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What is Flibanserin?

Feb 20，2020

Flibanserin is an N-alkylpiperazine that is 1-[2-(1,3-dihydro-2-oxobenzimidazol-1-yl)ethyl]piperazine in which the remaining amino proton is replaced by a 3-(trifluoromethyl)phenyl group. A multifunctional serotonin agonist and antagonist which is used for the treatment of pre-menopausal women with hypoactive sexual desire disorder. Flibanserin has a role as a serotonergic agonist, a serotonergic antagonist and an antidepressant. Flibanserin is a member of benzimidazoles, a N-arylpiperazine, a N-alkylpiperazine and an organofluorine compound.

Flibanserin is a novel multifunctional serotonin agonist and antagonist (MSAA) that improves sexual functioning in premenopausal women who suffer from reduced sexual interest and desire. IC50 value: Target: serotonin in vivo: The multifunctional serotonergic agent Flibanserin is both a serotonin 1A agonist and a serotonin 2A antagonist. Flibanserin theoretically improves sexual functioning by enhancing downstream release of dopamine and norepinephrine while reducing serotonin release in the brain circuits that mediate symptoms of reduced sexual interest and desire. Flibanserin, a new molecular entity for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. Flibanserin improves interest in and desire for sex by hypothetically targeting these circuits and causing the release of dopamine and norepinephrine while also reducing the release of serotonin. Flibanserin has demonstrated clinical efficacy in premenopausal women who have reduced interest in and desire for sex and has 2 principal pharmacologic actions in microcircuits: it is a full agonist at postsynaptic serotonin 5HT1A receptors and an antagonist at postsynaptic 5HT2A receptors[1-3].

Fig 1. Chemical structure formula and three-dimensional structure of Flibanserin

Flibanserin is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment, but has not been linked to instances of clinically apparent acute liver injury.

Flubanserin is a 5-HT1A receptor agonist and a 5-HT2A receptor antagonist. Flubanserin has high affinity for human 5-HT1A receptor (Ki=1nm), low affinity for 5-HT2A (Ki=49nm) and D4 (Ki=4-24nm) receptors, and The affinity of other neurotransmitter receptors and ion channels is negligible. Flubanserin is used as a new non-hormonal treatment for women with premenopausal hyposexuality (HSDD). Flubanserin. Recently, flubanserin was found to reduce L-DOPA-induced dyskinesia in a Parkinson's disease model[4].Flibansetrin has high affinity for serotonin receptors in the brain: it acts as an agonist on 5-HT1A and an antagonist on 5-HT2A. In vivo, flibanserin binds equally to 5-HT1A and 5-HT2A receptors. However, under higher levels of brain 5-HT (i.e., under stress), flibanserin may occupy 5-HT2A receptors in higher proportion than 5-HT(1A) receptors. It may also moderately antagonize D4 (dopamine) receptors and 5-HT2B and 5-HTB2C. Its action on neurotransmitter receptors may contribute to reduction in serotonin levels and increase in dopamine and norepinephrine levels, all of which may play part in reward processing.

Flibanserin is used to treat low sexual desire in women who have not gone through menopause and have never had low sexual desire in the past. Flibanserin is for use only when low sexual desire is NOT caused by a medical condition, a mental disorder, relationship problems, or by using drugs or other medicines.

Flibanserin is not for women who have already gone through menopause. flibanserin is also not for use by men. Flibanserin is available only under a special program. You must be registered in the program and understand the risks and benefits of this medicine. Flibanserin may also be used for purposes not listed in this medication guide.

References

[1]Rueter L E , Montigny C D , Blier P . In vivo electrophysiological assessment of the agonistic properties of flibanserin at pre- and postsynaptic 5-HT1A receptors in the rat brain[J]. Synapse, 1998, 29(4):392-405.

[2]Stahl S M , Sommer B , Allers K A . Multifunctional Pharmacology of Flibanserin: Possible Mechanism of Therapeutic Action in Hypoactive Sexual Desire Disorder[J]. Journal of Sexual Medicine, 2011, 8(1):15-27.

[3]Invernizzi R W , Sacchetti G , Parini S , et al. Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT1A receptors[J]. British Journal of Pharmacology, 2003, 139(7):1281-1288.

[4]Hwang H Y , Cho S M , Kwon H J . Approaches for discovering novel bioactive small molecules targeting autophagy[J]. Expert Opinion on Drug Discovery, 2017, 12(11):1-15.

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Flibanserin

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