From Wikipedia

Ohmefentanyl (β-hydroxy-3-methylfentanyl) is an extremely potent analgesic drug which selectively binds to the µ-opioid receptor.

Ohmefentanyl is one of the most potent μ-receptor agonists known, comparable to super-potent opioids such as carfentanil and etorphine which are used for tranquilizing large animals such as elephants in veterinary medicine. In mouse studies, the most active isomer 3R,4S,βS-ohmefentanyl was 28 times more powerful as a painkiller than fentanyl, the chemical from which it is derived, and 6300 times more effective than morphine.^[1]. Ohmefentanyl has three stereogenic centers and so has eight stereoisomers, which are named F9201-F9208. Researchers are studying the different pharmaceutical properties of these isomers.^[2].

The 4"-fluoro analogue of the 3R,4S,βS isomer of ohmefentanyl is the most potent opioid yet discovered, possessing an analgesic potency approximately 18,000-fold greater than morphine.^[3]

References

1. ↑ Guo, GW; He; Jin; Zou; Zhu; Chi (2000). [Expression error: Missing operand for > "Comparison of physical dependence of ohmefentanyl stereoisomers in mice"]. Life sciences 67 (2): 113–20. PMID 10901279.  edit
2. ↑ Liu, Z.; He, Y.; Jin, W.; Chen, X.; Shen, Q.; Chi, Z. (2004). [Expression error: Missing operand for > "Effect of chronic treatment of ohmefentanyl stereoisomers on cyclic AMP formation in Sf9 insect cells expressing human mu-opioid receptors"]. Life sciences 74 (24): 3001–3008. doi:10.1016/j.lfs.2003.10.027. PMID 15051423.  edit
3. ↑ Yong, Z; Hao; Weifang; Qiyuan; Xinjian; Wenqiao; Youcheng (2003). [Expression error: Missing operand for > "Synthesis and analgesic activity of stereoisomers of cis-fluoro-ohmefentanyl"]. Die Pharmazie 58 (5): 300–2. PMID 12779044.  edit

See also

• Opioid
• Fentanyl
• Signal transduction
• Regulation of gene expression
• Protein kinase

External links

• MeSH Ohmefentanyl