Table 1 Potency and efficacy (G protein-mediated) of I8-arachnotocin at human receptors.
From: I8-arachnotocin–an arthropod-derived G protein-biased ligand of the human vasopressin V2 receptor
I8-arachnotocin | VP/OT& | |||||
|---|---|---|---|---|---|---|
EC50 | pEC50 | Emax# | EC50 | pEC50 | Emax# | |
V2R | 34 nM | −7.47 ± 0.09 | 99 ± 3% | 6.7 pM | −11.17 ± 0.10 | 100% |
V1bR | 1.2 µM | −5.93 ± 0.15 | 104 ± 8% | 1.6 nM | −8.80 ± 0.09 | 100% |
V1aR | antagonist pA2 of 6.253 (~558 nM) | 0.56 nM | −9.25 ± 0.07 | 100% | ||
OTR | 790 nM | −6.11 ± 0.20 | 62 ± 6% | 12 nM | −7.91 ± 0.09 | 100% |
