ECB-ART-40123
Bioorg Med Chem
2007 Apr 15;158:3032-40. doi: 10.1016/j.bmc.2007.02.001.
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Substitution at the 8-position of 3''''-deoxy-cyclic ADP-carbocyclic-ribose, a highly potent Ca2+-mobilizing agent, provides partial agonists.
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We previously showed that 3''''-deoxy-cyclic ADP-carbocyclic-ribose (3''''-deoxy-cADPcR, 4) is a stable and highly potent analogue of cyclic ADP-ribose (cADPR, 1), a Ca(2+)-mobilizing second messenger. From these results, we designed and synthesized other 3''''-modified analogues of cADPcR having a substituent at the 8-position and found that this modification at the 8-position made them partial agonists. Among these compounds, 8-NH(2)-3''''-deoxy-cADPcR (10) was identified as a potent partial agonist with an EC(50) value of 17 nM.
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