| Bioactivity | 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[1][2][3]. |
| Target | -log IC50: 3.44 (PDE3); 4.16 (PDE4); approximately 3.8 (PDE5) |
| Invitro | 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]. |
| 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]. Animal Model: |
| Name | Fenspiride |
| CAS | 5053-06-5 |
| Formula | C15H20N2O2 |
| Molar Mass | 260.33 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |