Table 3 Effects of Ro 65-6570 and its dimeric derivatives in calcium mobilization studies performed on CHO cells coexpressing the NOP receptor and the Gαqi5 chimeric protein.

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

compound

n

Spacer length

pEC50(CL95%)

Emax ± SEM

Ro 65-6570

—

—

8.21 (8.01 – 8.40)

165 ± 14

19

1

18

7.57 (7.23–7.91)

131 ± 12

20

2

19

7.45* (7.18–7.73)

125 ± 6

21

3

20

7.29* (7.00–7.58)

135 ± 20

22

4

21

7.14* (6.71–7.58)

143 ± 18

23

5

22

6.99* (6.91–7.08)

132 ± 14

24

6

23

6.85* (5.81–7.89)

150 ± 35

25

7

24

7.14* (6.30–7.99)

131 ± 21

26

—

—

8.24 (7.84–8.65)

143 ± 9

  1. Data are the mean ± SEM of at least 4 separate experiments made in duplicate. Emax values are expressed as percent fluorescence intensity over the basal values. *P < 0.05 versus N/OFQ(1-13)-NH2 according to ANOVA followed by the Dunnett’s test for multiple comparisons.
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