Table 2 Antagonist potencies (pA2) determined by Schild analysis in functional assays measuring inhibition of agonist-induced [35S]GTPγS binding at the four opioid receptors.

From: Probing ligand recognition of the opioid pan antagonist AT-076 at nociceptin, kappa, mu, and delta opioid receptors through structure-activity relationships

Antagonist Potency (pA2 ± SEM)

 

NOP

KOP

MOP

DOP

1 (AT-076)

7.52

8.366

9.24

7.57

2

ND*

N/C#

ND

ND

8

ND

9.57 ± 0.18

8.09 ± 0.11

ND

10

6.88 ± 0.63

9.42 ± 0.13

7.81§

ND

12

8.30 ± 0.33

9.8 ± 0.8

9.16 ± 0.52

ND

13

N/C

N/C

ND

ND

14

ND

10.46 ± 0.0002

9.16 ± 0.11

7.3738 ± 0.31

15

ND

9.19 ± 0.16

7.98

ND

16

ND

10.56 ± 0.31

8.32

ND

SB-612111

9.28 ± 0.21

ND

ND

ND

  1. pA2 values are given as mean ± SEM of at least two experiments performed in triplicate on two separate days.
  2. *ND = antagonist potency was not determined for compounds whose binding affinity was >50 nM.
  3. #N/C = compound showed a noncompetitive profile in Schild analysis.
  4. §pA2 value from a single experiment done in triplicate.
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