Flibanserin (BIMT-17; BIMT-17BS) hydrochloride 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 hydrochloride 也能够结合多巴胺 D4 受体，Ki为 4-24 nM。Flibanserin hydrochloride 具有抗抑郁和抗焦虑作用，可用于性欲减退 (HSDD) 的研究。
| 生物活性 | Flibanserin (BIMT-17; BIMT-17BS) hydrochloride is an orally active serotonin5-HT1A receptoragonist and5-HT2A receptorantagonist withKivalues of 1 nM and 49 nM, respectively. Flibanserin hydrochloride binds to dopamine D4 receptors with anKivalue of 4-24 nM. Flibanserin hydrochloride shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research[1]-[5]. |
| IC50& Target | 5-HT1AReceptor 1 nM (Ki) | 5-HT2AReceptor 49 nM (Ki) |
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体外研究
(In Vitro) | Flibanserin hydrochloride (0.01-100 μM; 72 h) can transform into two degradation products DP1 and DP2 with no toxicity potential after oxidative degradation[1].
Cell Viability Assay[1] | Cell Line: | NHSF cell lin | | Concentration: | 0.01, 0.1, 1, 10, 100 μM | | Incubation Time: | 72 hours | | Result: | Resulted cell viability reached to 97.91% (DP1) and 96.73% (DP2) at 0.01 μM.
Showed non-toxic up to 100 μM (IC50>100 μM). |
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体内研究
(In Vivo) | Flibanserin hydrochloride (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[2].
Flibanserin hydrochloride (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[3].
Flibanserin hydrochloride (5, 10, 25, and 50 mg/kg; s.c.; single dose) has anxiolytic effects without locomotor side effects in rat ultrasonic vocalization model[4].
| Animal Model: | Long Evans female rats (225-250 g)[3] | | Dosage: | 15 mg/kg; 45 mg/kg | | Administration: | Oral gavage; twice a day for 22 days | | Result: | Increased the density of activated catecholaminergic neurons in the ventral tegmental area but not in the locus coeruleus.
Increased Fos expression in the medial preoptic area and arcuate nucleus of the hypothalamus, ventral tegmental area, locus coeruleus, and lateral paragigantocellular nucleus with chronic 22-day treatment. |
| Animal Model: | Rat pup ultrasonic vocalization model of anxiety[4] | | Dosage: | 5, 10, 25, and 50 mg/kg | | Administration: | Subcutaneous injection | | Result: | Reduced ultrasonic vocalizations in rat pups.
Showed effective within 30 min and has no severe locomotor side effects at active doses. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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