BML‐190 and AM251 act as inverse agonists at the human cannabinoid CB2 receptor: signalling via cAMP and inositol phosphates

  title={BML‐190 and AM251 act as inverse agonists at the human cannabinoid CB2 receptor: signalling via cAMP and inositol phosphates},
  author={D. C. New and Y. Wong},
  journal={FEBS Letters},
  • D. C. New, Y. Wong
  • Published 2003
  • Medicine, Chemistry
  • FEBS Letters
  • The aminoalkylindole BML‐190 and diarylpyrazole AM251 ligands have previously been shown to bind to cannabinoid CB2 and CB1 receptors, respectively. In HEK‐293 cells stably expressing the human CB2 receptor, BML‐190 and AM251 potentiated the forskolin‐stimulated accumulation of cAMP. Moreover, the CB2 receptor can interact productively with 16z44, a promiscuous Gα16/z chimera. BML‐190 and AM251 reduce the basal levels of inositol phosphate production in cells expressing the CB2 receptor and… CONTINUE READING
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