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. 2023 Nov;104(5):230–238. doi: 10.1124/molpharm.123.000722

TABLE 1.

Efficacy and potency values of indicated 5-HT1AR agonists acting on each Gαi/o/z protein. Each value represents the mean ± S.D. of 5–10 independent replicates

Compound Gα protein Emax ± S.D. pEC50 ± S.D. Compound Gα protein Emax ± S.D. pEC50 ± S.D.
GoA 0.082 ± 0.003 7.20 ± 0.15 GoA 0.048 ± 0.010 4.78 ± 0.18
GoB 0.066 ± 0.015 6.59 ± 0.46 GoB 0.040 ± 0.007 4.82 ± 0.39
5-HT Gi1 0.045 ± 0.002 6.52 ± 0.07 Nuciferine Gi1 0.030 ± 0.003
Gi2 0.060 ± 0.007 6.86 ± 0.09 Gi2 0.013 ± 0.009 4.75 ± 1.15
Gi3 0.042 ± 0.005 6.78 ± 0.06 Gi3 0.014 ± 0.009
Gz 0.061 ± 0.006 6.36 ± 0.06 Gz 0.020 ± 0.002 4.90 ± 0.66
GoA 0.084 ± 0.020 7.33 ± 0.20 GoA 0.036 ± 0.006 5.17 ± 0.20
GoB 0.070 ± 0.008 7.14 ± 0.06 GoB 0.042 ± 0.006 4.72 ± 0.18
8-OH-DPAT Gi1 0.032 ± 0.002 6.68 ± 0.18 Sumatriptan Gi1 0.021 ± 0.004
Gi2 0.054 ± 0.016 7.05 ± 0.18 Gi2 0.018 ± 0.005 4.92 ± 0.63
Gi3 0.032 ± 0.003 6.77 ± 0.12 Gi3 0.013 ± 0.007
Gz 0.053 ± 0.015 6.70 ± 0.19 Gz 0.036 ± 0.004 4.81 ± 0.08
GoA 0.050 ± 0.006 6.57 ± 0.10 GoA 0.106 ± 0.019 7.88 ± 0.15
GoB 0.025 ± 0.004 6.97 ± 0.09 GoB 0.071 ± 0.010 8.13 ± 0.14
Buspirone Gi1 0.011 ± 0.003 7.20 ± 0.20 Vilazodone Gi1 0.043 ± 0.004 6.97 ± 0.08
Gi2 0.017 ± 0.005 7.33 ± 0.19 Gi2 0.045 ± 0.004 5.75 ± 0.12
Gi3 0.012 ± 0.007 6.66 ± 0.87 Gi3 0.039 ± 0.006 7.34 ± 0.19
Gz 0.024 ± 0.006 6.85 ± 0.18 Gz 0.061 ± 0.005 5.81 ± 0.13
GoA 0.032 ± 0.009 5.88 ± 0.21 GoA 0.053 ± 0.018 4.94 ± 0.18
GoB 0.020 ± 0.005 5.76 ± 0.28 GoB 0.050 ± 0.010 5.02 ± 0.22
Aripiprazole Gi1 Vortioxetine Gi1 0.049 ± 0.009 4.86 ± 0.14
Gi2 0.011 ± 0.003 4.03 ± 0.82 Gi2 0.037 ± 0.008 4.98 ± 0.30
Gi3 0.013 ± 0.001 Gi3 0.031 ± 0.013 5.08 ± 1.02
Gz 0.020 ± 0.002 Gz 0.048 ± 0.009 5.14 ± 0.20
GoA 0.078 ± 0.019 6.77 ± 0.14 GoA 0.077 ± 0.014 6.27 ± 0.11
GoB 0.097 ± 0.008 6.93 ± 0.12 GoB 0.081 ± 0.017 7.77 ± 0.21
Flibanserin Gi1 0.061 ± 0.003 5.96 ± 0.38 F-15599 Gi1 0.060 ± 0.008 7.24 ± 0.14
Gi2 0.054 ± 0.013 6.13 ± 0.23 Gi2 0.066 ± 0.003 5.71 ± 0.10
Gi3 0.059 ± 0.010 6.08 ± 0.19 Gi3 0.056 ± 0.002 7.76 ± 0.11
Gz 0.070 ± 0.008 5.91 ± 0.32 Gz 0.060 ± 0.004 5.67 ± 0.13