Structureactivity Relations

Drugs that inhibit 5-HT reuptake vary in their selectivity (Table 13-1). Despite the tendency to lump the contemporary SSRIs into the same class designation, significant structural and activity differences exist. Their chemical structures help illustrate this diversity (Figures 13-2 and 13-3). In contrast to paroxetine and sertraline, which exist as single isomers, fluoxetine, like citalopram, is a racemate. The family of SSRIs manifests diverse structural and activity relations. Such data are in vitro and thus subject to methodological variability (Thomas et al. 1987). Fluoxetine is less potent than paroxetine in vitro and less selective for 5-HT reuptake inhibition, relative to norepinephrine (NE), than citalopram. However, note that in vitro potency does not necessarily equate with in vivo dosing experience, clinical efficacy, or adverse-event profile.

TABLE 13-1. Inhibition of [3H]monoamine uptake into rat brain synaptosomes in vitro
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