Preferred Name

Flibanserin
Synonyms
Definitions

An orally bioavailable, non-hormonal, multifunctional serotonin agonist and antagonist (MSAA) that may improve sexual desire and arousal in women. Upon oral administration, flibanserin selectively binds to serotonin receptors in the central nervous system, acting as an agonist on 5-HT1A receptors and an antagonist on 5-HT2A receptors. Agonist activity at 5-HT1A postsynaptic receptors may enhance the release of dopamine and other monoamines. Combined with 5-HT2A antagonism, flibanserin boosts levels of dopamine in the mesocortical area of the prefrontal cortex and produces a net increase of norepinephrine selectively in the prefrontal cortex through disinhibition of locus coeruleus noradrenergic neurons. In addition, flibanserin reduces concentrations of serotonin in the prefrontal cortex with chronic administration. Reducing serotonin, which modulates sexual activity in an inhibitory fashion through downstream decreases in dopamine release, while enhancing the release of norepinephrine and dopamine in the prefrontal cortex may improve sexual desire and interest.

ID

http://purl.obolibrary.org/obo/NCIT_C80769

CAS_Registry

167933-07-5

Chemical_Formula

C20H21F3N4O

code

C80769

Contributing_Source

CTRP

FDA

definition

An orally bioavailable, non-hormonal, multifunctional serotonin agonist and antagonist (MSAA) that may improve sexual desire and arousal in women. Upon oral administration, flibanserin selectively binds to serotonin receptors in the central nervous system, acting as an agonist on 5-HT1A receptors and an antagonist on 5-HT2A receptors. Agonist activity at 5-HT1A postsynaptic receptors may enhance the release of dopamine and other monoamines. Combined with 5-HT2A antagonism, flibanserin boosts levels of dopamine in the mesocortical area of the prefrontal cortex and produces a net increase of norepinephrine selectively in the prefrontal cortex through disinhibition of locus coeruleus noradrenergic neurons. In addition, flibanserin reduces concentrations of serotonin in the prefrontal cortex with chronic administration. Reducing serotonin, which modulates sexual activity in an inhibitory fashion through downstream decreases in dopamine release, while enhancing the release of norepinephrine and dopamine in the prefrontal cortex may improve sexual desire and interest.

Display_Name

Flibanserin

FDA_UNII_Code

37JK4STR6Z

in_subset

http://purl.obolibrary.org/obo/NCIT_C63923

http://purl.obolibrary.org/obo/NCIT_C176424

http://purl.obolibrary.org/obo/NCIT_C116977

http://purl.obolibrary.org/obo/NCIT_C116978

label

Flibanserin

Legacy Concept Name

Flibanserin

NCI_Drug_Dictionary_ID

797893

PDQ_Closed_Trial_Search_ID

797893

PDQ_Open_Trial_Search_ID

797893

Preferred_Name

Flibanserin

prefixIRI

NCIT:C80769

prefLabel

Flibanserin

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C0754280

subClassOf

http://purl.obolibrary.org/obo/NCIT_C66885

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