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Identification
NameFlibanserin
Accession NumberDB04908
TypeSmall Molecule
GroupsApproved
Description

Flibanserin is the first drug to be approved for hypoactive sexual desire disorder (HSDD) in premenopausal women by the FDA in August 2015. It was originally developed as an antidepressant medication by Boehringer Ingelheim, but showed lack of efficacy in trials and was further developed as a hypoactive sexual disorder drug by Sprout Pharmaceuticals. Flibanserin’s mechanism of action is attributed to its high affinity for 5-HTA1 and 5-HTA2 receptors, displaying agonist activity on 5-HTA1 and antagonist on 5-HTA2, resulting in lowering of serotonin in the brain as well as an effect on increasing norepinephrine and dopamine neurotransmitters.

Structure
Thumb
Synonyms
BIMT-17
BIMT-17-BS
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Addyitablet, film coated100 mg/1oralSprout Pharmaceuticals, Inc.2015-08-18Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EctrisNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Flibanserin hydrochloride
ThumbNot applicableDBSALT001321
Categories
UNII37JK4STR6Z
CAS number167933-07-5
WeightAverage: 390.4021
Monoisotopic: 390.166745929
Chemical FormulaC20H21F3N4O
InChI KeyPPRRDFIXUUSXRA-UHFFFAOYSA-N
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)
IUPAC Name
1-(2-{4-[3-(trifluoromethyl)phenyl]piperazin-1-yl}ethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
SMILES
FC(F)(F)C1=CC(=CC=C1)N1CCN(CCN2C(=O)NC3=CC=CC=C23)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazinanes
Sub ClassPiperazines
Direct ParentPhenylpiperazines
Alternative Parents
Substituents
  • N-arylpiperazine
  • Phenylpiperazine
  • Benzimidazole
  • Substituted aniline
  • Dialkylarylamine
  • N-alkylpiperazine
  • Aniline
  • Benzenoid
  • N-substituted imidazole
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Urea
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women.
PharmacodynamicsNot Available
Mechanism of actionFlibansetrin 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. However, under higher levels of brain 5-HT (i.e., under stress), flibanserin may occupy 5-HT2A receptors in higher proportion than 5-HT(1A) receptors. It may also moderately antagonize D4 (dopamine) receptors and 5-HT2B and 5-HTB2C. Its action on neurotransmitter receptors may contribute to reduction in serotonin levels and increase in dopamine and norepinephrine levels, all of which may play part in reward processing.
Related Articles
AbsorptionFlibanserin has an absolute oral availability of 33%.
Volume of distributionNot Available
Protein binding~98%, highly bound to proteins (mostly albumin) in serum.
Metabolism

Metabolism is primarily via CYP3A4, slightly CYP2C19. Minimal involvement of CYP1A2, CYP2B6, CYP2C8, CYP2C9 or CYP2D6. At least 35 metabolites of flibanserin are produced, 2 of which reach plasma concentrations as high as parent drug, however they are pharmacologically inactive.

Route of eliminationElimination via feces (51%) and urine (44%) following a single oral 50 mg dose of flibanserin solution.
Half life≈11 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9857
Caco-2 permeable-0.7652
P-glycoprotein substrateSubstrate0.6865
P-glycoprotein inhibitor IInhibitor0.8895
P-glycoprotein inhibitor IIInhibitor0.8741
Renal organic cation transporterInhibitor0.6378
CYP450 2C9 substrateNon-substrate0.7906
CYP450 2D6 substrateNon-substrate0.5905
CYP450 3A4 substrateSubstrate0.6954
CYP450 1A2 substrateInhibitor0.8379
CYP450 2C9 inhibitorNon-inhibitor0.7028
CYP450 2D6 inhibitorInhibitor0.5876
CYP450 2C19 inhibitorNon-inhibitor0.59
CYP450 3A4 inhibitorInhibitor0.7523
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9005
Ames testNon AMES toxic0.6798
CarcinogenicityNon-carcinogens0.9354
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6546 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6138
hERG inhibition (predictor II)Inhibitor0.9486
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet, film coatedoral100 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7151103 No2003-05-092023-05-09Us
US7420057 No2002-08-012022-08-01Us
US8227471 No2003-05-092023-05-09Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.178 mg/mLALOGPS
logP3.32ALOGPS
logP3.83ChemAxon
logS-3.3ALOGPS
pKa (Strongest Acidic)12.91ChemAxon
pKa (Strongest Basic)7.03ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area38.82 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity103.65 m3·mol-1ChemAxon
Polarizability38.69 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R: Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors. Br J Pharmacol. 2003 Aug;139(7):1281-8. [PubMed:12890707 ]
  2. Scandroglio A, Monferini E, Borsini F: Ex vivo binding of flibanserin to serotonin 5-HT1A and 5-HT2A receptors. Pharmacol Res. 2001 Feb;43(2):179-83. [PubMed:11243720 ]
  3. Borsini F, Cesana R: Mechanism of action of flibanserin in the learned helplessness paradigm in rats. Eur J Pharmacol. 2001 Dec 14;433(1):81-9. [PubMed:11755137 ]
  4. Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S: Pharmacology of flibanserin. CNS Drug Rev. 2002 Summer;8(2):117-42. [PubMed:12177684 ]
  5. Deeks ED: Flibanserin: First Global Approval. Drugs. 2015 Oct;75(15):1815-22. doi: 10.1007/s40265-015-0474-y. [PubMed:26412054 ]
  6. Stahl SM: Mechanism of action of flibanserin, a multifunctional serotonin agonist and antagonist (MSAA), in hypoactive sexual desire disorder. CNS Spectr. 2015 Feb;20(1):1-6. doi: 10.1017/S1092852914000832. Epub 2015 Feb 9. [PubMed:25659981 ]
External Links
ATC CodesG02CX02
AHFS Codes
  • 28:92
PDB EntriesNot Available
FDA labelDownload (788 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Flibanserin.
