Details
Stereochemistry | RACEMIC |
Molecular Formula | C12H16F3N |
Molecular Weight | 231.2573 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCNC(C)CC1=CC(=CC=C1)C(F)(F)F
InChI
InChIKey=DBGIVFWFUFKIQN-UHFFFAOYSA-N
InChI=1S/C12H16F3N/c1-3-16-9(2)7-10-5-4-6-11(8-10)12(13,14)15/h4-6,8-9,16H,3,7H2,1-2H3
Molecular Formula | C12H16F3N |
Molecular Weight | 231.2573 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
DescriptionSources: https://www.drugbank.ca/drugs/DB00574Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/fenfluramine.html | https://www.ncbi.nlm.nih.gov/pubmed/24790728 | https://clinicaltrials.gov/ct2/show/NCT02655198 | https://www.ncbi.nlm.nih.gov/pubmed/27264138 | https://www.ncbi.nlm.nih.gov/pubmed/22554283 | https://www.ncbi.nlm.nih.gov/pubmed/26600876
Sources: https://www.drugbank.ca/drugs/DB00574
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/fenfluramine.html | https://www.ncbi.nlm.nih.gov/pubmed/24790728 | https://clinicaltrials.gov/ct2/show/NCT02655198 | https://www.ncbi.nlm.nih.gov/pubmed/27264138 | https://www.ncbi.nlm.nih.gov/pubmed/22554283 | https://www.ncbi.nlm.nih.gov/pubmed/26600876
Fenfluramine (former brand names Pondimin, Ponderax and Adifax), also known as 3-trifluoromethyl-N-ethylamphetamine, is an anorectic that is no longer marketed. In combination with phentermine, it was part of the anti-obesity medication Fen-phen. Fenfluramine was introduced on the U.S. market in 1973 and withdrawn in 1997. It is the racemic mixture of two enantiomers, dexfenfluramine, and levofenfluramine. The drug increases the level of serotonin, a neurotransmitter that regulates mood, appetite and other functions. Fenfluramine causes the release of serotonin by disrupting vesicular storage of the neurotransmitter and reversing serotonin transporter function. The drug was withdrawn from the U.S. market in 1997 after reports of heart valve disease and pulmonary hypertension, including a condition known as cardiac fibrosis. It was subsequently withdrawn from other markets around the world. In this small exploratory and retrospective study, remarkably good results were reported on the use of fenfluramine as an add-on medication for controlling seizures in patients with the Dravet syndrome. The side effects were rare and nonserious and did not result in termination of the treatment. It is possible that this drug may have anticonvulsive effects for other severe epilepsy syndromes, especially in those characterized by photosensitive or induced seizures.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: GO:0001820 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16237679 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Pondimin Approved UseUnknown |
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Primary | Pondimin Approved UseUnknown |
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Primary | Pondimin Approved UseUnknown |
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Primary | Pondimin Approved UseUnknown |
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Primary | Pondimin Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
68 ng/mL |
0.35 mg/kg 2 times / day steady-state, oral dose: 0.35 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENFLURAMINE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1390 ng × h/mL |
0.35 mg/kg 2 times / day steady-state, oral dose: 0.35 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENFLURAMINE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20 h |
0.35 mg/kg 2 times / day steady-state, oral dose: 0.35 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENFLURAMINE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
50% |
0.35 mg/kg 2 times / day steady-state, oral dose: 0.35 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENFLURAMINE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
60 mg/day 1 times / day steady, oral Highest studied dose Dose: 60 mg/day, 1 times / day Route: oral Route: steady Dose: 60 mg/day, 1 times / day Sources: |
unhealthy, 11 years |
|
0.2 mg/kg/day 2 times / day steady, oral Studied dose Dose: 0.2 mg/kg/day, 2 times / day Route: oral Route: steady Dose: 0.2 mg/kg/day, 2 times / day Sources: |
unhealthy, 11.7 ± 4.4 years (range: 3‐17 years) Health Status: unhealthy Age Group: 11.7 ± 4.4 years (range: 3‐17 years) Sex: M+F Sources: |
Other AEs: Decreased appetite... |
0.7 mg/kg/day 1 times / day steady, oral Studied dose Dose: 0.7 mg/kg/day, 1 times / day Route: oral Route: steady Dose: 0.7 mg/kg/day, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: unknown Sources: |
Disc. AE: Somnolence... AEs leading to discontinuation/dose reduction: Somnolence (3.3%) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Decreased appetite | 2 patients | 0.2 mg/kg/day 2 times / day steady, oral Studied dose Dose: 0.2 mg/kg/day, 2 times / day Route: oral Route: steady Dose: 0.2 mg/kg/day, 2 times / day Sources: |
unhealthy, 11.7 ± 4.4 years (range: 3‐17 years) Health Status: unhealthy Age Group: 11.7 ± 4.4 years (range: 3‐17 years) Sex: M+F Sources: |
Somnolence | 3.3% Disc. AE |
0.7 mg/kg/day 1 times / day steady, oral Studied dose Dose: 0.7 mg/kg/day, 1 times / day Route: oral Route: steady Dose: 0.7 mg/kg/day, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: unknown Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
minor | ||||
minor | unlikely (co-administration study) Comment: The effect of coadministration of CBD on fenfluramine and norfenfluramine PK was evaluated in Study 1604. The study demonstrated that co-administration of CBD with ZX008 increased fenfluramine AUC0-t by approximately 59% and the Cmax was not changed significantly. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
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minor | unlikely (co-administration study) Comment: The effect of coadministration of CBD on fenfluramine and norfenfluramine PK was evaluated in Study 1604. The study demonstrated that co-administration of CBD with ZX008 increased fenfluramine AUC0-t by approximately 59% and the Cmax was not changed significantly. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
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no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | ||||
yes | unlikely (co-administration study) Comment: The effect of coadministration of CBD on fenfluramine and norfenfluramine PK was evaluated in Study 1604. The study demonstrated that co-administration of CBD with ZX008 increased fenfluramine AUC0-t by approximately 59% and the Cmax was not changed significantly. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
|||
yes | unlikely (co-administration study) Comment: The effect of coadministration of CBD on fenfluramine and norfenfluramine PK was evaluated in Study 1604. The study demonstrated that co-administration of CBD with ZX008 increased fenfluramine AUC0-t by approximately 59% and the Cmax was not changed significantly. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212102Orig1s000OtherR.pdf#page=38 Page: 38.0 |
PubMed
Title | Date | PubMed |
---|---|---|
A case of systemic sclerosis that developed under dexfenfluramine use. | 1999 Apr |
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Dose effect of fenfluramine-phentermine in the production of valvular heart disease. | 1999 Apr |
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Detailed examination of fenfluramine-phentermine users with valve abnormalities identified in Fargo, North Dakota. | 1999 Aug 1 |
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Echocardiographic prevalence of mitral and/or aortic regurgitation in patients exposed to either fenfluramine-phentermine combination or to dexfenfluramine. | 1999 Dec 1 |
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Serial echocardiographic and clinical evaluation of valvular regurgitation before, during, and after treatment with fenfluramine or dexfenfluramine and mazindol or phentermine. | 1999 Jul |
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Valve replacement for appetite suppressant-induced valvular heart disease. | 1999 Jun |
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Complex vascular lesions at autopsy in a patient with phentermine-fenfluramine use and rapidly progressing pulmonary hypertension. | 1999 Jun |
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Serotonergic function in cocaine addicts: prolactin responses to sequential D,L-fenfluramine challenges. | 1999 May 15 |
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Prevalence and determinants of valvulopathy in patients treated with dexfenfluramine. | 1999 Nov 23 |
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[Appetite suppressants and heart valve disorders]. | 1999 Sep |
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Beneficial effects of pharmacotherapy on weight loss, depressive symptoms, and eating patterns in obese binge eaters and non-binge eaters. | 1999 Sep |
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Dose-effect of fenfluramine use on the severity of valvular heart disease among fen-phen patients with valvulopathy. | 1999 Sep |
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The promotion effect of anorectic drugs on aflatoxin B(1)-induced hepatic preneoplastic foci. | 1999 Sep |
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[Obesity: principles of drug therapy]. | 2000 Aug |
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[Valvular regurgitation caused by anorectic agents]. | 2000 Dec |
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Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. | 2000 Dec 5 |
