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. 2023 Oct 19;66(21):14853–14865. doi: 10.1021/acs.jmedchem.3c01415

Table 2. OTR, V1aR, and V1bR Potencies (EC50) and Efficacies (Emax) of OT and VP and 814a.

  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              
a

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)].