AlprazolamThe serum concentration of Flibanserin can be increased when it is combined with Alprazolam.
AmiodaroneThe serum concentration of Flibanserin can be increased when it is combined with Amiodarone.
AmlodipineThe serum concentration of Flibanserin can be increased when it is combined with Amlodipine.
AprepitantThe serum concentration of Flibanserin can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Flibanserin can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Flibanserin can be increased when it is combined with Atorvastatin.
AzelastineFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Flibanserin.
BexaroteneThe serum concentration of Flibanserin can be decreased when it is combined with Bexarotene.
BicalutamideThe serum concentration of Flibanserin can be increased when it is combined with Bicalutamide.
BoceprevirThe serum concentration of Flibanserin can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Flibanserin can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Flibanserin.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Flibanserin.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
BuprenorphineFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CarbamazepineThe serum concentration of Flibanserin can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Flibanserin can be increased when it is combined with Ceritinib.
ChloramphenicolThe serum concentration of Flibanserin can be increased when it is combined with Chloramphenicol.
ChlorotrianiseneThe serum concentration of Flibanserin can be increased when it is combined with Chlorotrianisene.
CilostazolThe serum concentration of Flibanserin can be increased when it is combined with Cilostazol.
CimetidineThe serum concentration of Flibanserin can be increased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Flibanserin can be increased when it is combined with Ciprofloxacin.
ClarithromycinThe serum concentration of Flibanserin can be increased when it is combined with Clarithromycin.
ClotrimazoleThe serum concentration of Flibanserin can be increased when it is combined with Clotrimazole.
CobicistatThe serum concentration of Flibanserin can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Flibanserin.
ConivaptanThe serum concentration of Flibanserin can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Flibanserin can be increased when it is combined with Crizotinib.
CyclosporineThe serum concentration of Flibanserin can be increased when it is combined with Cyclosporine.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Flibanserin.
DabrafenibThe serum concentration of Flibanserin can be decreased when it is combined with Dabrafenib.
DanazolThe serum concentration of Flibanserin can be increased when it is combined with Danazol.
DarunavirThe serum concentration of Flibanserin can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Flibanserin can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Flibanserin can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Flibanserin can be increased when it is combined with Delavirdine.
DexamethasoneThe serum concentration of Flibanserin can be decreased when it is combined with Dexamethasone.
DienogestThe serum concentration of Flibanserin can be increased when it is combined with Dienogest.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Flibanserin.
DiltiazemThe serum concentration of Flibanserin can be increased when it is combined with Diltiazem.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Flibanserin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
DronedaroneThe serum concentration of Flibanserin can be increased when it is combined with Dronedarone.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Flibanserin.
EfavirenzThe serum concentration of Flibanserin can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Flibanserin can be decreased when it is combined with Enzalutamide.
ErythromycinThe serum concentration of Flibanserin can be increased when it is combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Flibanserin can be decreased when it is combined with Eslicarbazepine acetate.
EthanolEthanol may increase the hypotensive activities of Flibanserin.
EtonogestrelThe serum concentration of Flibanserin can be increased when it is combined with Etonogestrel.
EtravirineThe serum concentration of Flibanserin can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Flibanserin.
FluconazoleThe serum concentration of Flibanserin can be increased when it is combined with Fluconazole.
FluvoxamineThe serum concentration of Flibanserin can be increased when it is combined with Fluvoxamine.
FosamprenavirThe serum concentration of Flibanserin can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Flibanserin can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Flibanserin can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Flibanserin can be increased when it is combined with Fusidic Acid.
GemfibrozilThe serum concentration of Flibanserin can be increased when it is combined with Gemfibrozil.
Glycerol PhenylbutyrateThe serum concentration of Flibanserin can be increased when it is combined with Glycerol Phenylbutyrate.
HydrocodoneFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
IdelalisibThe serum concentration of Flibanserin can be increased when it is combined with Idelalisib.
IloperidoneThe serum concentration of Flibanserin can be increased when it is combined with Iloperidone.
ImatinibThe serum concentration of Flibanserin can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Flibanserin can be increased when it is combined with Indinavir.
IsavuconazoniumThe serum concentration of Flibanserin can be increased when it is combined with Isavuconazonium.
IsoniazidThe serum concentration of Flibanserin can be increased when it is combined with Isoniazid.
