Org 28312 Explained

Org 28312 is a drug developed by Organon International which acts as a potent cannabinoid receptor full agonist at both the CB₁ and CB₂ receptors. It was developed with the aim of finding a water-soluble cannabinoid agonist suitable for intravenous use as an analgesic, but did not proceed to human trials, with the related compound Org 28611 chosen instead due to its better penetration into the brain.^[1] The structure-activity relationships of these compounds have subsequently been investigated further leading to the development of a number of more potent analogues, derived by cyclisation around the indole or piperazine rings.^{[2] [3]}

See also

• LBP-1
• Org 28611

References

1. Adam, J. M.. Design, synthesis, and structure–activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists . 10.1039/c0md00022a . MedChemComm. Royal Society of Chemistry. 1 . 54 . 2010 . etal.
2. Kiyoi T, York M, Francis S, Edwards D, Walker G, Houghton AK, Cottney JE, Baker J, Adam JM . Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists . Bioorganic & Medicinal Chemistry Letters . 20 . 16 . 4918–21 . August 2010 . 20634067 . 10.1016/j.bmcl.2010.06.067 .
3. Moir EM, Yoshiizumi K, Cairns J, Cowley P, Ferguson M, Jeremiah F, Kiyoi T, Morphy R, Tierney J, Wishart G, York M, Baker J, Cottney JE, Houghton AK, McPhail P, Osprey A, Walker G, Adam JM . Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists . Bioorganic & Medicinal Chemistry Letters . 20 . 24 . 7327–30 . December 2010 . 21074434 . 10.1016/j.bmcl.2010.10.061 .