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1. Serotonin transporters(SERTs) and serotonin 5-HT1A are occupied after administration of Serotonin Partial Agonist Reuptake Inhibitor(SPARI) .
2. Serotonin level increases initially in the somatodendritic areas of the serotonin neuron due to the blockage of the serotonin transporter (SERTs).
3. After increment of serotonin in the somatodendritic areas of the serotonin neuron, somatodendritic 5-HT1A autoreceptors de-sensitize or down-regulate.
4. As a result of the somatodendritic receptors’ down-regulation, inhibition of impulse flow in the serotonin neuron never exists. Therefore, serotonin is released in the axon terminal when the neuronal impulse flow restarted.
1. Asset type: SSRI & Partial 5-HT1A Agonist
2. Indication: Depression
3. Modality: Small molecular
4. Research phase: Phase II/ III
5. Cooperation demands: License-out or co-development
6. Research progress：
(1) Compared with the benchmark molecule Vilazodone, this asset demonstrated a better clinical PK profile at the same dose level. And based on the BBB data in animals, the concentration of this asset in human CSF will be much higher than that of Vilazodone. Phase I clinical results showed that the incidence of gastrointestinal side effects was lower than that from Vilazodone.
(2) Phase III clinical research is ongoing in China.
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