Page last updated: 2024-11-11

flibanserin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID6918248
CHEMBL ID231068
CHEBI ID90865
SCHEMBL ID247579
MeSH IDM0257768

Synonyms (76)

Synonym
flibanserin ,
bimt-17-bs
girosa
bimt-17
167933-07-5
addyi (tn)
D02577
flibanserin (usan/inn)
flibanserin [usan]
1-(2-(4-(alpha,alpha,alpha-trifluoro-m-tolyl)-1-piperazinyl)ethyl)-2-benzimidazolinone
1-(2-(4-alpha,alpha,alpha-trifluoro-m-tolyl)-1-piperazinyl)ethyl)-2-benzimidazolinone
1-(2-(4-(3-trifluoromethylphenyl)piperazin-1-yl)ethyl)benzimidazol(1h)-2-one
bimt 17
1,3-dihydro-1-(2-(4-(3-(trifluoromethyl)phenyl)-1-piperazinyl)ethyl)-2h-benzimidazol-2-one
ectris
CHEMBL231068
bimt 17 bs
L001463
AKOS005146139
FT-0659246
3-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-1h-benzimidazol-2-one
A810922
3-[2-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]ethyl]-1h-benzimidazol-2-one
S3716
flibanserin [usan:inn]
37jk4str6z ,
female viagra [street name]
hsdb 8278
addyi
unii-37jk4str6z
AM84577
2h-benzimidazol-2-one, 1,3-dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-
SCHEMBL247579
girosa (proposed trade name)
gtpl8182
DB04908
flibanserin [who-dd]
1-(2-(4-(.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)-1-piperazinyl)ethyl)-2-benzimidazolinone
flibanserin [orange book]
flibanserin [mart.]
flibanserin [inn]
flibanserin [mi]
CS-4671
1-(2-(4-alpha,alpha,alpha-trifluoro-m-tolyl)-1-(piperazinyl)ethyl)-2-benzimidazolinone
CHEBI:90865 ,
female viagra (street name)
1-(2-{4-[3-(trifluoromethyl)phenyl]piperazin-1-yl}ethyl)-1,3-dihydro-2h-benzimidazol-2-one
1-[2-[4-(3-trifluoromethylphenyl)piperazin-1-yl]ethyl]benzimidazol-[1h]-2-one
HY-A0095
flibanserine
1-(2-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)ethyl)-1h-benzo[d]imidazol-2(3h)-one
mfcd00918402
bdbm50476735
2h-benzimidazol-2-one, 1,3-dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-; bimt 17; bimt 17bs; flibanserin
NCGC00386567-01
bimt-17bs
Q415996
BCP02131
EX-A2807
flibanserin; bimt-17; bimt-17bs
NCGC00386567-03
HMS3885K21
filbanserin.
CCG-268528
NCGC00386567-02
pprrdfixuusxra-uhfffaoysa-n
female viagra
dtxcid8090936
g02cx02
flibanserinum
flibanserin (mart.)
1-(2-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)ethyl)-1,3-dihydro-2h-benzimidazol-2-one
flibanserina
F1239
EN300-18167232
1-(2-{4-[3-(trifluoromethyl)phenyl]piperazin-1-yl}ethyl)-2,3-dihydro-1h-1,3-benzodiazol-2-one

Research Excerpts

Overview

Flibanserin (FLB) is a multifunctional serotonergic agent used for treating hypoactive sexual desire disorder in premenopausal women via oral administration. FlibansERin is a novel, non-hormonal drug for the treatment of HSDD in pre- and post menopausal women.

