On the Mechanism of Interaction of Potent Surmountable and Insurmountable Antagonists with the Prostaglandin D2 Receptor CRTH2

  title={On the Mechanism of Interaction of Potent Surmountable and Insurmountable Antagonists with the Prostaglandin D2 Receptor CRTH2},
  author={J. Mathiesen and A. Christopoulos and T. Ulven and J. F. Royer and M. Campillo and A. Heinemann and L. Pardo and E. Kostenis},
  journal={Molecular Pharmacology},
  pages={1441 - 1453}
  • J. Mathiesen, A. Christopoulos, +5 authors E. Kostenis
  • Published 2006
  • Chemistry, Medicine
  • Molecular Pharmacology
  • Chemoattractant receptor-homologous molecule expressed on T helper 2 cells (CRTH2) has attracted interest as a potential therapeutic target in inflammatory diseases. Ramatroban, a thromboxane A2 receptor antagonist with clinical efficacy in allergic rhinitis, was recently found to also display potent CRTH2 antagonistic activity. Here, we present the pharmacological profile of three ramatroban analogs that differ chemically from ramatroban by either a single additional methyl group (TM30642), or… CONTINUE READING
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