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G蛋白偶联受体/G蛋白
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/ 5-羟色胺受体 / Flibanserin/氟立班丝氨

Flibanserin/氟立班丝氨 {[allProObj[0].p_purity_real_show]}

货号：A101358 同义名： 氟班色林 / BIMT-17; BIMT-17BS

Flibanserin is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. It is also a P-Glycoprotein Inhibitor.

Flibanserin/氟立班丝氨 化学结构 CAS号：167933-07-5
Flibanserin/氟立班丝氨 化学结构
CAS号：167933-07-5
Flibanserin/氟立班丝氨 3D分子结构
CAS号：167933-07-5
Flibanserin/氟立班丝氨 化学结构 CAS号：167933-07-5
Flibanserin/氟立班丝氨 3D分子结构 CAS号：167933-07-5
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Flibanserin/氟立班丝氨 纯度/质量文件 产品仅供科研

货号：A101358 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		98%
Venlafaxine ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

 		98%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

 		98%
Tropisetron ✔ 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron HCl dihydrate ✔ 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

 		++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Flibanserin/氟立班丝氨 生物活性

靶点

  • 5-HT2

    5-HT2A, Ki:49 nM

  • 5-HT1

    5-HT1A, Ki:1 nM
描述 Flibanserin, also named as BIMT 17, is a kind of 5-HT2A receptor antagonist and 5-HT1A receptor full agonist. In vitro studies, it was found that flibanserin showed a good affinity for 5-HT1A and 5-HT2A receptors with the pKi of 7.72 and 6.90 respectively in cerebral cortical, while no appreciable affinity for the other 5-HT receptor subtypes. Besides this, flibanserin could also reduce the forskolin-stimulated cAMP accumulation in the cerebral cortex and in the hippocampus, as well as inhibit the 5-HT-induced phosphatidylinositol turnover in the cerebral cortex[3]. In vivo studies, flibanserin could act as a full agonist in the dorsal raphe nucleus (DRN) and the medial prefrontal cortex (mPFC), but as a partial agonist in the CA3 region of the hippocampus in the rat brain, when applied by the local microiontophoretic[4]. In addition, systemic administration of flibanserin could contribute to the change of some monoamine’s level in rat brain, such as neurotransmitters serotonin (5-HT), norepinephrine (NE) and so on[5].

Flibanserin/氟立班丝氨 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00360555 Sexual Dysfunctions, Psycholog... 展开 >>ical 收起 << Phase 3 Completed - -
NCT00491829 Sexual Dysfunctions, Psycholog... 展开 >>ical 收起 << Phase 3 Completed - -
NCT00360555 - Completed - -

Flibanserin/氟立班丝氨 参考文献

[1]Gao Z, Yang D, et al. Efficacy and Safety of Flibanserin in Women with Hypoactive Sexual Desire Disorder: A Systematic Review and Meta-Analysis. J Sex Med. 2015 Nov;12(11):2095-104.

[2]Simon JA, Kingsberg SA, et al. Efficacy and safety of flibanserin in postmenopausal women with hypoactive sexual desire disorder: results of the SNOWDROP trial. Menopause. 2014 Jun;21(6):633-40.

[3]Borsini F, Giraldo E, Monferini E, Antonini G, Parenti M, Bietti G, Donetti A. BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex. Naunyn Schmiedebergs Arch Pharmacol. 1995 Sep;352(3):276-82. doi: 10.1007/BF00168557. PMID: 8584042.

[4]Rueter LE, de Montigny C, Blier P. In vivo electrophysiological assessment of the agonistic properties of flibanserin at pre- and postsynaptic 5-HT1A receptors in the rat brain. Synapse. 1998 Aug;29(4):392-405. doi: 10.1002/(SICI)1098-2396(199808)29:4<392::AID-SYN11>3.0.CO;2-T. PMID: 9661257.

[5]Allers KA, Dremencov E, Ceci A, Flik G, Ferger B, Cremers TI, Ittrich C, Sommer B. Acute and repeated flibanserin administration in female rats modulates monoamines differentially across brain areas: a microdialysis study. J Sex Med. 2010 May;7(5):1757-67. doi: 10.1111/j.1743-6109.2010.01763.x. Epub 2010 Feb 12. PMID: 20163532.

Flibanserin/氟立班丝氨 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.81mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL

Flibanserin/氟立班丝氨 技术信息

CAS号167933-07-5
分子式C20H21F3N4O
分子量 390.4
SMILES Code O=C1N(C2=C(N1)C=CC=C2)CCN3CCN(C4=CC(C(F)(F)F)=CC=C4)CC3
MDL No. MFCD00918402
别名 氟班色林 ;BIMT-17; BIMT-17BS; EBD6396
运输蓝冰
InChI Key PPRRDFIXUUSXRA-UHFFFAOYSA-N
Pubchem ID 6918248
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 50 mg/mL(128.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Flibanserin | 167933-07-5 | BIMT-17 | BIMT-17BS | BIMT17 | BIMT 17 | Serotonin Modulator | GPCR/G Protein | Neuronal Signaling | 5-HT Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Flibanserin/氟立班丝氨 纯度/质量文件 | Flibanserin/氟立班丝氨 亚型比较 | Flibanserin/氟立班丝氨 生物活性 | Flibanserin/氟立班丝氨 临床数据 | Flibanserin/氟立班丝氨 参考文献 | Flibanserin/氟立班丝氨 实验方案 | Flibanserin/氟立班丝氨 技术信息

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