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Wf-516

CAS No. : 310392-94-0

MCE 站：Wf-516

产品活性：Wf-516 是一种 5-HT reuptake 的抑制剂，同时为 5-HT1A 和 5-HT2A 受体拮抗剂，对人体 5-HT1A 和 5-HT2A 受体的 K_i 值分别为 5 nM 和 40 nM，具有抗抑郁作用。

研究领域：Neuronal Signaling  |  GPCR/G Protein

作用靶点：Serotonin Transporter  |  5-HT Receptor

In Vitro: Wf-516 shows high affinity for 5-HT1A receptors in the hippocampus and raphe nucleus of rats with K_i of 8.1 nM and 7.9 nM, respectively.

In Vivo: Wf-516 (0.5 mg/kg, i.v.) does not induce any change in the firing activity of 5-HT neurons, but significantly blocks the inhibitory effect of 8-OHDPAT (a 5-HT autoreceptor agonist) by 70%. A full dose-response relationship between the suppression of DRN firing activity and different doses of LSD shows a significant fourfold shift to the right in the Wf-516 pretreated rats (ED₅₀?=?32.4?±?1.0 μg/kg) as compared to controls (ED₅₀?=?7.5?±?1.2 μg/kg). After intravenous administration of successive doses of 1.25 mg/kg of Wf-516 (up to 10 mg/kg), the effect of microiontophoretically applied 5-HT is prolonged and reaches statistical significance at 7.5 mg/kg. At this dose, the RT₅₀ value is increased by 53% and, by 75% at the highest dose of 10 mg/kg of Wf-516 used. Oral administration of 30 mg/kg Wf-516 to these 5,7-DHT-treated rats induces a significant decrease of BPND in the hippocampus as compared with baseline, but no additional reduction of BPND is observed in the raphe nucleus. Oral ED₅₀ values for Wf-516 in the hippocampus and raphe nucleus are 5.3 mg/kg and 4.2 mg/kg, respectively.

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