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.
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.
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