (IC50) values for these new analogues were measured; for compounds that have IC50 value less than 60 nM for PDE10A
IMIDAZOL [1,2-A] PYRIDINES AND RELATED COMPOUNDS WITH ACTIVITY AT CANNABINOID CB2 RECEPTORS
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Page/Page column 50-51, (2009/01/20)
Disclosed are compounds of Formula (I) or Formula (II) or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula (I) or Formula (II) with the cannabinoid CB2 receptor. Said compounds are useful in the treatment of various condition and disorders such as pain, and neurodegenerative disorders.