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Abstract
Multi-target compounds where more than one functional activity is incorporated into
the same molecule may have advantages in treating disease states. Selective serotonin
re-uptake inhibitors (SSRIs)(a) (i.e., (R)- and (S)-norfluoxetine) were chemically
linked to a PDE4 inhibitor via a five carbon bridge. The new dual PDE4 inhibitor/SSRIs
(i.e., (R)-8 and (S)-8) showed moderately potent but highly selective serotonin re-uptake
inhibition (IC(50) values of 173 and 42 nM, respectively) in vitro. The dual PDE4
inhibitor/SSRIs (R)-8 and (S)-8 also inhibited PDE4D2 (i.e., K(i) values of 106 and
253 nM, respectively). Due to the synergistic functional activity, PDE4 inhibitor/SSRIs
may be effective in treating diseases such as depression.