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[Anorectics and pulmonary hypertension]. | 2000 Feb 16 |
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Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine. | 2000 Jan |
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Dose and duration of fenfluramine-phentermine therapy impacts the risk of significant valvular heart disease. | 2000 Jul 1 |
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Anorexigens and pulmonary hypertension in the United States: results from the surveillance of North American pulmonary hypertension. | 2000 Mar |
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Effects of repeated systemic administration of d-Fenfluramine on serotonin and glutamate release in rat ventral hippocampus: comparison with methamphetamine using in vivo microdialysis. | 2001 Apr |
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The quest for biological correlates of social phobia: an interim assessment. | 2001 Apr |
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Anorectic drugs and pulmonary hypertension from the bedside to the bench. | 2001 Apr |
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Appetite suppressants and valvular heart disease. | 2001 Apr |
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Effects of dietary sucrose on hippocampal serotonin release: a microdialysis study in the freely-moving rat. | 2001 Aug |
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Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5-HT2C receptors. | 2001 Aug |
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Fenfluramine-induced pulmonary vasoconstriction: role of serotonin receptors and potassium channels. | 2001 Aug |
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Relationship between central serotonergic neurotransmission and reduction in alcohol intake by citalopram. | 2001 Aug 1 |
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The progression of fenfluramine-associated valvular heart disease assessed by echocardiography. | 2001 Feb 20 |
|
Elevations in plasmatic titers of corticosterone and aldosterone, in the absence of changes in ACTH, testosterone, or glial fibrillary acidic protein, 72 h following D,L-fenfluramine or D-fenfluramine administration to rats. | 2001 Jan-Feb |
|
Low risk of significant echocardiographic valvulopathy in patients treated with anorectic drugs. | 2001 Jul |
|
"Diet pills" and major depression in the Canadian population. | 2001 Jun |
|
Bitter pills, bad medicine. | 2001 Jun 4 |
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Long-term impairment of anterograde axonal transport along fiber projections originating in the rostral raphe nuclei after treatment with fenfluramine or methylenedioxymethamphetamine. | 2001 May |
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Serotonin transporter promoter polymorphism is associated with attenuated prolactin response to fenfluramine. | 2001 May 8 |
|
[Serotonin receptor changes in depression: evidences and limitations]. | 2001 May-Jun |
|
Fluorometric determination of DL-fenfluramine, DL-norfenfluramine and phentermine in plasma by achiral and chiral high-performance liquid chromatography. | 2001 Nov 5 |
|
High performance liquid chromatography with UV detection for the simultaneous determination of sympathomimetic amines using 4-(4,5-diphenyl-1H-imidazole-2-yl)benzoyl chloride as a label. | 2001 Oct |
|
Neuroendocrine effects of d-fenfluramine and bromocriptine following repeated smoked cocaine in humans. | 2001 Sep 1 |
|
Anorexigen-induced pulmonary hypertension and the serotonin (5-HT) hypothesis: lessons for the future in pathogenesis. | 2002 |
|
Inhibition of cocaine self-administration by fluoxetine or D-fenfluramine combined with phentermine. | 2002 Jan-Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22554283
0.12–0.90 mg/kg/day
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19298257
Rat midbrain slices were used to make intracellular recordings from dopaminergic neurons of the substantia nigra and the ventral tegmental area. Gamma-aminobutyric acid (GABA)-mediated synaptic transmission was assessed from the inhibitory postsynaptic potentials (IPSPs) mediated by GABAA and GABAB receptors. Intracellular recordings from midbrain SNpc and VTA dopaminergic neurons were performed at 33.0 +/- 0.5°C in a recording chamber submerged with aCSF flowing at a rate of 2.5–3 mL•min-1 and continuously oxygenated, on the stage of an upright (inverted) microscope (Axioscope FS, Zeiss, Gottingen, Germany), equipped for infrared video microscopy (Hamamatsu, Tokyo, Japan) in order to allow a direct visualization of the recorded cells. Neurons, selected for their morphology, were identified as dopaminergic by their electrophysiological properties such as the presence of a regular spontaneous