1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Flibanserin hydrochloride

Flibanserin hydrochloride  (Synonyms: 盐酸氟立班丝氨; BIMT-17 hydrochloride; BIMT-17BS hydrochloride)

目录号: HY-A0095A
产品使用指南

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。

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Flibanserin hydrochloride Chemical Structure

Flibanserin hydrochloride Chemical Structure

CAS No. : 147359-76-0

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Flibanserin hydrochloride 的其他形式现货产品:

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MCE 顾客使用本产品发表的 2 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Flibanserin (BIMT-17; BIMT-17BS) hydrochloride is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride binds to dopamine D4 receptors with an Ki value 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-HT1A Receptor

1 nM (Ki)

5-HT2A Receptor

49 nM (Ki)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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).
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

426.86

Formula

C20H22ClF3N4O

CAS 号
中文名称

盐酸氟立班丝氨;盐酸氟立班丝胺;盐酸氟利班丝氨

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.

纯度 & 产品资料
参考文献

Flibanserin hydrochloride 相关分类

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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