Fenspiride

Modify Date: 2025-08-25 12:23:46

Fenspiride structure	Common Name	Fenspiride
	CAS Number	5053-06-5	Molecular Weight	260.332
	Density	1.2±0.1 g/cm3	Boiling Point	408.3±55.0 °C at 760 mmHg
	Molecular Formula	C₁₅H₂₀N₂O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	200.7±31.5 °C

Use of 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[1][2][3].

Name	8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one
Synonym	More Synonyms

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	Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
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

Triphosgene

CAS#:32315-10-9

4-(aminomethyl)...

CAS#:23808-42-6

~69%

Fenspiride

CAS#:5053-06-5

Literature: Somanathan; Rivero; Nunez; Hellberg Synthetic Communications, 1994 , vol. 24, # 10 p. 1483 - 1487

1-Phenethyl-4-p...

CAS#:39742-60-4

Fenspiride

CAS#:5053-06-5

Literature: Synthetic Communications, , vol. 24, # 10 p. 1483 - 1487

1-(2-phenethyl)...

CAS#:156215-50-8

Fenspiride

CAS#:5053-06-5

Literature: Synthetic Communications, , vol. 24, # 10 p. 1483 - 1487

4-(aminomethyl)...

CAS#:23808-42-6

Ethyl carbonate

CAS#:105-58-8

Fenspiride

CAS#:5053-06-5

Literature: Chimica Therapeutica, , vol. 4, p. 185 - 194

Precursor 4
CAS#:32315-10-9 Triphosgene CAS#:23808-42-6 4-(aminomethyl)... CAS#:39742-60-4 1-Phenethyl-4-p... CAS#:105-58-8 Ethyl carbonate
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%

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]

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