[CAS NO. 5053-08-7] Fenspiridehydrochloride
PRODUCTS SPECIFICATIONS [5053-08-7]
DESCRIPTION [5053-08-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 296.79 |
| Molecular Formula | C15H21ClN2O2 |
| SMILES | O=C1OC2(CCN(CCC3=CC=CC=C3)CC2)CN1.[H]Cl |
Summary
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 IC 50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases [1] [2] [3] .
IC50 & Target
-log IC 50 : 3.44 (PDE3); 4.16 (PDE4); approximately 3.8 (PDE5) [2]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum and in the bronchoalveolar lavage fluid (BALF) of the model of endotoxemia
[3]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Lipopolysaccharide-treated Male Dunkin-Hartley guinea-pigs weighing 400-600 g [3] |
| Dosage: | 60 mg/kg |
| Administration: | Orally for 3 days; pretreated |
| 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 B 2 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 168.47 mM ; Need ultrasonic)
DMSO : 33.33 mg/mL ( 112.30 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3694 mL | 16.8469 mL | 33.6939 mL |
| 5 mM | 0.6739 mL | 3.3694 mL | 6.7388 mL |
| 10 mM | 0.3369 mL | 1.6847 mL | 3.3694 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 120 mg/mL (404.33 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.75 mg/mL (9.27 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.75 mg/mL (9.27 mM); Clear solution
References
- [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.
- [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.
- [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.
Synonyms