Table 1.
Sequences of opioid peptides and their activity in β-arrestin-1 recruitment.
| ACKR3 | MOR | DOR | KOR | NOP | ||
|---|---|---|---|---|---|---|
| Name | Sequence | EC50 nM - Max % | EC50 nM - Max % | EC50 nM - Max % | EC50 nM - Max % | EC50 nM - Max % |
| Dynorphin A | YGGFLRRIRPKLKWDNQ | 110 (94.7–129)–119 | ∼1500–66 | 240 (115–2143)–76 | 12.7 (10.5–15.2)–100 | NA–6 |
| Dynorphin A 2–17 | -GGFLRRIRPKLKWDNQ | ∼2000–87a | NA–0 | NA–0 | NA–0 | NA–0 |
| Dynorphin A 2–13 | -GGFLRRIRPKLK-NH2 | ∼6000–83a | NA–0 | NA–0 | NA–0 | NA–0 |
| Dynorphin A 1–13 | YGGFLRRIRPKLK | 61.9 (50.4–76.1)–94 | ∼2000–67 | 319 (188–1038)–81 | 2.5 (1.5–3.7)–93 | NA–6 |
| Dynorphin B | YGGFLRRQFKVVT | 727 (385–8608)–103 | ∼2000–53 | 158 (101–331)–90 | 10.9 (6.3–17.2)–99 | NA–3 |
| Leumorphin | YGGFLRRQFKVVTRSQEDPNAYSGELFDA | 1320 (841–3050)–96a | ND–17 | ∼3000–53 | 21.4 (17.4–26.4)–88 | NA–8 |
| Big Dynorphin | YGGFLRRIRPKLKWDNQKRYGGFLRRQFKVVT | 108 (89.3–133.9)–127 | 652 (502–966)–92 | 529 (251–8197)–97 | 19.1 (12.9–30.6)–138 | ND–11 |
| Adrenorphin | YGGFMRRV-NH2 | 56.5 (36.6–95.0)–96 | 41.6 (30.7–57.3)–96 | 157 (104–310)–96 | 43.5 (33.7–57.9)–98 | NA–3 |
| BAM22 | YGGFMRRVGRPEWWMDYQKRYG | 23.5 (11.0–53.1)–112 | 10.0 (7.1–13.8)–100 | 367 (193–2930)–95 | 44.2 (33.6–58.2)–111 | NA–2 |
| Met enkephalin | YGGFM | NA–0a | 419 (350–528)–95 | 16.3 (12.0–21.6)–100 | NA–2 | NA–0 |
| Nociceptin | FGGFTGARKSARKLANQ | >10,000–49a | NA–0 | NA–0 | NA–1 | 19.6 (13.4–28.5)–100 |
| Nociceptin 1–13 | FGGFTGARKSARK-NH2 | ∼10,000–63a | NA–0 | NA–0 | NA–2 | 15.7 (10.7–22.1)–107 |
| FΨG nociceptin 1–13 | [Fψ(CH2-NH)G]GFTGARKSARK-NH2 | 2966 (1660–22,000)–95a | NA–0 | NA–0 | NA–2 | 56.5 (34.9–106.7)–18 |
| Endomorphin-1 | YPWF-NH2 | ND–20a | 216 (111–8640)–95a | NA–0 | NA–0 | NA–0 |
| Endomorphin-2 | YPFF-NH2 | ND–11a | 231 (124–876)–80a | NA–0 | NA–0 | NA–0 |
| β-endorphin | YGGFMTSEKSQTPLVTLFKNAIIKNAYKKGE | ND–13a | ∼1000–85a | 441 (339–679)–102 | ND–14 | NA–0 |
| LIH383 | FGGFMRRK-NH2 | 0.61 (0.19–1.17)–99 | NA–1 | NA–1 | NA–9 | NA–1 |
EC50 values are indicated in nanomolar (nM) with 95% confidence interval (CI).
Max: maximum signal measured at 3 µM expressed as % of the positive control/reference peptide.
ND: Not determinable since saturation was not reached.
NA: No activity or activity below 10% of positive control in the concentration range tested.
YGGF motif conserved in most of the opioid peptides is bold.
Full name of FΨG nociceptin 1–13: [Phe1Ψ(CH2-NH)-gly2]nociceptin-(1–13)-NH2.
aMeasured at 9 μM.