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 |