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  • P2Y1
  • The determination of the X-ray crystallographic structures of the P2Y1 receptor and an agonist bound A2A adenosine receptor by our lab in collaboration with Ray Stevens of Scripps Research Institute is providing a new path to designing drugs that act at these receptors. (nih.gov)
  • We have synthesized the first P2Y1 receptor-selective antagonists through functionalization of adenine nucleotides. (nih.gov)
  • potent
  • Substances developed as potent and selective agents acting through adenosine and P2 receptors have proven useful as pharmacological probes and have potential for treating diseases of the central nervous system, immune system, and cardiovascular system. (nih.gov)
  • Recent accomplishments include the design and synthesis of the highly potent and selective A3 adenosine receptor agonists and antagonists, using a combination of library screening and optimization of known adenosine receptor ligands. (nih.gov)
  • Data produced by the group, using animal models, demonstrates potent anticonvulsive and antiepileptogenic properties of P2X7 antagonists and, critically, suggests a disease-modifying potential for P2X7 antagonism. (purines-epilepsylab.eu)
  • Novel
  • Novel ligands (small molecules) for these receptors are developed using classical synthetic approaches and also by semirational methods based on molecular modeling and template design. (nih.gov)
  • To further advance P2X7 targeting into the clinic, however, we must establish signalling pathways downstream of P2X7 and test the effectiveness of novel, brain stable P2X7 antagonists in both animal models relevant to the human condition and patient tissue. (purines-epilepsylab.eu)
  • human
  • Our overall goals are to design, chemically synthesize, and characterize pharmacologically new agonists and antagonists for the four subtypes of adenosine receptors (ARs) and eight subtypes of P2Y receptors and to explore their potential for treating human disease conditions. (nih.gov)