142665-13-2Relevant articles and documents
Fluorescent-Labeled Selective Adenosine A2B Receptor Antagonist Enables Competition Binding Assay by Flow Cytometry
K?se, Meryem,Gollos, Sabrina,Karcz, Tadeusz,Fiene, Amelie,Heisig, Fabian,Behrenswerth, Andrea,Kie?-Kononowicz, Katarzyna,Namasivayam, Vigneshwaran,Müller, Christa E.
, p. 4301 - 4316 (2018/05/07)
Fluorescent ligands represent powerful tools for biological studies and are considered attractive alternatives to radioligands. In this study, we developed fluorescent antagonists for A2B adenosine receptors (A2BARs), which are targeted by antiasthmatic xanthines and were proposed as novel targets in immuno-oncology. Our approach was to merge a small borondipyrromethene (BODIPY) derivative with the pharmacophore of 8-substituted xanthine derivatives. On the basis of the design, synthesis, and evaluation of model compounds, several fluorescent ligands were synthesized. Compound 29 (PSB-12105), which displayed high affinity for human, rat, and mouse A2BARs (Ki = 0.2-2 nM) and high selectivity for this AR subtype, was selected for further studies. A homology model of the human A2BAR was generated, and docking studies were performed. Moreover, 29 allowed us to establish a homogeneous receptor-ligand binding assay using flow cytometry. These compounds constitute the first potent, selective fluorescent A2BAR ligands and are anticipated to be useful for a variety of applications.
Selective, high affinity A2B adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines
Kalla, Rao V.,Elzein, Elfatih,Perry, Thao,Li, Xiaofen,Gimbel, Art,Yang, Ming,Zeng, Dewan,Zablocki, Jeff
, p. 1397 - 1401 (2008/09/21)
A series of N-1 monosubstituted 8-pyrazolyl xanthines have been synthesized and evaluated for their affinity for the adenosine receptors (AdoRs). We have discovered two compounds 18 (CVT-7124) and 28 (CVT-6694) that display good affinity for the A2B AdoR (Ki = 6 nM and 7 nM, respectively) and greater selectivity for the human A1, A2A, and A3 AdoRs (>1000-, >830-, and >1500-fold; >850-, >700-, and >1280-fold, respectively). CVT-6694 has been shown to block the release of interleukin-6 and monocyte chemotactic protein-1 from bronchial smooth muscle cells (BSMC), a process believed to be promoted by activation of A2B AdoR.
Method of wound healing using A2B adenosine receptor antagonists
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Page/Page column 19, (2008/06/13)
The present invention relates to methods of wound healing using A2B adenosine receptor antagonists. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.