Serotonin Transporter Ligand

Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (K_i=198 nM), α2A adrenergic receptor (K_i=180 nM; EC₅₀=440 nM) and 5-HT_2A receptor (EC₅₀=172 nM, E_max=76%). Z8779877149 inhibits 5-HT reuptake and activates G_i and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders.

MADAM exhibits high affinity and selectivity for 5-HTT with a K_i value of 1.6 nM. MADAM has the potential to serve as a PET radiotracer for visualizing the serotonin transporter.

LuAF60097 is a serotonin transporter (SERT) ligand. LuAF60097 binds to the extracellular vestibule (S2 site) of SERT with high affinity and to the central binding site (S1) with lower affinity, triggering conformational changes that exert combined competitive and non-competitive inhibitory effects on serotonin reuptake. LuAF60097 is applicable to research related to depression and anxiety disorders.