3512-87-6

Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC50s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.

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[1] Creed, et al. Isolation and pharmacological characterization of six opioidergic Picralima nitida alkaloids. J. Nat. Prod. 84(1), 71-80 (2021).