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5053-06-5

5053-06-5 structure
5053-06-5 structure
  • Name: Fenspiride
  • Chemical Name: 8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one
  • CAS Number: 5053-06-5
  • Molecular Formula: C15H20N2O2
  • Molecular Weight: 260.332
  • Catalog: API Respiratory medication Asthma
  • Create Date: 2018-09-01 17:35:59
  • Modify Date: 2024-01-11 17:58:44
  • 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].
Name 8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one
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]
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].
Related Catalog
Target

-log IC50: 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].
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.
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.
Density 1.2±0.1 g/cm3
Boiling Point 408.3±55.0 °C at 760 mmHg
Molecular Formula C15H20N2O2
Molecular Weight 260.332
Flash Point 200.7±31.5 °C
Exact Mass 260.152466
PSA 41.57000
LogP 1.91
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.609

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 DATA

ACUTE 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
HS Code 2934999090
Precursor  4

DownStream  0

HS Code 2934999090
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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