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. 2019 May 16;24(10):1892. doi: 10.3390/molecules24101892

Table 3.

Dynamic cAMP stimulation upon ligand incubation, washout, and α-MSH re-challenge, showing persistent signaling by certain MC4R ligands (adapted from Molden et al. [34]).

MC4R Ligands and Incubation Concentration Dynamic cAMP Response Comment
Time = 0 min Time = 10–20 min Time = 20–50 min Time = 55–60 min
Initial (time 0–10 min) Ligand challenge at 10 min Ligand washed out after 10 min incubation and measured cAMP 20–30 min post washing cAMP following 500 nM α-MSH re-challenge at 55 min
α-MSH, 200 nM ++++ ++++ Full reversal of signal upon washing out
LY2112688, 100 nM ++++ ++++ Full reversal of signal upon washing out
THIQ, 1 µM ++++ ++ ++++ Partial reversal upon washout
MT-II, 200 nM ++++ ++++ ++++ No reversal upon washout
RM-511, 100 nM ++++ ++++ ++++ No reversal upon washout

− represents a zero or basal level response, or response without any ligand exposure; ++ represents about half the maximal cAMP stimulation response; ++++ represents a 100% cAMP stimulation response.