ExcerptReferenceRelevance
"Flibanserin is a new drug used for the treatment of hypoactive sexual desire disorder. "( Determination of flibanserin in the presence of confirmed degradation products by a third derivative emission spectrofluorometric method: Application to pharmaceutical formulation.
Abdallah, IA; Ahmed, RM, 2020
)
2.34
"Flibanserin (FLB) is a multifunctional serotonergic agent used for treating hypoactive sexual desire disorder in premenopausal women via oral administration. "( Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin.
Abdulaal, WH; Ahmed, OAA; Aldawsari, HM; Alhakamy, NA; Alomary, MN; Awan, ZA; Badr-Eldin, SM; Bakhrebah, MA; Fahmy, UA; Medina, C; Okbazghi, SZ, 2020
)
2.21
"Flibanserin is a serotonin 5-HT"( The pharmacodynamic effects of combined administration of flibanserin and alcohol.
Barbour, KA; Brown, L; Stahl, SM; Stevens, DM; Weems, JM, 2017
)
2.14
"Flibanserin is a postsynaptic 5-HT-1A agonist and 5-HT-2A antagonist for the treatment of generalized acquired hypoactive sexual desire disorder in premenopausal women."( Flibanserin Efficacy and Safety in Premenopausal Women With Generalized Acquired Hypoactive Sexual Desire Disorder.
Fisher, WA; Pyke, RE, 2017
)
3.34
"Flibanserin is a mixed 5-HT1A agonist and 5-HT2A antagonist for treatment of premenopausal women with hypoactive sexual desire disorder. "( Flibanserin for hypoactive sexual desire disorder in premenopausal women.
Clements, JN; Thompson, B, 2018
)
3.37
"Flibanserin is a mixed 5-HT1A agonist/5-HT2A antagonist that has been developed for the treatment of hypoactive sexual desire disorder in women."( Flibanserin treatment increases appetitive sexual motivation in the female rat.
Allers, KA; Gelez, H; Giuliano, F; Greggain-Mohr, J; Pfaus, JG, 2013
)
3.28
"Flibanserin is a novel, non-hormonal drug for the treatment of HSDD in pre- and postmenopausal women, although the application submitted to the U.S."( Flibanserin for female sexual dysfunction.
Reviriego, C, 2014
)
2.57
"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. "( Mechanism of action of flibanserin, a multifunctional serotonin agonist and antagonist (MSAA), in hypoactive sexual desire disorder.
Stahl, SM, 2015
)
2.17
"Flibanserin, is a postsynaptic agonist of serotonin receptor 1A and an antagonist of serotonin receptor 2A, has been shown to increase sexual desire and reduce distress in women with hypoactive sexual desire disorder (HSDD)."( Efficacy and Safety of Flibanserin in Women with Hypoactive Sexual Desire Disorder: A Systematic Review and Meta-Analysis.
Cui, Y; Gao, Z; Yang, D; Yu, L, 2015
)
2.17
"Flibanserin is a serotonin receptor subtype 1A agonist and 2A antagonist that has been approved by the Food and Drug Administration for treating female sexual interest and arousal disorder. "( Preclinical Abuse Potential Assessment of Flibanserin: Effects on Intracranial Self-Stimulation in Female and Male Rats.
Blough, BE; Lazenka, MF; Negus, SS, 2016
)
2.14
"Flibanserin is a novel pharmacologic agent in late-stage clinical testing for hypoactive sexual desire disorder (HSDD) in premenopausal women."( Multifunctional pharmacology of flibanserin: possible mechanism of therapeutic action in hypoactive sexual desire disorder.
Allers, KA; Sommer, B; Stahl, SM, 2011
)
2.1
"Flibanserin is a 5-HT(1A) agonist/5-HT(2A) antagonist that is under investigation as a treatment for HSDD in women."( Flibanserin: a potential treatment for Hypoactive Sexual Desire Disorder in premenopausal women.
Clayton, AH; Dennerstein, L; Pyke, R; Sand, M, 2010
)
2.52
"Flibanserin is a 5-HT(1A) agonist/5-HT(2A) antagonist that has been shown to increase sexual desire and reduce distress in premenopausal women with Hypoactive Sexual Desire Disorder (HSDD)."( Continued efficacy and safety of flibanserin in premenopausal women with Hypoactive Sexual Desire Disorder (HSDD): results from a randomized withdrawal trial.
Breaux, J; Goldfischer, ER; Katz, M; Kaufman, J; Kimura, T; Pyke, R; Sand, M; Smith, WB, 2011
)
2.09
"Flibanserin is a 5-HT1A receptor agonist and 5-HT2A receptor antagonist developed to possibly induce a more rapid onset of antidepressant action through its preferential postsynaptic 5-HT1A receptor agonism."( Electrophysiological examination of the effects of sustained flibanserin administration on serotonin receptors in rat brain.
Blier, P; Rueter, LE, 1999
)
1.27
"Flibanserin is a 5-HT1A agonist that, in contrast to other 5-HT1A receptor agonists, is capable of activating 5-HT1A receptors in frontal cortex. "( Behavioral effects of flibanserin (BIMT 17).
Borsini, F; Brambilla, A; Grippa, N; Pitsikas, N, 1999
)
2.06

Effects

Flibanserin has been approved in the USA for the treatment of premenopausal women with acquired, generalized HSDD. The drug has been shown to cause statistically significant increases in the number of satisfying sexual events and in sexual desire scores on standardized/validated measures.

