Supplementary Materials

This PDF file includes:

  • Fig. S1. KOR agonists do not stimulate cAMP accumulation.
  • Fig. S2. KOR agonist potency for inhibiting forskolin-stimulated cAMP accumulation is not affected by changing the incubation time.
  • Fig. S3. RGS protein effects on KOR-regulated adenylyl cyclase activity.
  • Fig. S4. Triazole 1.1 and iso 2.1 display similar signaling profiles in CHO and U2OS cells stably expressing mouse KOR as they do expressing human KOR.
  • Fig. S5. β-arrestins are not required for KOR-regulated adenylyl cyclase activity.
  • Fig. S6. β-arrestins are required for KOR internalization.
  • Table S1. Signaling parameters for the time course inhibition of forskolin-stimulated cAMP accumulation in CHO-hKOR cells.
  • Table S2. Signaling parameters for the KOR agonists in the functional assays in CHO-mKOR cells.
  • Table S3. Signaling parameters for the KOR agonists in the inhibition of forskolin-stimulated cAMP accumulation in WT and β-arrestin1/2-KO MEF-mKOR cells.
  • Table S4. Signaling parameters for the inhibition of cAMP accumulation in CHO cells stably expressing hKOR alone or with hRGS4, hRGS9.2, or hRGS12.3.
  • Table S5. Primer sequences.

[Download PDF]