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AM-4030

Chemical compound

Chemical compound

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AM-4030 is an analgesic drug which is a cannabinoid receptor agonist. It is a derivative of HU-210 which has been substituted with a 6β-((E)-3-hydroxyprop-1-enyl) group. This adds a "southern" aliphatic hydroxyl group to the molecule as seen in the CP-series of nonclassical cannabinoid drugs, and so AM-4030 represents a hybrid structure between the classical and nonclassical cannabinoid families, with the 6-hydroxyalkyl chain rigidified with a double bond with defined stereochemistry. This gives AM-4030 a greater degree of selectivity, so while it is still a potent agonist at both CB1 and CB2, it is reasonably selective for CB1, with a Ki of 0.7nM at CB1 and 8.6nM at CB2, a selectivity of around 12x. Resolution of the enantiomers of AM-4030 yields an even more potent compound, although with less selectivity, with the (−) enantiomer AM-4030a having a Ki of 0.6nM at CB1 and 1.1nM at CB2.

References

References

  1. Pertwee, Roger. "Cannabinoids". Springer.
  2. (1995). "Classical/non-classical cannabinoid hybrids; stereochemical requirements for the southern hydroxyalkyl chain". Life Sciences.
  3. (September 1998). "Classical/nonclassical hybrid cannabinoids: southern aliphatic chain-functionalized C-6beta methyl, ethyl, and propyl analogues". Journal of Medicinal Chemistry.
  4. (December 2002). "Enantiomeric resolution of a novel chiral cannabinoid receptor ligand". Journal of Biochemical and Biophysical Methods.
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benzochromenes primary-alcohols hydroxyarenes am-cannabinoids
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