Table 2.
Affinity of the synthesized compounds for opioid and neurokinin receptors.
| IC50 ± SEM 1 (nM) | |||
|---|---|---|---|
| Compound | MOR | DOR | NK1R |
|
YaGF-
(enkephalin-derivative) | |||
| 1a [33] | 12.73 ± 0.75 | 74.20 ± 0.40 | 4.24 µM ± 0.80 |
| 1b | 110.64 ± 12.66 | 413.45 ± 105.15 | >1000 |
| 1c | 5.25 ± 1.14 | 161.65 ± 8.75 | >1000 |
| 1d | 4.73 ± 0.02 | 44.04 ± 2.75 | >1000 |
|
YaGW-
(enkephalin-derivative) | |||
| 2a | 112.01 ± 16.89 | 914.4 ± 43.50 | >1000 |
| 2b | 93.465 ± 32.84 | 467.05 ± 36.95 | >1000 |
|
YaFF-
(TAPP) | |||
| 3a | 90.4 ± 9.91 | >1000 | 722.8 ± 58.2 |
| 3b | 391.05 ± 57.85 | >1000 | >1000 |
| YaW- | |||
| 4a | 118.11 ± 40.19 | 621.0 ± 65.20 | >1000 |
| 4b | >1000 | >1000 | >1000 |
|
YPFF-
(endomorphin-2) | |||
| 5a | 28.5 ± 9.41 | >1000 | >1000 |
|
YPF-
(truncated endomorphin-2) | |||
| 6a | 113.1 ± 7.00 | >1000 | >1000 |
1 IC50 values represent means ± SEM of at least two experiments performed in duplicates.