Table 1.
Affinities of racemic and enantiomerically pure perhydroquinolines and reference compounds for KOR and related receptors.
|
| ||||||
|---|---|---|---|---|---|---|
|
Compd. |
Configuration |
K i±SEM [nM] [a,b] |
||||
|
KOR |
MOR |
DOR |
σ1 |
σ2 |
||
|
[3H]U‐69,593 |
[3H]DAMGO |
[3H]DPDPE |
[3H](+)‐pentazocine |
[3H]DTG |
||
|
(±)‐2 12 |
racemate |
5.6±0.6 |
573 |
413 |
2 % |
0 % |
|
3 19 |
|
0.25±0.08 |
43±9.2 |
58±8.4 |
0 % |
8 % |
|
(±)‐4 |
racemate |
1.2±0.6 |
1200 |
1400 |
0 % |
0 % |
|
4 |
4aR,8S,8aS |
0.81±0.32 |
0 % |
0 % |
676 |
3300 |
|
ent ‐4 |
4aS,8R,8aR |
195±67 |
0 % |
0 % |
0 % |
12 % |
|
U‐50,488 |
1S,2S |
0.34±0.07 |
– |
– |
– |
– |
|
naloxone |
|
7.3±0.40 |
2.3±1.1 |
103 |
– |
– |
|
morphine |
|
– |
5.2±1.6 |
– |
– |
– |
|
SNC80 |
|
– |
– |
1.2±0.5 |
– |
– |
|
(+)‐pentazocine |
|
– |
– |
– |
5.4±0.5 |
– |
|
haloperidol |
|
– |
– |
– |
6.6±0.9 |
78±2.3 |
[a] A value in % reflects the inhibition of the radioligand binding at a test compound concentration of 1 μM. K i values without SEM values represent the mean of two experiments (n=2) and K i values with SEM values represent the mean of three experiments (n=3). [b] Guinea pig brain membrane preparations were used in the KOR, MOR and σ1 assay. In the DOR assay rat brain and in the σ2 assay rat liver membrane preparations were used.