Flibanserin(Addyi)

Description

Flibanserin

The commecial name is Addyi

Density：1.292±0.06 g/cm3(Predicted)
Storage temp.：2-8°C
Solubility DMSO: soluble10mg/mL, clear
Form：powder
Pka：12.12±0.30(Predicted)
Color：white to beige
InChI：InChI=1S/C20H21F3N4O/c21-20(22,23)15-4-3-5-16(14-15)26-11-8-25(9-12-26)10-13-27-18-7-2-1-6-17(18)24-19(27)28/h1-7,14H,8-13H2,(H,24,28)
InChIKey：PPRRDFIXUUSXRA-UHFFFAOYSA-N
SMILES：C1(=O)N(CCN2CCN(C3=CC=CC(C(F)(F)F)=C3)CC2)C2=CC=CC=C2N1

Flibanserin Usage And Synthesis

Description
Flibanserin (Addyi-Sprout Pharmaceuticals) is a first-in-class oral medication approved by FDA for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. Although it meets the need for drugs that address women’s sexual function, flibanserin is unlike agents that treat erectile dysfunction, as it is intended to increase sexual desire, not performance.
Flibanserin is the first prescription medicine for the treatment of this sexual dysfunction. The FDA approval is not without warnings; flibanserin is subject to the Risk Evaluation and Mitigation Strategy (REMS) to ensure safe use by patients, and has a boxed warning directed to prescribing providers. The goal is to inform patients and providers of the increased risk of hypotension and syncope (Vallejos 2017).
Uses:
Filbanserin is an agonist of serotonin-5HT1A receptor and an antagonist of the 5-HT2A receptor. Binds dopamine receptors with Ki values ranging from 4-24 nM. Used to treat hypoactive sexual desire disorder in females.
Application:
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.
Mechanism of action:
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.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 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..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.
Drugs for enhancing female sexuality：
Flibanserin is the world’s first New drug for enhancing female sexuality. It can reduce the amount of 5-hydroxytryptamine which inhibits sexuality and improve sexual stimulant dopamine levels. It is already submitted to Food and Drug Administration of the United States for approval.This drug can directly effect on the sexual pleasure control area of the female brain to restore female Flagging libido. By adjusting the aphrodisiac body system, Flibanserin Helps to restore the balance of sexual appetite suppression and exciting mechanism and lead to form a healthy sexual performance. The curative effect can be obtained a few weeks later. At the same time, the female viagra also has a certain side effects. One-eighth of tested women appeared dizziness, fatigue and sleepiness. Similar to antidepressants, Flibanserin will affect the brain secretion chemicals associated with emotions and desires. In fact, it was used as a drug for the treatment of depression before before it becomes a sex medicine.Different from the working principle of “viagra”, Flibanserin works by adjusting the chemicals in female brains.In addition, “viagra” only works for most men, Flibanserin has effects on women with low libido. If the patient does not have a sexual interest to someone, Flibanserin will not affect her. Flibanserin will not cause hyperaphrodisia. Clayton. Anita, adviser of the drug companies says :“it is not an aphrodisiac and it only helps to balance the chemicals in the female brain to make a female restore sex desire, but not more than the normal level. However, it takes some time for this drug to work and women should take the drug every day.