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. Author manuscript; available in PMC: 2016 Oct 12.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Nov 4;19(24):6978–6980. doi: 10.1016/j.bmcl.2009.10.045

Figure 2.

Figure 2

Compound 4 (KMN-21) is an antagonist in HEK-293 cells coexpressing μ- and κ-opioid receptors. Intracellular calcium release experiments were performed using appropriate agonist ligands and compounds 3-6 in HEK-293 cells stably expressing (a) mu, (b) kappa, (c& d) mu/kappa opioid receptors. Cells were transiently transfected with chimeric G-protein, Δ6-Gqi4-myr (200 ng for every 40,000 cells) and pre-incubated with antagonist compounds 3-6 (1 μM) and dye from calcium release kit (Molecular Devices). Intracellular calcium release was measured in a Flexstation apparatus (Molecular Devices) using DAMGO or U69593 (1 μM). Experiments were performed in triplicate (n=4) and significance was measured using ANOVA (** = p<0.01).