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. Author manuscript; available in PMC: 2018 Oct 1.
Published in final edited form as: Biochim Biophys Acta. 2017 Apr 19;1863(10 Pt A):2486–2495. doi: 10.1016/j.bbadis.2017.04.010

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]