Chemistry:Atoxifent
From HandWiki
Atoxifent It is an extremely potent opioid; its pain-relieving effect is comparable to that of fentanyl, and atoxifent, even at doses that induce complete analgesia, does not cause severe respiratory depression.[1][2]
Pharmacology
Pharmacodynamics
Atoxifent is an agonist of the μ-opioid and δ-opioid receptors. its EC50 value for MOR is 0.39 ± 0.03 nM, with an efficacy (Emax) of 98.9 ± 0.6 per cent. Atoxifent is a partial agonist of δ-opioid receptors with an EC50 value of 2.18 ± 0.50 nM and an Emax of 56.8 ± 11.0% it is a full κ-opioid receptor antagonist with an EC50 value of 356.50 ± 106.49 nM and an Emax of 93.0 ± 2.0 per cent. It showed no affinity for nociceptin receptors.[1][2]
References
- ↑ 1.0 1.1 "Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression". Journal of Medicinal Chemistry 67 (11): 9173–9193. June 2024. doi:10.1021/acs.jmedchem.4c00333. PMID 38810170.
- ↑ 2.0 2.1 "N-(3-Hydroxyphenyl)-3,8-diazabicyclooctanes as opioid receptors probes. 1. Investigation of the phenolic hydroxyl group". European Journal of Medicinal Chemistry 298. November 2025. doi:10.1016/j.ejmech.2025.117991. PMID 40730064.
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