Table 2 Effects of N/OFQ(1-13)-NH2, C-terminal truncated derivatives, and their homo and heterodimers in calcium mobilization studies performed on CHO cells coexpressing the NOP receptor and the Gaqi5 chimeric protein and in the electrically stimulated mouse vas deferens bioassay.

From: Structure- and conformation-activity studies of nociceptin/orphanin FQ receptor dimeric ligands

cpd

Structure

Ca2+mobilization

mVD

pEC50 (CL95%)

Emax ± SEM

pEC50 (CL95%)

Emax ± SEM

—

N/OFQ

9.70 (9.49–9.91)

200 ± 22%

7.11 (7.00–7.22)

87 ± 5%

—

N/OFQ(1-13)-NH2

9.83 (9.51–10.16)

199 ± 20%

7.02 (6.94–7.10)

89 ± 3%

9

9.40 (9.15–9.65)

213 ± 24%

7.31 (7.14–7.49)

88 ± 3%

10

N/OFQ(1-12)-NH2

9.70 (9.41–9.98)

204 ± 16%

5.59* (5.22–5.95)

60 ± 4%a

11

9.38* (9.06–9.70)

205 ± 18%

7.27 (7.09–7.45)

84 ± 5%

12

N/OFQ(1-11)-NH2

8.21* (8.11–8.32)

182 ± 34%

5.28* (5.05–5.51)

65 ± 5%a

13

8.87* (8.58–9.16)

193 ± 22%

5.93* (5.81–6.05)

85 ± 4%

14

N/OFQ(2-12)-NH2

Inactive

inactive

15

9.49 (9.07–9.91)

205 ± 27%

7.31 (7.18–7.44)

92 ± 3%

  1. Data are the mean ± SEM of at least 4 separate experiments made in duplicate. Emax values are expressed as fluorescence intensity in percent over the basal values for calcium mobilization experiments and as percent of the control twitch for mouse vas deferens experiments. *P < 0.05 versus N/OFQ(1-13)-NH2 according to ANOVA followed by the Dunnett’s test for multiple comparisonsa.The concentration response curve was incomplete due to the low potency of the compound.
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