Lu AF60097 / Lundbeck, University of Copenhagen, National Institutes of Health - LARVOL DELTA

[VIRTUAL] Towards discovering higher-affinity allosteric inhibitors of the serotonin transporter for practical therapeutic interventions on depression (ACS-Fall 2021) - "SERT is the primary target for several antidepressants, e.g., S-citalopram and imipramine, to alleviate depression symptoms. The SERT inhibition by Lu AF60097 is demonstrated by the potentiated imipramine binding and increased rat hippocampal serotonin level. These understandings of the S1-S2 coupling mechanism facilitate the rational design and discovery of even higher-affinity SERT allosteric inhibitors, which will lead towards practical therapeutic interventions on depression with allosteric modulations."

CNS Disorders • Depression • Mood Disorders • Psychiatry

The mechanism of a high-affinity allosteric inhibitor of the serotonin transporter. (PubMed, Nat Commun) - "SERT activity is modulated by antidepressants, e.g., S-citalopram and imipramine, to alleviate symptoms of depression and anxiety. The SERT inhibition by Lu AF60097 is demonstrated by the potentiated imipramine binding and increased hippocampal serotonin level in rats. Together, we reveal a S1-S2 coupling mechanism that will facilitate rational design of high-affinity SERT allosteric inhibitors."

Journal • CNS Disorders • Depression • Mood Disorders

New drug can ease the side effects of medication against severe depression (Eurekalert) - "Researchers from the Faculty of Health and Medical Sciences at the University of Copenhagen, in collaboration with Lundbeck A/S and the National Institutes of Health in Baltimore, have discovered a substance....'We have discovered a substance, Lu AF60097, that works in a different way....If the new substance works, it may help the existing drugs get rid of the serious side effects'."

New molecule