ExcerptReferenceRelevance
"Flibanserin thus far has been trialed in only a narrow patient range: premenopausal women in long-term relationships with acquired or generalized HSDD."( Ignorance Is Not Bliss: If We Don't Understand Hypoactive Sexual Desire Disorder, How Can Flibanserin Treat It? Commentary.
Anderson, R; Moffatt, CE, 2018
)
1.42
"Flibanserin has been shown to cause statistically significant increases in the number of satisfying sexual events and in sexual desire scores on standardized/validated measures while reducing FSD-related distress of premenopausal women diagnosed with HSDD."( Flibanserin for the treatment of hypoactive sexual desire disorder in premenopausal women.
Dhanuka, I; Simon, JA, 2015
)
2.58
"Flibanserin has been approved in the USA for the treatment of premenopausal women with acquired, generalized HSDD."( Flibanserin: First Global Approval.
Deeks, ED, 2015
)
2.58
"Flibanserin (BIMT 17) has been described as a 5-HT1A agonist with preferential affinity for postsynaptic 5-HT1A receptors and as a 5-HT2A antagonist. "( In vivo electrophysiological assessment of the agonistic properties of flibanserin at pre- and postsynaptic 5-HT1A receptors in the rat brain.
Blier, P; de Montigny, C; Rueter, LE, 1998
)
1.98
"Flibanserin has been reported to be an agonist at 5-HT1A-receptors and an antagonist at 5-HT2A receptors, with higher affinity for 5-HT1A receptors. "( Ex vivo binding of flibanserin to serotonin 5-HT1A and 5-HT2A receptors.
Borsini, F; Monferini, E; Scandroglio, A, 2001
)
2.08
"Flibanserin has shown antidepressant-like properties in some animal models. "( Further characterisation of potential antidepressant action of flibanserin.
Borsini, F; Cesana, R, 2001
)
1.99

Actions

ExcerptReferenceRelevance
"Flibanserin displays antidepressant-like activity in most animal models sensitive to antidepressants."( Pharmacology of flibanserin.
Alexander, B; Borsini, F; Evans, K; Jason, K; Pollentier, S; Rohde, F, 2002
)
1.38

Treatment

ExcerptReferenceRelevance
"Treatment with flibanserin, on average, resulted in one-half additional SSE per month while statistically and clinically significantly increasing the risk of dizziness, somnolence, nausea, and fatigue. "( Efficacy and Safety of Flibanserin for the Treatment of Hypoactive Sexual Desire Disorder in Women: A Systematic Review and Meta-analysis.
Bramer, WM; Feys, F; Franco, OH; Jaspers, L; Laan, ET; Leusink, P, 2016
)
1.1

Toxicity

FDA concerns were raised about the risks of hypotension, syncope, and sedation-related adverse events, which increase with alcohol use. The most frequent adverse events associated with flibanserin were dizziness, somnolence, nausea, and headache.

