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. 2020 Jun 2;15(13):1175–1186. doi: 10.1002/cmdc.202000180

Table 1.

Binding affinities of known ligands derived from diprenorphine (2).

graphic file with name CMDC-15-1175-g007.jpg

compound

R1=

K i [nM]

μ

κ

δ

2 33

H

0.14

2.0

0.73

4 37

H

2.19±0.65

4.15±1.3

3.66±0.92

5 34

H

0.7±0.25

2.6±0.0

0.7±0.05

6 38

Me

14.4

0.15

89.3

7 38

Me

1.91

25.8

1753

8 38

Me

1.87

0.74