Table 3.
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.