Structure-activity relationships of suramin and pyridoxal-5'-phosphate derivatives as P2 receptor antagonists.

摘要: Extracellular adenine and uracil 5-nucleotides are important signalling molecules that exert a great variety of effects in numerous tissues cell types through the activation P2 receptors. In past eight years, an extended series receptors (P2X1-7, ionotropic subunits, P2Y1,2,4,6,11,12, metabotropic receptors) has been cloned from vertebrate tissues. this rapidly expanding field, one main current challenges is to relate receptor subtypes diverse physiological responses mediated by pharmacological phenotypes native Unfortunately, subtype-selective ligands, especially potent selective antagonists, have only slowly forthcoming, acts as considerable impediment progress. However, number new antagonists recently described which some degree more than earlier like suramin or pyridoxal-5- phosphate-6-azophenyl-2,4-disulfonic acid (PPADS). This work moves us closer ideal goal classifying recombinant on basis antagonist profiles. review begins with brief account status their ligands. It then focuses structureactivity relationships PPADS analogues will finish discussion related therapeutic possibilities.