KOR agonist 7

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. It shows no activity on μ and δ opioid receptors or the σ1 receptor, and exhibits very low affinity for the σ2 receptor (Ki = 2.8 μM) . This compound significantly reduces the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, and IFN-γ, while increasing the secretion of the anti-inflammatory cytokine IL-10. Additionally, KOR agonist 7 decreases the expression of pro-inflammatory M1 macrophage marker (CD80) and increases the expression of anti-inflammatory M2 macrophage marker (CD163) . It can be utilized for pain relief and immunomodulation.