Experimental design for kinetic dissociation experiments Binding of [125I]RTI-55 (0.01 nM) to hSERT proceeded for 2 h at 25°C. At this point (time 0), 1 μM RTI-55 was added to conditions 2 and 4. Ten minutes later, test drugs were added to conditions 3 and 4. For the purpose of data analysis, the 100% of control point was ′time 0 min′ for conditions 1 and 2 and ′time 10 min′ for conditions 3 and 4. Each data point is the mean ± S.D. of three experiments. The data were fit to a one- or two-component exponential decay model to calculate the k-1 constant and half-life.


1st Addition (Time 0)

2nd Addition (Time 10 min)
1. Control None None
2. RTI-55 RTI-55 (1 μM) None
3. Test drug None Test drug: TB-1-099 (25 μM) or SoRI-6238 (50 μM)
4. RTI-55 + test drug
RTI-55 (1 μM)
Test drug: TB-1-099 (25 μM) or SoRI-6238 (50 μM)