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. 2013 Dec 5;1(2):e00013. doi: 10.1002/prp2.13

Figure 6.

Figure 6

Concentration–response curves for the inhibition of 5-HT7 binding sites by MEL-9 and LP-211 in preincubation/washout experiments in radioligand binding studies in whole HEK-hu5-HT7 cells. Cells were preincubated in the absence (control) or presence of either MEL-9 or LP-211 at increasing concentrations (ranging from 100 pmol/L to 10 μmol/L), 10 μmol/L clozapine (Δ) as reference competitive antagonist, or 1 μmol/L methiothepin (▲) as reference irreversible antagonist, for 30 min. After a compound washout procedure (see Materials and Methods), the cells were subjected to whole-cell radioligand binding assays to determine specific [3H]-SB-269970 binding. [3H]-SB-269970 specific binding is expressed in each case as percent of [3H]-SB-269970 specific binding in cells preincubated in the absence of compound (control). The total radioactivity bound was less than 20% of total radioactivity added in all the experiments. Data are the mean values ± SEM from three to five independent experiments performed in duplicate. Concentration–response data were fitted to a sigmoidal dose–response curve (nH = 1).