O-1812 Explained

O-1812 is an eicosanoid derivative related to anandamide that acts as a potent and highly selective agonist for the cannabinoid receptor CB₁, with a K_i of 3.4 nM at CB₁ and 3870 nM at CB₂.^[1] Unlike most related compounds, O-1812 is metabolically stable against rapid breakdown by enzymes, and produces a cannabinoid-like discriminative effect in rats, which is similar but not identical to that produced by cannabinoid drugs of other chemical classes.^{[2] [3] [4] [5]}

See also

• AM-1235
• AM-2232
• AM-2389
• Methanandamide
• O-774
• O-1057

Notes and References

1. Di Marzo V, etal . Highly selective CB₁ cannabinoid receptor ligands and novel CB₁/VR₁ vanilloid receptor "hybrid" ligands . Biochemical and Biophysical Research Communications . 281 . 2 . 444–51 . February 2001 . 11181068 . 10.1006/bbrc.2001.4354 .
2. Baskfield CY, Martin BR, Wiley JL . Differential effects of Δ⁹-tetrahydrocannabinol and methanandamide in CB₁ knockout and wild-type mice . The Journal of Pharmacology and Experimental Therapeutics . 309 . 1 . 86–91 . April 2004 . 14718593 . 10.1124/jpet.103.055376 . 36621393 .
3. Wiley JL, etal . A comparison of the discriminative stimulus effects of Δ⁹-tetrahydrocannabinol and O-1812, a potent and metabolically stable anandamide analog, in rats . . 12 . 3 . 173–9 . August 2004 . 15301634 . 10.1037/1064-1297.12.3.173 .
4. Wiley JL, Smith FL, Razdan RK, Dewey WL . Task specificity of cross-tolerance between Δ⁹-tetrahydrocannabinol and anandamide analogs in mice . European Journal of Pharmacology . 510 . 1–2 . 59–68 . March 2005 . 15740725 . 10.1016/j.ejphar.2005.01.006 .
5. Breivogel CS, etal . Sensitivity to Δ⁹-tetrahydrocannabinol is selectively enhanced in β-arrestin2 -/- mice . Behavioural Pharmacology . 19 . 4 . 298–307 . July 2008 . 18622177 . 2751575 . 10.1097/FBP.0b013e328308f1e6 .