Mixed opioid receptor agonist/antagonist. Acts as a potent and full agonist at κ
, a partial agonist at μ
opioid receptors (pEC50
values are 9.45, 8.74 and 8.61 in a cAMP assay, 9.70, 8.59 and 8.49 in a [35
S binding assay respectively). Fails to exert agonist effects at NOP receptors and antagonizes agonist-induced NOP activation. Stimulates κ
- and δ
-mediated analgesia and blocks NOP-induced supraspinal nociception.
Soluble to 50 mM in DMSO
Desiccate at +4°C
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