Fenspiride
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
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- CAS No.: 5053-06-5
- Formule: C15H20N2O2
- Masse moléculaire:260.33
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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
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Activité biologique
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H1 Receptor |
PDE3 |
PDE4 |
PDE5 |
Fenspiride (around 100 μM) inhibits histamine-induced contraction of isolated guinea pig trachea[2].
Fenspiride (≤1000 μM) produces less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages[3].
Fenspiride (60 mg/kg; p.o. for 3 days) reduces the increased serum concentrations of extracellular type II phospholipase A 2, the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lipopolysaccharide-treated Male Dunkin-Hartley guinea-pigs weighing 400-600 g[3]
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Dosage:60 mg/kg
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Administration:orally for 3 days; pretreated
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Result:Reduced the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum (4.2 vs. 2.3 ng/ml) and in the BALF (55.7 vs. 19.7 ng/ml).
Reduced the lipopolysaccharide-induced primed stimulation of alveolar macrophages, (1551.5 vs 771.5 pg/μg protein, P<0.05 for thromboxane B2 and 12.6 vs. 3.6 pg/μg protein, P<0.05 for leukotriene C4).
Reduced the increased serum concentrations of extracellular type II phospholipase A 2 (3.9 vs. 1.2 nmol/ml per min), the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide.
Chemical Information
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CAS No. 5053-06-5
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Appearance Solid
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Masse moléculaire 260.33
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Formule C15H20N2O2
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Color White to off-white
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SMILES
O=C1OC2(CCN(CCC3=CC=CC=C3)CC2)CN1
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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.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Matuszewska A, et al. Long-term administration of fenspiride has no negative impact on bone mineral density and bone turnover in young growing rats. Adv Clin Exp Med. 2019 Jun;28(6):771-776. [Content Brief]
[2]. Cortijo J, et al. Effects of fenspiride on human bronchial cyclic nucleotide phosphodiesterase isoenzymes: functional and biochemical study. Eur J Pharmacol. 1998 Jan 2;341(1):79-86. [Content Brief]
[3]. De Castro CM, et al. Fenspiride: an anti-inflammatory drug with potential benefits in the treatment of endotoxemia. Eur J Pharmacol. 1995 Dec 29;294(2-3):669-76. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fenspiride Related Classifications
HY-A0027A Related Classifications
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