From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies

Research output: Contribution to journalJournal articleResearchpeer-review

Jonas Nii Nortey Eildal, Jacob Andersen, Anders Skov Kristensen, Anne Marie Jørgensen, Benny Bang-Andersen, Morten Jørgensen, Kristian Strømgaard

Citalopram and talopram are structurally closely related, but they have very distinct pharmacological profiles as selective inhibitors of the serotonin and norepinephrine transporters, respectively. A systematic structure-activity relationship study was performed, in which each of the four positions distinguishing the two compounds were varied. The inhibitory potencies of the resulting 16 compounds were tested at both serotonin and norepinephrine transporters. This showed that particularly two of the four positions are determinants for the biological activity.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Volume51
Issue number10
Pages (from-to)3045-3048
ISSN0022-2623
DOIs
Publication statusPublished - 2008

Bibliographical note

Keywords: Animals; Benzofurans; Blood Platelets; Brain; Cell Line; Citalopram; Humans; Norepinephrine Plasma Membrane Transport Proteins; Propylamines; Rats; Recombinant Proteins; Serotonin Plasma Membrane Transport Proteins; Serotonin Uptake Inhibitors; Structure-Activity Relationship; Synaptosomes

ID: 8378305