It is an irreversible agonist, with a reactive thiocyanate group that forms a bond to the κ-opioid receptor (KOR), resulting in very high potency.

[1] It is functionally selective, activating G proteins more potently than β-arrestin-2.

[2] RB-64 has a bias factor of up to 96 and is analgesic with fewer of the side-effects associated with unbiased KOR agonists.

Compared with unbiased agonists, RB-64 evokes considerably less receptor internalization.

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