Sections
History and Discovery | Structure–Activity Relations | Pharmacological Profile | Pharmacokinetics and Distribution | Mechanism of Action | Indications and Efficacy | Side Effects and Toxicology | Drug–Drug Interactions | Conclusion | References
Excerpt
Research has implicated dysregulation of serotonin (5-HT)
in mood and anxiety disorders. Despite the effectiveness of the
monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants
(TCAs), which exert their effects by inhibiting the enzymatic degradation
and reuptake of monoamines, respectively, side effects and potential
serious adverse events limited their utility. Researchers thus identified
compounds that are selective in blocking neurotransmitter reuptake
and yet have little agonist and antagonist activity at receptors
thought to be associated with adverse effects. Sertraline [(+)-cis-(1S,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthylamine],
a naphthylamino compound that is structurally different from MAOIs
and TCAs (Figure 14–1), is one of this class of drugs (Guthrie 1991; Heym and Koe 1988).