Table 1 Sequences of opioid peptides and their activity in β-arrestin-1 recruitment.

From: The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides

  

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

  1. EC50 values are indicated in nanomolar (nM) with 95% confidence interval (CI).
  2. Max: maximum signal measured at 3 µM expressed as % of the positive control/reference peptide.
  3. ND: Not determinable since saturation was not reached.
  4. NA: No activity or activity below 10% of positive control in the concentration range tested.
  5. YGGF motif conserved in most of the opioid peptides is bold.
  6. Full name of FΨG nociceptin 1–13: [Phe1Ψ(CH2-NH)-gly2]nociceptin-(1–13)-NH2.
  7. aMeasured at 9 μM.