ExcerptReferenceRelevance
" The most frequent adverse events associated with flibanserin were dizziness, somnolence, nausea, and headache."( Efficacy and safety of flibanserin in postmenopausal women with hypoactive sexual desire disorder: results of the SNOWDROP trial.
Garcia, M; Hanes, V; Kingsberg, SA; Sand, M; Shumel, B; Simon, JA, 2014
)
0.97
"This meta-analysis indicates that flibanserin to be an effective and safe treatment for HSDD in women."( Efficacy and Safety of Flibanserin in Women with Hypoactive Sexual Desire Disorder: A Systematic Review and Meta-Analysis.
Cui, Y; Gao, Z; Yang, D; Yu, L, 2015
)
1.01
" Safety outcomes included, among others, 4 common adverse events (AEs): dizziness, somnolence, nausea, and fatigue."( Efficacy and Safety of Flibanserin for the Treatment of Hypoactive Sexual Desire Disorder in Women: A Systematic Review and Meta-analysis.
Bramer, WM; Feys, F; Franco, OH; Jaspers, L; Laan, ET; Leusink, P, 2016
)
0.74
" Adverse effects were mostly minor: dizziness and drowsiness."( [Efficacy and safety of flibanserin "new female Viagra
Terrier, C; Terrier, JE,
)
0.44
" The most common side effect of flibanserin was somnolence."( Systematic Review and Meta-analysis of Flibanserin's Effects and Adverse Events in Women with Hypoactive Sexual Desire Disorder.
Hosseinialhashemi, M; Kabir, A; Panahi, Y; Rahmani, K; Saadat, SH; Sahebkar, A, 2017
)
1.01
"Safety assessment included adverse events and symptoms of depression and anxiety."( Safety of Flibanserin in Women Treated With Antidepressants: A Randomized, Placebo-Controlled Study.
Brown, L; Clayton, AH; Croft, HA; Kissling, R; Yuan, J, 2018
)
0.88
" The most common adverse events (incidence ≥ 2% in the flibanserin group and higher than that in the placebo group) included dry mouth (5."( Safety of Flibanserin in Women Treated With Antidepressants: A Randomized, Placebo-Controlled Study.
Brown, L; Clayton, AH; Croft, HA; Kissling, R; Yuan, J, 2018
)
1.13
"In this small trial, flibanserin 100 mg qhs was generally safe and well tolerated in premenopausal women with mild or remitted depression taking a serotonergic antidepressant."( Safety of Flibanserin in Women Treated With Antidepressants: A Randomized, Placebo-Controlled Study.
Brown, L; Clayton, AH; Croft, HA; Kissling, R; Yuan, J, 2018
)
1.2
"The primary end point of this OLE study was the incidence of adverse events (AEs)."( Flibanserin for Hypoactive Sexual Desire Disorder: An Open-Label Safety Study.
Brown, L; Derogatis, L; Kissling, R; Portman, D; Simon, JA; Yuan, J, 2018
)
1.92
"In this open-label study, flibanserin 100 mg once daily at bedtime was generally safe and well tolerated by premenopausal and naturally postmenopausal women with HSDD."( Flibanserin for Hypoactive Sexual Desire Disorder: An Open-Label Safety Study.
Brown, L; Derogatis, L; Kissling, R; Portman, D; Simon, JA; Yuan, J, 2018
)
2.22
" During the FDA's review of flibanserin, concerns were raised about the risks of hypotension, syncope, and sedation-related adverse events, which increase with alcohol use."( Evaluation of Flibanserin Safety: Comparison with Other Serotonergic Medications.
Clayton, AH; Kingsberg, SA; McElroy, SL, 2019
)
1.17
"To evaluate the adverse event profile of flibanserin in the context of that seen with other medications that affect serotonin in the brain and are commonly prescribed for women."( Evaluation of Flibanserin Safety: Comparison with Other Serotonergic Medications.
Clayton, AH; Kingsberg, SA; McElroy, SL, 2019
)
1.14
"The incidence of adverse events was assessed."( Evaluation of Flibanserin Safety: Comparison with Other Serotonergic Medications.
Clayton, AH; Kingsberg, SA; McElroy, SL, 2019
)
0.87
"The incidences of hypotension, syncope, and sedation-related adverse events (eg, dizziness, somnolence, fatigue) in studies of flibanserin were within the ranges observed for serotonergic antidepressants; the rates of these adverse events were generally lower with triptan medications."( Evaluation of Flibanserin Safety: Comparison with Other Serotonergic Medications.
Clayton, AH; Kingsberg, SA; McElroy, SL, 2019
)
1.08
"Although medications that affect the serotonin system have varying adverse event profiles (likely mediated by differences in serotonin-related mechanisms of action, specific brain structures affected, and effects on other neurotransmitter systems), the occurrence of central nervous system-related adverse events was not dissimilar between flibanserin and serotonergic antidepressants."( Evaluation of Flibanserin Safety: Comparison with Other Serotonergic Medications.
Clayton, AH; Kingsberg, SA; McElroy, SL, 2019
)
1.05

Pharmacokinetics

Results from this study suggest that increased incidence of hypotension- and syncope-related events may result from a pharmacodynamic interaction between flibanserin and alcohol. The clinical significance of these interactions in real-world populations remains unclear.

