Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.

@article{Hamada2010RemovalOS,
  title={Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.},
  author={Maiko Hamada and Mitsuharu Nakamura and Masatoshi Kiuchi and Kaoru Marukawa and Ayumi Tomatsu and Kyoko Shimano and Noriko Sato and Kunio Sugahara and Mahoko Asayama and Kan Takagi and Kunitomo Adachi},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 8},
  pages={3154-68}
}
A series of 2-substituted 2-aminopropane-1,3-diols having a biphenyl moiety and their phosphate esters were synthesized to obtain sphingosine 1-phosphate receptor-1 (S1P(1)) receptor agonists with potent immunomodulatory activity accompanied by little or no effect on heart rate. Many of the synthesized compounds sufficiently decreased the number of peripheral blood lymphocytes. Some of the phosphates had potent agonism at S1P(1) but no agonism at S1P(3), which had been reported to be a receptor… CONTINUE READING

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