Table 2 Potency and efficacy (β-arrestin recruitment) of I8-arachnotocin at human receptors.
From: I8-arachnotocin–an arthropod-derived G protein-biased ligand of the human vasopressin V2 receptor
I8-arachnotocin | OT/VP& | |||||
|---|---|---|---|---|---|---|
EC50 | pEC50 | Emax# | EC50 | pEC50 | Emax# | |
V2Rβ-arr1 | n.d. | 56 nM | −7.25 ± 0.07 | 100% | ||
V2Rβ-arr2 | n.d. | 60 nM | −7.22 ± 0.07 | 100% | ||
V1bR | 1.2 µM | −5.92 ± 0.14 | 65 ± 5% | 6.9 nM | −8.16 ± 0.09 | 100% |
V1aR | n.d. | 28 nM | −7.55 ± 0.12 | 100% | ||
OTR | 5.7 µM | −5.24 ± 0.26 | 32 ± 5% | 170 nM | −6.77 ± 0.15 | 100% |
