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Flibanserin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Flibanserin图片
CAS NO:167933-07-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Flibanserin (BIMT-17; BIMT-17BS) 是一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂,Ki 值分别为 1 nM 和 49 nM。
Cas No.167933-07-5
别名氟立班丝氨; BIMT-17; BIMT-17BS
化学名1,3-dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-2H-benzimidazol-2-one
Canonical SMILESO=C1N(CCN2CCN(C3=CC(C(F)(F)F)=CC=C3)CC2)C4=CC=CC=C4N1
分子式C20H21F3N4O
分子量390.4
溶解度≤15mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Flibanserin is a full agonist of the serotonin 5-HT1A receptor and an antagonist of 5-HT2A.

Atypical antipsychotic drugs, all of which are relatively more potent as serotonin (5-HT)(2A) than dopamine D(2) antagonists, improve negative symptoms and cognitive dysfunction in schizophrenia partiallly by increasing cortical dopamine release. 5-HT(1A) agonism is also reported to contribute to the ability to increase cortical dopamine release.

In vitro: Previous study found that flibanserin was a 5-HT(1A) agonist, a very weak partial agonist on dopamine D(4) receptors, and a 5-HT(2A) antagonist. Flibanserin could reduce neuronal firing rate and flibanserin-induced reduction in firing rate was likely mediated via stimulation of postsynaptic 5-HT(1A) receptors. Moreover, flibanserin could quickly desensitize somatic 5-HT autoreceptors and enhance tonic activation of postsynaptic 5-HT(1A) receptors. In addition, flibanserin was able to reduce synthesis and extracellular levels of 5-HT in the cortex [1].

In vivo: Previous animal study showd that flibanserin had antidepressant-like activity in most animal models sensitive to antidepressants, and such activity seemed different from that exerted by other antidepressants. In addition, flibanserin did not show consistent effects in animal models of anxiety and seemed to exert potential antipsychotic effects [1].

Clinical trial: In premenopausal women with HSDD, flibanserin showed significant improvements in the number of SSE and sexual desire. Flibanserin treatment also led to significant reductions in distress associated with sexual dysfunction and distress associated with low sexual desire [2].

References:
[1] Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S.  Pharmacology of flibanserin. CNS Drug Rev. 2002 Summer;8(2):117-42.
[2] Katz M et al.  Efficacy of flibanserin in women with hypoactive sexual desire disorder: results from the BEGONIA trial. J Sex Med. 2013 Jul;10(7):1807-15.