N-Phenethyl-14-ethoxymetopon

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

N-Phenethyl-14-ethoxymetopon is a drug which is a derivative of metopon. It is a potent analgesic, around 60 times stronger than morphine, but produces significantly less constipation.^[1]

N-Phenethyl-14-ethoxymetopon acts as an agonist at both μ- and δ-opioid receptors, with a Ki of 0.16nM at μ and 3.14nM at δ.^[2]

References

↑ Ananthan S. Opioid ligands with mixed mu/delta opioid receptor interactions: an emerging approach to novel analgesics. AAPS Journal. 2006 Mar 10;8(1):E118-25. PMID 16584118
↑ Lattanzi R, Spetea M, Schüllner F, Rief SB, Krassnig R, Negri L, Schmidhammer H. Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities. Journal of Medicinal Chemistry. 2005 May 5;48(9):3372-8. PMID 15857143

Template:Opioids

Template:WikiDoc Sources

[1] Ananthan S. Opioid ligands with mixed mu/delta opioid receptor interactions: an emerging approach to novel analgesics. AAPS Journal. 2006 Mar 10;8(1):E118-25. PMID 16584118

[2] Lattanzi R, Spetea M, Schüllner F, Rief SB, Krassnig R, Negri L, Schmidhammer H. Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities. Journal of Medicinal Chemistry. 2005 May 5;48(9):3372-8. PMID 15857143

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