A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties FASEB J. Maillet et al.
21: 2124
Supplemental Data
Files in this Data Supplement:
Supplemental Figure 1
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(06-7683SuppFigure1.TIF; 811 KB) The effects of LPI805 on binding and dissociation kinetics are reversible. Reversal of LPI805 effects was obtained by washing the cells. 20 nM NKAbo was incubated for 30 min with or without 20 μM LPI805. Cells were then washed twice for 10 min with a 20 nM NKAbo solution containing either 20 μM LPI805 or no LPI805. The percentage of FRET and the proportion of the fast dissociation component A1 were then determined (mean ± SE of 2 independent experiments).
