Table 2.
Opioid receptor efficacy of 8aa
| Compound | EC50 (nM) | % stimulation | ||||
|---|---|---|---|---|---|---|
| MOR-1 | KOR-1 | DOR-1 | MOR-1 | KOR-1 | DOR-1 | |
| 8a | 1.38 ± 0.8 | 36.5 ± 19.2 | 9.1 ± 3.0 | 95.3 ± 0.8 | 106.3 ± 8.5 | 101.7 ± 2.8 |
| DPDPE | ndb | ndb | 2.05 ± 0.6 | |||
| DAMGO | 5.6 ± 3 | ndb | ndb | |||
| U50,488H | ndb | 21.7 ± 4.6 | ndb | |||
a
Efficacy data were obtained using agonist induced stimulation of [35S]GTPγS binding assay. Efficacy is represented as EC50 (nM) and percent maximal stimulation relative to standard agonist DAMGO (MOR-1), DPDPE (DOR-1), or U50,488H (KOR-1) at 100 nM. All values are expressed as the mean ± SEM of three separate assays performed in triplicate.
b
Not determined