Biochem/physiol Actions
Orally active, multimodal serotonergic compound with in vivo psychotropic efficacy by targeting 5-HT-1A/1B/1D/3A/7 and SERT.
Vortioxetine (Lu AA21004) is an orally active, multimodal serotonergic compound with high affinity toward human 5-HT1A (Ki = 15 nM), 5-HT1B (Ki = 33 nM), 5-HT1D (Ki = 54 nM), 5-HT3A (Ki = 3.7 nM), 5-HT7 (Ki = 19 nM), noradrenergic β1 (Ki = 46 nM) receptors, and serotonin (5-HT) transporter (SERT Ki = 1.6 nM). Vortioxetine exhibits in vivo psychotropic efficacy by exerting antagonist activity against 5-HT-1D/3A/7, agonist activity on 5-HT1A, partial agonist activity on 5-HT1B, as well as potent SERT inhibitory activity.