Flibanserin salicylate
Based on 2 publication(s) in Google Scholar
Flibanserin (BIMT-17) salicylate is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin salicylate binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin salicylate shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research-.
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- CAS No.: 1231148-54-1
- Formule: C27H27F3N4O4
- Masse moléculaire:528.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Flibanserin salicylate
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Activité biologique
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5-HT1A Receptor 1 nM (Ki) |
5-HT2A Receptor 49 nM (Ki) |
dopamine D4 receptors 4-24 nM (Ki) |
Flibanserin (0.01-100 μM; 72 h) salicylate can transform into two degradation products DP1 and DP2 with no toxicity potential after oxidative degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NHSF cell lin
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Concentration:0.01, 0.1, 1, 10, 100 μM
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Incubation Time:72 hours
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Result:Resulted cell viability reached to 97.91% (DP1) and 96.73% (DP2) at 0.01 μM.
Showed non-toxic up to 100 μM (IC50 >100 μM).
Flibanserin (15, 45 mg/kg; p.o.; twice a day; 22 d) salicylate preferentially activates the brain regions belonging to the mesolimbic dopaminergic pathway and hypothalamic structures involved in the integration of sexual cues related to sexual motivation[3].
Flibanserin (5, 10, 25, and 50 mg/kg; s.c.; single dose) salicylate has anxiolytic effects without locomotor side effects in rat ultrasonic vocalization model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long Evans female rats (225-250 g)[3]
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Dosage:15 mg/kg; 45 mg/kg
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Administration:Oral gavage; twice a day for 22 days
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Result:Increased the density of activated catecholaminergic neurons in the ventral tegmental area but not in the locus coeruleus.
Increased Fos expression in the medial preoptic area and arcuate nucleus of the hypothalamus, ventral tegmental area, locus coeruleus, and lateral paragigantocellular nucleus with chronic 22-day treatment.
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Animal Model:Rat pup ultrasonic vocalization model of anxiety[4]
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Dosage:5, 10, 25, and 50 mg/kg
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Administration:Subcutaneous injection
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Result:Reduced ultrasonic vocalizations in rat pups.
Showed effective within 30 min and has no severe locomotor side effects at active doses.
Chemical Information
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CAS No. 1231148-54-1
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Masse moléculaire 528.52
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Formule C27H27F3N4O4
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SMILES
O=C1NC2=C(N1CCN3CCN(CC3)C4=CC=CC(C(F)(F)F)=C4)C=CC=C2.OC(C5=CC=CC=C5O)=O
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Synonyms
BIMT-17 salicylate; BIMT-17BS salicylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Mol Pharmacol
2023 Nov;104(5):230-238. PMID: 37567783 -
Pureté et documentation
Références
[2]. Invernizzi RW, et al. 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. [Content Brief]
[3]. Gelez H, et al. Brain neuronal activation induced by flibanserin treatment in female rats. Psychopharmacology (Berl). 2013 Dec;230(4):639-52. [Content Brief]
[4]. Podhorna J, et al. Flibanserin has anxiolytic effects without locomotor side effects in the infant rat ultrasonic vocalization model of anxiety. Br J Pharmacol. 2000 Jun;130(4):739-46. [Content Brief]
[5]. Gelman F, et al. Flibanserin for hypoactive sexual desire disorder: place in therapy. Ther Adv Chronic Dis. 2017 Jan;8(1):16-25. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Flibanserin salicylate Related Classifications
HY-A0095C Related Classifications
Powered by Bioz
- Flibanserin
- 1231148-54-1
- BIMT-17
- BIMT-17BS
- BIMT17
- BIMT 17
- 5-HT Receptor
- Dopamine Receptor
- affinity
- neurotransmitter
- hypoactive
- sexual
- desire
- disorder
- antidepressant
- antianxiety
- hypoactive sexual desire disorder
- HSDD
- orally active
- DP1
- DP2
- no cytotoxicity
- NHSF cell line
- prefrontal cortex
- hippocampus
- midbrain
- Inhibitor
- inhibitor
- inhibit