1190749-75-7Relevant academic research and scientific papers
Development of a High-Affinity PET Radioligand for Imaging Cannabinoid Subtype 2 Receptor
Moldovan, Rare?-Petru,Teodoro, Rodrigo,Gao, Yongjun,Deuther-Conrad, Winnie,Kranz, Mathias,Wang, Yuchuan,Kuwabara, Hiroto,Nakano, Masayoshi,Valentine, Heather,Fischer, Steffen,Pomper, Martin G.,Wong, Dean F.,Dannals, Robert F.,Brust, Peter,Horti, Andrew G.
, p. 7840 - 7855 (2016)
Cannabinoid receptors type 2 (CB2) represent a target with increasing importance for neuroimaging due to its upregulation under various pathological conditions. Encouraged by preliminary results obtained with [11C](Z)-N-(3-(2-methoxyethyl)-4,5-dimethylthiazol-2(3H)-ylidene)-2,2,3,3-tetramethyl-cyclopropanecarboxamide ([11C]A-836339, [11C]1) in a mouse model of acute neuroinflammation (induced by lipopolysaccharide, LPS), we designed a library of fluorinated analogues aiming for an [18F]-labeled radiotracer with improved CB2 binding affinity and selectivity. Compound (Z)-N-(3-(4-fluorobutyl)-4,5-dimethylthiazol-2(3H)-ylidene)-2,2,3,3-tetramethyl-cyclopropanecarboxamide (29) was selected as the ligand with the highest CB2 affinity (Ki = 0.39 nM) and selectivity over those of CB1 (factor of 1000). [18F]29 was prepared starting from the bromo precursor (53). Specific binding was shown in vitro, whereas fast metabolism was observed in vivo in CD-1 mice. Animal PET revealed a brain uptake comparable to that of [11C]1. In the LPS-treated mice, a 20-30% higher uptake in brain was found in comparison to that in nontreated mice (n = 3, P 0.05).
NOVEL COMPOSITIONS FOR LABELING BIOMOLECULES AND METHODS USING SAME
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Sheet 14, (2017/12/01)
The present invention includes novel compounds useful for labeling biomolecules. The present invention further includes a novel method of labeling a biomolecule using a compound of the invention. The present invention further includes a novel method of im
Glucopyranosyl derivative and application thereof in medicines
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Paragraph 0661; 0662; 0667; 0668; 0669; 0670, (2016/10/08)
The invention relates to a glucopyranosyl derivative used as a sodium-dependent glucose transporter (SGLT) inhibitor, a medicinal composition containing the derivative, and an application of the derivative and the medicinal composition in medicines, and especially relates to the glucopyranosyl derivative represented by formula (I) or a pharmaceutically acceptable salt or all stereoisomers thereof, or the medicinal composition containing the derivative, and a use of the derivative and the medicinal composition in the preparation of medicines for treating diabetes and diabetes related diseases.
