5770-23-0Relevant articles and documents
Synthesis and Pharmacological Evaluation of Identified and Putative Metabolites of the A1 Adenosine Receptor Antagonist 8-Cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine (CPFPX)
Holschbach, Marcus H.,Bier, Dirk,Sihver, Wiebke,Schulze, Annette,Neumaier, Bernd
, p. 770 - 784 (2017/05/26)
The A1 adenosine receptor (A1AR) antagonist [18F]8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ([18F]CPFPX), used in imaging human brain A1ARs by positron emission tomography (PET), is stable in t
Allosteric competitive inhibitors of the glucose-1-phosphate thymidylyltransferase (RmlA) from pseudomonas aeruginosa
Alphey, Magnus S.,Pirrie, Lisa,Torrie, Leah S.,Boulkeroua, Wassila Abdelli,Gardiner, Mary,Sarkar, Aurijit,Maringer, Marko,Oehlmann, Wulf,Brenk, Ruth,Scherman, Michael S.,McNeil, Michael,Rejzek, Martin,Field, Robert A.,Singh, Mahavir,Gray, David,Westwood, Nicholas J.,Naismith, James H.
, p. 387 - 396 (2013/04/24)
Glucose-1-phosphate thymidylyltransferase (RmlA) catalyzes the condensation of glucose-1-phosphate (G1P) with deoxy-thymidine triphosphate (dTTP) to yield dTDP-d-glucose and pyrophosphate. This is the first step in the l-rhamnose biosynthetic pathway. l-R
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.