Table 1. Biased ligands of neural MCRs.
Biased ligand | Receptor | Pathway | Cell system | Reference |
---|---|---|---|---|
AgRP | MC4R | Inhibiting Gs Activating Gi, Kir7.1, ERK1/2, and Akt |
GT1-7 (Gi, Akt) PVH neurons (Kir7.1) HEK293T (ERK1/2) |
[47, 50, 54, 56] |
MC3R | Inhibiting Gs Activating ERK1/2 |
HEK293T | [56] | |
MCL0020 ML00253764 Ipsen 5i |
MC4R | Inhibiting Gs Activating ERK1/2 |
HEK293T | [50] |
AP1189 | MC3R | Not increasing Gs Activating ERK1/2 and calcium mobilization |
HEK293A | [55] |
THIQ NBI55886 NBI56453 NBI58702 NBI58704 |
MC4R | Activating Gs Impaired in calcium mobilization and receptor internalization |
HEK293 | [45] |