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. 2022 Nov 3;16:964724. doi: 10.3389/fnins.2022.964724

TABLE 2.

Determination of in vitro agonist biases of nalfurafine [Reproduced from (Zhou et al., 2022)].

References G protein signaling;
cells used		 β-arrestin signaling;
cells used		 Agonist bias
(Reference compound)
Schattauer et al. (2017) ERK1/2 phosphorylation;
HEK293 cells stably expressing rat KOR-GFP		 P38 MAPK phosphorylation;
HEK293 cells stably expressing rat KOR-GFP		 G protein-biased, 7.2
(U50,488H)
Schattauer et al. (2017) ERK1/2 phosphorylation;
HEK293 cells stably expressing FLAG-human KOR		 P38 MAPK phosphorylation;
HEK293 cells stably
expressing FLAG-human KOR		 G protein-biased, 300
(U50,488H)
Liu et al. (2019) [35S]GTPγS binding;
neuro2A cells stably expressing mouse KOR		 γ-galactosidase fragment complementation;
HEK cells stably expressing mouse KOR-donor and β-arrestin1 or 2-acceptor		 Unbiased
(U50,488H)
Dunn et al. (2019) [35S]GTPγS binding;
human KOR-expressing U2OS cells (PathHunter, DiscoveRx)		 γ-galactosidase fragment complementation;
human KOR-expressing U2OS cells (PathHunter, DiscoveRx)		 β-arrestin-biased
(U69,593)
Kaski et al. (2019) GloSensor (cAMP);
HEK293T cells transiently transfected with 3 × HA-hKOR and pGloSensor-22F cAMP biosensor		 Tango luciferase-based assay;
HTLA cells transiently transfected with human KOR-V2-TEV-tTA		 G protein-biased, 7.7
(U50,488)
Cao et al. (2020) GloSensor (cAMP);
HEK293-T cells stably expressing human KOR were transfected with GloSensor for cAMP		 Tango β-arrestin2 recruitment;
HEK293 cells stably expressing a tTA-dependent luciferase reporter and a β-arrestin2-TEV fusion gene were transfected with the human KOR		 G protein-biased, 2.85
(U50,488H)