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CAS No. : 167933-07-5
MCE 国际站:Flibanserin
产品活性:Flibanserin (BIMT-17; BIMT-17BS) 是一种具有口服活性的 5- 羟色胺的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂,结合亲和力 Ki 分别为 1 nM 和 49 nM。Flibanserin 也能够结合多巴胺 D4 受体,Ki 为 4-24 nM。Flibanserin 具有抗抑郁和抗焦虑作用,可用于性欲减退 (HSDD) 的研究。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:5-HT Receptor
In Vitro: Flibanserin (0.01-100 μM; 72 h) can transform into two degradation products DP1 and DP2 with no toxicity potential after oxidative degradation.
In Vivo: Flibanserin (1, 10, 30 mg/kg; i.p.; single dose) shows different pharmacological properties in prefrontal cortex, hippocampus and midbrain. The 5-HT1A receptor occupancy in cortex indicates it’s the more sensitive than other brain region.
Flibanserin (15, 45 mg/kg; p.o.; twice a day; 22 d) preferentially activates the brain regions belonging to the mesolimbic dopaminergic pathway and hypothalamic structures involved in the integration of sexual cues related to sexual motivation.
Flibanserin (5, 10, 25, and 50 mg/kg; s.c.; single dose) has anxiolytic effects without locomotor side effects in rat ultrasonic vocalization model.
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