ExcerptReferenceRelevance
"Results from this study suggest that increased incidence of hypotension- and syncope-related events may result from a pharmacodynamic interaction between flibanserin and alcohol, although the clinical significance of these interactions in real-world populations remains unclear."( The pharmacodynamic effects of combined administration of flibanserin and alcohol.
Barbour, KA; Brown, L; Stahl, SM; Stevens, DM; Weems, JM, 2017
)
0.9
"The assay procedure was fully validated and successfully applied in pharmacokinetic interaction study of flibanserin with bosentan in rats."( A validated UPLC-MS/MS method for flibanserin in plasma and its pharmacokinetic interaction with bosentan in rats.
Al-Rashood, KA; Bajrai, AA; Ezzeldin, E; Iqbal, M; Rezk, NL, 2018
)
0.97
" The developed method was used to quantitate FLB in the plasma and brain tissue of a single-dose oral pharmacokinetic and brain tissue distribution study in female rats."( Mass Spectrometry-Based Rapid Quantitative Bioanalysis of Flibanserin: Pharmacokinetic and Brain Tissue Distribution Study in Female Rats.
Rathod, R; Sengupta, P; Sharma, MK, 2020
)
0.8

Compound-Compound Interactions

ExcerptReferenceRelevance
" Effects of Alcohol Administered With Flibanserin in Healthy Premenopausal Women: A Randomized, Double-Blind, Single-Dose Crossover Study."( Effects of Alcohol Administered With Flibanserin in Healthy Premenopausal Women: A Randomized, Double-Blind, Single-Dose Crossover Study.
Apfel, SC; Clayton, AH; Millheiser, L; Parish, SJ; Simon, JA, 2020
)
1.1

Bioavailability

ExcerptReferenceRelevance
"Solubility and dissolution relationships in the gastrointestinal tract can be critical for the oral bioavailability of poorly soluble drugs."( Predicting the precipitation of poorly soluble weak bases upon entry in the small intestine.
Becker, R; Bock, T; Brauns, U; Dressman, JB; Kostewicz, ES; Wunderlich, M, 2004
)
0.32
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" FLB has a reported limited oral bioavailability of 33% that could be attributed to the drug's first-pass metabolism."( Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin.
Abdulaal, WH; Ahmed, OAA; Aldawsari, HM; Alhakamy, NA; Alomary, MN; Awan, ZA; Badr-Eldin, SM; Bakhrebah, MA; Fahmy, UA; Medina, C; Okbazghi, SZ, 2020
)
0.77
"The aforementioned results highlight the safety of FLB-NLC in situ nasal gel and its potential to improve the drug bioavailability and brain delivery."( Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin.
Abdulaal, WH; Ahmed, OAA; Aldawsari, HM; Alhakamy, NA; Alomary, MN; Awan, ZA; Badr-Eldin, SM; Bakhrebah, MA; Fahmy, UA; Medina, C; Okbazghi, SZ, 2020
)
0.77

Dosage Studied

Sustained increases in baseline of DA and norepinephrine are observed in the PFC, and flibanserin dosing increases DA and NE levels above the basal changes. Limitations include the morning dosing of study medication, which is inconsistent with the bedtime dosing recommended for flibANSerin.

