Introduction：Basic information about CAS 5053-06-5|Fenspiride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Fenspiride |
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| CAS Number | 5053-06-5 | Molecular Weight | 260.332 |
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| Density | 1.2±0.1 g/cm3 | Boiling Point | 408.3±55.0 °C at 760 mmHg |
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| Molecular Formula | C15H20N2O2 | Melting Point | / |
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| MSDS | / | Flash Point | 200.7±31.5 °C |
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Names
| Name | 8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one |
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| Synonym | More Synonyms |
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Fenspiride BiologicalActivity
| Description | 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]. |
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| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorSignaling Pathways >>Metabolic Enzyme/Protease >>Phosphodiesterase (PDE)Research Areas >>Inflammation/ImmunologySignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
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| Target | -log IC50: 3.44 (PDE3); 4.16 (PDE4); approximately 3.8 (PDE5)[2] |
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| 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]. |
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| 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: 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 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. |
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| 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. |
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Chemical & Physical Properties
| Density | 1.2±0.1 g/cm3 |
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| Boiling Point | 408.3±55.0 °C at 760 mmHg |
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| Molecular Formula | C15H20N2O2 |
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| Molecular Weight | 260.332 |
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| Flash Point | 200.7±31.5 °C |
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| Exact Mass | 260.152466 |
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| PSA | 41.57000 |
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| LogP | 1.91 |
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| Vapour Pressure | 0.0±1.0 mmHg at 25°C |
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| Index of Refraction | 1.609 |
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| InChIKey | FVNFBBAOMBJTST-UHFFFAOYSA-N |
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| SMILES | O=C1NCC2(CCN(CCc3ccccc3)CC2)O1 |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- RO0373000
- CHEMICAL NAME :
- 1-Oxa-3,8-diazaspiro(4.5)decan-2-one, 8-phenethyl-
- CAS REGISTRY NUMBER :
- 5053-06-5
- LAST UPDATED :
- 199712
- DATA ITEMS CITED :
- 1
- MOLECULAR FORMULA :
- C15-H20-N2-O2
- MOLECULAR WEIGHT :
- 260.37
- WISWESSER LINE NOTATION :
- T6N CXTJ A2R& C-& DT5MVOX EHJ
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 230 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- CHTPBA Chimica Therapeutica. (Paris, France) V.1-8, 1965-73. For publisher information, see EJMCA5. Volume(issue)/page/year: 4,185,1969
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Safety Information
Customs
| HS Code | 2934999090 |
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| Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| 8-phenethyl-1-oxa-3,8-diaza-spiro[4.5]decan-2-one |
| 1-Oxa-3,8-diazaspiro[4.5]decan-2-one, 8-(2-phenylethyl)- |
| Fluiden |
| Fenspiridum [INN-Latin] |
| Fenspiride [INN] |
| EINECS 225-751-3 |
| Viarespan |
| 1-Oxa-3,8-diazaspiro[4.5]dec-2-en-2-ol, 8-(2-phenylethyl)- |
| 8-(2-Phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one |
| Fenspiride |
| Respiride |
| Fenspirida [INN-Spanish] |
