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Vilazodone

CAS No. : 163521-12-8

MCE 站：Vilazodone

产品活性：Vilazodone (EMD 68843;SB 659746A) 是一种有效的，具有口服活性的，选择性 5 -羟色胺再摄取抑制剂 (SSRI) 和部分 5-HT₁A 受体激动剂。Vilazodone 在动物体内表现出抗抑郁作用，可用于抑郁症 (MDD) 和情绪性疾病的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor  |  Serotonin Transporter

In Vitro: Vilazodone shows an IC₅₀ of 0.2 nM at the human 5-HT₁A receptor and 0.5 nM for the SERT. Vilazodone preferentially binds to the high agonist affinity state of human 5-HT₁A?receptors, and it displays high affinity (pK_i≥9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT_1A?receptors.
Vilazodone acts as a high efficacy partial agonist at 5-HT₁A?receptors. In [³⁵S]GTPγS binding studies in Sf9 cells expressing h5-HT₁A?receptors, a single concentration of Vilazodone (100nM) increases basal binding by approximately 70% of that produced by the full 5-HT₁A?receptor agonist, 8‐OH‐PIPAT.
In [³⁵S]GTPγS binding studies in rat hippocampal membranes, Vilazodone acts as a potent 5‐HT_1A?receptor partial agonist with a pEC₅₀?of 8.1 and an intrinsic activity of 0.61.
Vilazodone acts as a potent 5‐HT reuptake inhibitor in rat and guinea pig cortex. In LLCPK cells expressing human SERT, whereby vilazodone inhibits [³H]5‐HT uptake with a pIC₅₀?of 8.8.

In Vivo: Vilazodone (intraperitoneal injection; 3 mg/kg ; single dose) produces increases in extracellular levels of 5‐HT in both the frontal cortex (FC) and ventral hippocampus (vHipp) of rats in vivo?microdialysis studies. Maximum increases are observed at 3 mg/kg and reaches 527% and 558% of preinjection baseline values in the FC and vHipp, respectively.
Vilazodone (oral gavage ;55 mg/kg ; single dose) inhibits stress‐induced vocalizations in the rat ultrasonic vocalizations test at 120 and 210 min post dose.

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