firing activity (0.5–4 Hz), a large inward current (Ih) in response to hyperpolarizing voltages and a membrane hyperpolarization due to dopamine (10–30 mmol•L-1) application . The recording electrodes were filled with 2 mol•L-1 KCl and had a tip resistance of 30–80 MW. GABAB synaptic potentials were evoked using a bipolar tungsten stimulating electrode with a tip separation of 300–700 mkm. Representative recordings showing the effect of fenfluramine in reducing the GABAB-mediated IPSP. Such effects were evident at concentrations below 1 mmol•L-1. The amplitude of synaptic potentials was halved by fenfluramine at concentration around 10 mmol•L-1 and was completely blocked by CGP (1 mmol•L-1), a selective GABAB receptor antagonist. Fenfluramine and sibutramine induce a concentration-dependent reduction of the GABAB-mediated inhibitory postsynaptic potentials (IPSPs).
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 17:48:46 GMT 2025
by
admin
on
Mon Mar 31 17:48:46 GMT 2025
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Record UNII |
2DS058H2CF
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Record Status |
Validated (UNII)
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Record Version |
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CFR |
21 CFR 216.24
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FDA ORPHAN DRUG |
584217
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NCI_THESAURUS |
C29728
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WHO-VATC |
QA08AA02
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WHO-ATC |
A08AA02
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DEA NO. |
1670
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Code System | Code | Type | Description | ||
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3337
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D005277
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4328
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PRIMARY | RxNorm | ||
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100000081293
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5220-89-3
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SUPERSEDED | |||
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1150
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PRIMARY | |||
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3080
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C81418
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FENFLURAMINE
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2DS058H2CF
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1596
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5000
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2DS058H2CF
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CHEMBL87493
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4613
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458-24-2
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207-276-3
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SUB07561MIG
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DB00574
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25990-46-9
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SUPERSEDED | |||
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m5274
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PRIMARY | Merck Index | ||
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DTXSID4023044
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PRIMARY |
Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR | |||
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OFF-TARGET->AGONIST |
5-HT2B receptors, which were subsequently identified as the target for cardiac valvulopathy and pulmonary hypertension. Release of serotonin leads to 5-HT2B signaling.
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TRANSPORTER -> INHIBITOR |
IC50
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TARGET -> AGONIST |
STIMULATES THE RELEASE OF SEROTONIN RESULTS IN APPETITE SUPPRESSION; LEAD TO 6-16 FOLD INCREASE IN SEROTONIN IN THE HYPOTHALMUS
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> SUBSTRATE |
STIMULATES SEROTONIN RELEASE.
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
Percent of dose excreted in urine as metabolite.
AMOUNT EXCRETED
URINE
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METABOLITE TOXIC -> PARENT |
Responsible for
MAJOR
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METABOLITE -> PARENT |
Metabolite to parent drug ratio in non-uraemic human plasma.
A positive correlation exists between plasma norfenfluramine levels and weight loss in man.
METABOLITE TO PARENT DRUG RATIO
PLASMA; URINE
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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