Figure 4. Reactivation of risperidone-inactivated h5-HT₇ receptors.

Four inactivating antagonists and six non-inactivating antagonists (competitive antagonists) were tested for their ability to reverse risperidone inactivation of the h5-HT₇ receptor. Cells were exposed to risperidone, thoroughly washed, then exposed to 1 μM of the various drugs for 90 min. After removal of drugs, receptor activity was tested with 10 μM 5-HT. The four inactivators (risperidone, 9-OH-risperidone, methiothepin, and bromocriptine) as well as ICI169369 did not reactivate the receptor; all other drugs reactivated the receptor as defined by sensitivity to 10 μM 5-HT. ICI169369 proved to be a low potency reactivator due to its relatively low affinity for the h5-HT₇ receptor (Teitler et al., 2010) (Figure 5). These results are from (Teitler et al., 2010) and are the mean±S.E.M. of three experiments performed in triplicate (*p<0.001 vs. control, one-way ANOVA with Dunnett's post-test).