ItraconazoleThe serum concentration of Flibanserin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Flibanserin can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Flibanserin can be increased when it is combined with Ketoconazole.
LapatinibThe serum concentration of Flibanserin can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Flibanserin.
LevonorgestrelThe serum concentration of Flibanserin can be increased when it is combined with Levonorgestrel.
LomitapideThe serum concentration of Flibanserin can be increased when it is combined with Lomitapide.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Flibanserin.
LuliconazoleThe serum concentration of Flibanserin can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Flibanserin can be increased when it is combined with Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
Medroxyprogesterone acetateThe serum concentration of Flibanserin can be increased when it is combined with Medroxyprogesterone Acetate.
MethotrimeprazineFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineFlibanserin may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Flibanserin can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
MirtazapineFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MitotaneThe serum concentration of Flibanserin can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Flibanserin can be decreased when it is combined with Modafinil.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
NafcillinThe serum concentration of Flibanserin can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Flibanserin.
NefazodoneThe serum concentration of Flibanserin can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Flibanserin can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Flibanserin can be increased when it is combined with Nicardipine.
NilotinibThe serum concentration of Flibanserin can be increased when it is combined with Nilotinib.
NorethisteroneThe serum concentration of Flibanserin can be increased when it is combined with Norethindrone.
OrphenadrineFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Flibanserin can be increased when it is combined with Palbociclib.
ParaldehydeFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Flibanserin is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Flibanserin.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
PhenobarbitalThe serum concentration of Flibanserin can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Flibanserin can be decreased when it is combined with Phenytoin.
PosaconazoleThe serum concentration of Flibanserin can be increased when it is combined with Posaconazole.
PramipexoleFlibanserin may increase the sedative activities of Pramipexole.
PrimidoneThe serum concentration of Flibanserin can be decreased when it is combined with Primidone.
PropofolThe serum concentration of Flibanserin can be increased when it is combined with Propofol.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Flibanserin.
QuinidineThe serum concentration of Flibanserin can be increased when it is combined with Quinidine.
RanolazineThe serum concentration of Flibanserin can be increased when it is combined with Ranolazine.
RifabutinThe serum concentration of Flibanserin can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Flibanserin can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Flibanserin can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Flibanserin.
RitonavirThe serum concentration of Flibanserin can be increased when it is combined with Ritonavir.
RopiniroleFlibanserin may increase the sedative activities of Ropinirole.
RotigotineFlibanserin may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flibanserin.
SaquinavirThe serum concentration of Flibanserin can be increased when it is combined with Saquinavir.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Flibanserin.
SiltuximabThe serum concentration of Flibanserin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Flibanserin can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
StiripentolThe serum concentration of Flibanserin can be increased when it is combined with Stiripentol.
SuvorexantFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
TelaprevirThe serum concentration of Flibanserin can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Flibanserin can be increased when it is combined with Telithromycin.
ThalidomideFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TicagrelorThe serum concentration of Flibanserin can be increased when it is combined with Ticagrelor.
TiclopidineThe serum concentration of Flibanserin can be increased when it is combined with Ticlopidine.
TocilizumabThe serum concentration of Flibanserin can be decreased when it is combined with Tocilizumab.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Flibanserin.
VerapamilThe serum concentration of Flibanserin can be increased when it is combined with Verapamil.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Flibanserin.
VoriconazoleThe serum concentration of Flibanserin can be increased when it is combined with Voriconazole.
ZolpidemFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R: Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors. Br J Pharmacol. 2003 Aug;139(7):1281-8. [PubMed:12890707 ]
  2. Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S: Pharmacology of flibanserin. CNS Drug Rev. 2002 Summer;8(2):117-42. [PubMed:12177684 ]
  3. Deeks ED: Flibanserin: First Global Approval. Drugs. 2015 Oct;75(15):1815-22. doi: 10.1007/s40265-015-0474-y. [PubMed:26412054 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S: Pharmacology of flibanserin. CNS Drug Rev. 2002 Summer;8(2):117-42. [PubMed:12177684 ]
  2. Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R: Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors. Br J Pharmacol. 2003 Aug;139(7):1281-8. [PubMed:12890707 ]
  3. Deeks ED: Flibanserin: First Global Approval. Drugs. 2015 Oct;75(15):1815-22. doi: 10.1007/s40265-015-0474-y. [PubMed:26412054 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S: Pharmacology of flibanserin. CNS Drug Rev. 2002 Summer;8(2):117-42. [PubMed:12177684 ]
  2. Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R: Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors. Br J Pharmacol. 2003 Aug;139(7):1281-8. [PubMed:12890707 ]
  3. Deeks ED: Flibanserin: First Global Approval. Drugs. 2015 Oct;75(15):1815-22. doi: 10.1007/s40265-015-0474-y. [PubMed:26412054 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Deeks ED: Flibanserin: First Global Approval. Drugs. 2015 Oct;75(15):1815-22. doi: 10.1007/s40265-015-0474-y. [PubMed:26412054 ]
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Drug created on October 21, 2007 16:23 / Updated on July 27, 2016 01:58