Dezocine

Dezocine is a partial agonist of the µ- and κ-opioid receptors.¹ It is selective for µ- and κ-opioid receptors (K_is = 1.46 and 22.01 nM, respectively) over the δ-opioid receptor (K_i = 398.6 nM). Dezocine inhibits the norepinephrine transporter (NET) and serotonin transporter (SERT) with K_i 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 E_max 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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1. Wang, Y.-H., Chai, J.-R., Xu, X.-J., et al. Pharmacological characterization of dezocine, a potent analgesic acting as a κ partial agonist and μ partial agonist. Sci. Rep. 8(1), 14087 (2018).

2. Liu, R., Huang, X.-P., Yeliseev, A., et al. Novel molecular targets of dezocine and their clinical implications. Anesthesiology 120(3), 714-723 (2014).

3. Morgan, D., Cook, C.D., Smith, M.A., et al. An examination of the interactions between the antinociceptive effects of morphine and various mu-opioids: the role of intrinsic efficacy and stimulus intensity. Anesth. Analg. 88(2), 407-413 (1999).

4. Song, Q., Liu, G., Liu, D., et al. Dezocine promotes T lymphocyte activation and inhibits tumor metastasis after surgery in a mouse model. Invest New Drugs 38(5), 1342-1349 (2020).