Flibanserin-d4 is intended for use as an internal standard for the quantification of flibanserin by GC- or LC-MS. Flibanserin is a full agonist of the serotonin 5-HT1A receptor and an antagonist of 5-HT2A (Kis = 1 and 49 nM, respectively).1 It also binds to dopamine D4 receptors with Ki values ranging from 4-24 nM, but demonstrates no affinity for the other 5-HT subtypes or other neurotransmitter receptors.1 In vitro, flibanserin has been shown to reduce forskolin-stimulated cAMP formation in cells and rat tissues and to antagonize the accumulation of phosphatidyl inositol turnover induced by 5-HT in the mouse cortex.1 At 10 mg/kg, flibanserin can reduce serotonin in the prefrontal cortex and dorsal raphe of conscious rats while increasing extracellular noradrenaline and dopamine.1
1.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 receptorsBr. J. Pharmacol.139(7)1281-1288(2003)