ExcerptRelevanceReference
" Sustained increases in baseline of DA and norepinephrine (NE) are observed in the PFC, and flibanserin dosing increases DA and NE levels above the basal changes."( Multifunctional pharmacology of flibanserin: possible mechanism of therapeutic action in hypoactive sexual desire disorder.
Allers, KA; Sommer, B; Stahl, SM, 2011
)
0.87
" At week 24, women who showed a predefined response, measured using an eDiary, were randomized to 24 weeks of continued flibanserin therapy at optimized dosage (N = 163) or placebo (N = 170)."( Continued efficacy and safety of flibanserin in premenopausal women with Hypoactive Sexual Desire Disorder (HSDD): results from a randomized withdrawal trial.
Breaux, J; Goldfischer, ER; Katz, M; Kaufman, J; Kimura, T; Pyke, R; Sand, M; Smith, WB, 2011
)
0.86
"To assess the acute and chronic dose-response effects of flibanserin on measures of sexual desire and copulation in ovariectomized rats primed with estradiol benzoate (EB) alone or in combination with progesterone (P)."( Flibanserin treatment increases appetitive sexual motivation in the female rat.
Allers, KA; Gelez, H; Giuliano, F; Greggain-Mohr, J; Pfaus, JG, 2013
)
2.08
"The objective of this study was to determine the next-day residual effects of acute and steady-state nighttime dosing of flibanserin on simulated driving performance and cognitive function in healthy premenopausal women."( Next-day residual effects of flibanserin on simulated driving performance in premenopausal women.
Hochadel, T; Kay, GG; Kim, NN; Natarajan, KK; Sicard, E, 2017
)
0.95
" Simulated driving assessments were conducted 9 hr after dosing and cognitive function tests were administered immediately before or during the driving assessment."( Next-day residual effects of flibanserin on simulated driving performance in premenopausal women.
Hochadel, T; Kay, GG; Kim, NN; Natarajan, KK; Sicard, E, 2017
)
0.75
"7% after flibanserin dosing and 57."( Effects of Timing of Flibanserin Administration Relative to Alcohol Intake in Healthy Premenopausal Women: A Randomized, Double-Blind, Crossover Study.
Clayton, AH; Kim, NN; Kingsberg, SA; Millheiser, L; Parish, SJ; Simon, JA, 2019
)
1.25
" Treatments were administered using a worst-case approach that included morning dosing and consumption of alcohol within 10 minutes."( Effects of Alcohol Administered With Flibanserin in Healthy Premenopausal Women: A Randomized, Double-Blind, Single-Dose Crossover Study.
Apfel, SC; Clayton, AH; Millheiser, L; Parish, SJ; Simon, JA, 2020
)
0.83
" Limitations include the morning dosing of study medication, which is inconsistent with the bedtime dosing recommended for flibanserin, and the method of handling missing vital sign measurements."( Effects of Alcohol Administered With Flibanserin in Healthy Premenopausal Women: A Randomized, Double-Blind, Single-Dose Crossover Study.
Apfel, SC; Clayton, AH; Millheiser, L; Parish, SJ; Simon, JA, 2020
)
1.04
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
serotonergic agonistAn agent that has an affinity for serotonin receptors and is able to mimic the effects of serotonin by stimulating the physiologic activity at the cell receptors. Serotonin agonists are used as antidepressants, anxiolytics, and in the treatment of migraine disorders.
serotonergic antagonistDrugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
N-arylpiperazine
N-alkylpiperazine
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.48660.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency18.99910.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency7.56370.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency18.99910.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency18.99910.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.01180.00010.532610.0000AID1907040
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC50 (µMol)0.63100.00010.25718.0000AID298093
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (60)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID298095Induction of forepaw treading in orally dosed rat after 60 mins2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID298098Antidepressant like activity in orally dosed rat after 60 mins by forced swimming test2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID298092Binding affinity to 5HT1A receptor in rat cortex membrane2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID298094Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to 5-hydroxytryptamine2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID298096Induction of flat body posture in orally dosed rat as after 60 mins2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID1907040Displacement of [3H]-5-OH-DPAT from human 5-HT1AR in human brain tissue by radioligand binding assay
AID298093Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2002CNS drug reviews, Summer, Volume: 8, Issue:2
Pharmacology of flibanserin.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)2002CNS drug reviews, Summer, Volume: 8, Issue:2
Pharmacology of flibanserin.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (162)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (4.94)18.2507
2000's13 (8.02)29.6817
2010's118 (72.84)24.3611
2020's23 (14.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.13

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index56.13 (24.57)
Research Supply Index5.21 (2.92)
Research Growth Index5.28 (4.65)
Search Engine Demand Index170.35 (26.88)
Search Engine Supply Index3.74 (0.95)

This Compound (56.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials14 (8.33%)5.53%
Reviews33 (19.64%)6.00%
Case Studies2 (1.19%)4.05%
Observational0 (0.00%)0.25%
Other119 (70.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]