Related Diseases
Depression
Size
10.0mg; 25.0mg; 50.0mg
Description
Flibanserin is a full agonist of the 5-HT1A receptor (Ki = 1 nM) and, with lower affinity, as an antagonist of the 5-HT2A receptor (Ki = 49 nM) and antagonist or very weak partial agonist of the D4 receptor (Ki = 4–24 nM). Despite the much greater affinity of flibanserin for the 5-HT1A receptor, and for reasons that are unknown, flibanserin occupies the 5-HT1A and 5-HT2A receptors in vivo with similar percentages. Flibanserin also has low affinity for the 5-HT2B receptor (Ki = 89.3 nM) and the 5-HT2C receptor (Ki = 88.3 nM), both of which it behaves as an antagonist of. Flibanserin preferentially activates 5-HT1A receptors in the prefrontal cortex, demonstrating regional selectivity, and has been found to increase dopamine and norepinephrine levels and decrease serotonin levels in the rat prefrontal cortex, actions that were determined to be mediated by activation of the 5-HT1A receptor.[12] As such, flibanserin has been described as a norepinephrine-dopamine disinhibitor (NDDI). Flibanserin was approved in August 2015 for the treatment of pre-menopausal women with hypoactive sexual desire disorder (HSDD).
Chemical Formula
C20H21F3N4O
Elemental Analysis
C, 61.53; H, 5.42; F, 14.60; N, 14.35; O, 4.10
Synonym
BIMT 17; BIMT-17; BIMT17; BIMT 17BS; BIMT-17BS; BIMT17BS; EBD6396; EBD 6396; EBD-6396; Flibanserin. Brand name: Addyi.
IUPAC/Chemical Name
1-(2-{4-[3-(Trifluoromethyl)phenyl]piperazin-1-yl}ethyl)-1,3-dihydro-2H-benzimidazol-2-one
InChi Key
PPRRDFIXUUSXRA-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
O=C1NC2=CC=CC=C2N1CCN3CCN(C4=CC=CC(C(F)(F)F)=C4)CC3
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).
HS Tariff Code
2934.99.9001