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Dezocine is a partial agonist of the µ- and κ-opioid receptors.1 It is selective for µ- and κ-opioid receptors (Kis = 1.46 and 22.01 nM, respectively) over the δ-opioid receptor (Ki = 398.6 nM). Dezocine inhibits the norepinephrine transporter (NET) and serotonin transporter (SERT) with Ki values of 0.001 and 109 nM, respectively.2 It stimulates [35S]GTPγS binding to CHO membranes expressing the human µ- and κ-opioid receptors with Emax values of 45.8 and 33.6% compared to the µ- and κ-agonists DAMGO and U50,488 H, respectively, when used at a concentration of 10 µM.1 It has antinociceptive effects in mice in the acetic acid abdominal constriction test (ED50 = 0.02 mg/kg) and the formalin test (ED50s = 0.4 mg/kg for both phases).1 Dezocine (10 mg/kg) increases the latency to tail withdrawal in the tail-flick test in rats.3 It also decreases the number of lung metastases in a 4T1 murine mammary cancer model when administered at doses ranging from 0.75 to 2 mg/kg.4 Formulations containing dezocine have been used in the treatment of post-operative pain.

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