Table 2. OTR, V1aR, and V1bR Potencies (EC50) and Efficacies (Emax) of OT and VP and 8–14a.
| OTR |
V1aR |
V1bR |
||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| EC50 ± SEM [nM] | Emax ± SEM [%] | E/Z ratio EC50 | EC50 ± SEM [nM] | Emax ± SEM [%] | E/Z ratio EC50 | EC50 ± SEM [nM] | Emax ± SEM [%] | E/Z ratio EC50 | ||
| OT | 2.46 ± 0.58 | 100 | VP | 0.64 ± 0.09 | 100 | 3.33 ± 0.48 | 100 | |||
| E-8 | 4501 ± 1014 | 45 ± 3 | 1.3 | E-12 | 722 ± 53 | 104 ± 1 | 2.0 | 107 ± 13 | 95 ± 1 | 5.3 |
| Z-8 | 3496 ± 1887 | 35 ± 1 | Z-12 | 1439 ± 108 | 99 ± 1 | 20.2 ± 6 | 95 ± 1 | |||
| E-9 | 346 ± 30 | 89 ± 1 | 2.5 | E-13 | >10 μM | 11,260 ± 1829 | 45 ± 3 | 1.6 | ||
| Z-9 | 136 ± 6 | 90 ± 1 | Z-13 | >10 μM | 7228 ± 1575 | 52 ± 5 | ||||
| E-10 | 94.6 ± 19 | 80 ± 1 | 3.1 | E-14 | >10 μM | 4967 ± 754 | 48 ± 2 | 2.1 | ||
| Z-10 | 30.7 ± 4 | 92 ± 0 | Z-14 | >10 μM | 2373 ± 607 | 67 ± 2 | ||||
| E-11 | 263 ± 21 | 75 ± 1 | 2.0 | |||||||
| Z-11 | 134 ± 17 | 86 ± 1 | ||||||||
Determined in an IP-One accumulation assay performed with stable HEK293 cell lines expressing hOTR, hV1aR, and hV1bR. Efficacies were determined relative to the effect of OT (OTR) and VP (VPRs). Data represent mean values from at least three independent experiments performed in triplicate [standard error of the mean (SEM)].