CAS 5053-08-7|fenspiride hydrochloride

Introduction：Basic information about CAS 5053-08-7|fenspiride hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. fenspiride hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Articles3
7. Synonyms

Common Name	fenspiride hydrochloride
CAS Number	5053-08-7	Molecular Weight	296.79200
Density	1.19g/cm3	Boiling Point	474.3ºC at 760mmHg
Molecular Formula	C₁₅H₂₁ClN₂O₂	Melting Point	235-238ºC (dec.)
MSDS	ChineseUSA	Flash Point	240.6ºC
Symbol	GHS07	Signal Word	Warning

Names

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

fenspiride hydrochloride BiologicalActivity

Description	Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist.IC50 value:Target: Adrenergic receptor; H1 receptorFenspiride hydrochloride is a bronchodilator with anti-inflammatory properties. Fenspiride hydrochloride inhibits mucus secretion and reduces the release of tachykinins at a prejunctional level. Fenspiride hydrochloride also may be an antagonist at α adrenergic and H1 histamine receptors.
Related Catalog	Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorSignaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorNatural Products >>AlkaloidResearch Areas >>Inflammation/Immunology
References	[1]. Lebedenko AA, Mal'tsev SV. .[The efficacy of application of fenspiride (erespal) for the treatment of exacerbation of bronchial asthma in children.] Vestn Otorinolaringol. 2011;(4):66-67. [2]. Khawaja AM, Liu YC, Rogers DF. et al.Effect of fenspiride, a non-steroidal antiinflammatory agent, on neurogenic mucus secretion in ferret trachea in vitro. Pulm Pharmacol Ther. 1999;12(6):363-8. [3]. Zielnik-Jurkiewicz B, Jurkiewicz D. et al. Usefulness of fenspiride in the treatment of acute otitis media in children. Pol Merkur Lekarski. 2005 Jun;18(108):624-8. [4]. Bee D, Laude EA, Emery CJ, Howard P. Effect of fenspiride on pulmonary function in the rat and guinea pig. Clin Sci (Lond). 1995 Mar;88(3):325-30. [5]. Fenspiride

Description

Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist.IC50 value:Target: Adrenergic receptor; H1 receptorFenspiride hydrochloride is a bronchodilator with anti-inflammatory properties. Fenspiride hydrochloride inhibits mucus secretion and reduces the release of tachykinins at a prejunctional level. Fenspiride hydrochloride also may be an antagonist at α adrenergic and H1 histamine receptors.

Related Catalog

Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorSignaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorNatural Products >>AlkaloidResearch Areas >>Inflammation/Immunology

References

[1]. Lebedenko AA, Mal'tsev SV. .[The efficacy of application of fenspiride (erespal) for the treatment of exacerbation of bronchial asthma in children.] Vestn Otorinolaringol. 2011;(4):66-67.

[2]. Khawaja AM, Liu YC, Rogers DF. et al.Effect of fenspiride, a non-steroidal antiinflammatory agent, on neurogenic mucus secretion in ferret trachea in vitro. Pulm Pharmacol Ther. 1999;12(6):363-8.

[3]. Zielnik-Jurkiewicz B, Jurkiewicz D. et al. Usefulness of fenspiride in the treatment of acute otitis media in children. Pol Merkur Lekarski. 2005 Jun;18(108):624-8.

[4]. Bee D, Laude EA, Emery CJ, Howard P. Effect of fenspiride on pulmonary function in the rat and guinea pig. Clin Sci (Lond). 1995 Mar;88(3):325-30.

[5]. Fenspiride

Chemical & Physical Properties

Density	1.19g/cm3
Boiling Point	474.3ºC at 760mmHg
Melting Point	235-238ºC (dec.)
Molecular Formula	C₁₅H₂₁ClN₂O₂
Molecular Weight	296.79200
Flash Point	240.6ºC
Exact Mass	296.12900
PSA	41.57000
LogP	2.87220
Appearance of Characters	powder \| white
InChIKey	FIKFLLIUPUVONI-UHFFFAOYSA-N
SMILES	Cl.O=C1NCC2(CCN(CCc3ccccc3)CC2)O1
Storage condition	Refrigerator

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RO0375000

CHEMICAL NAME :: 1-Oxa-3,8-diazaspiro(4.5)decan-2-one, 8-phenethyl-, monohydrochloride

CAS REGISTRY NUMBER :: 5053-08-7

LAST UPDATED :: 199012

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C15-H20-N2-O2.Cl-H

MOLECULAR WEIGHT :: 296.83

WISWESSER LINE NOTATION :: T6N CXTJ A2R& C-& DT5MVOX EHJ &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 437 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle weakness Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 19,1263,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 122 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 193,111,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 250 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 193,111,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 230 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle weakness Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 19,1263,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 106 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle weakness Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 19,1263,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 74 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Behavioral - aggression

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 117,343,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 260 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 193,111,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 210 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 193,111,1971

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H312-H332
Precautionary Statements	P280
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes	Xn
Risk Phrases	20/21/22
Safety Phrases	36
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	RO0375000

Articles3

Fenspiride and membrane transduction signals in rat alveolar macrophages.

Biochem. Pharmacol. 54 , 293, (1997)

Fenspiride inhibits the calcium signal evoked by the inflammatory peptide formyl-Met-Leu-Phe (fMLP) in peritoneal macrophages, but at concentrations (approximately 1 mM) far above the therapeutic rang...

Effects of fenspiride on human bronchial cyclic nucleotide phosphodiesterase isoenzymes: functional and biochemical study.

Eur. J. Pharmacol. 341 , 79, (1998)

We have investigated the role of human bronchial cyclic nucleotide phosphodiesterases in the effects of fenspiride, a drug endowed with bronchodilator and anti-inflammatory properties. Functional stud...

Fenspiride inhibits histamine-induced responses in a lung epithelial cell line.

Eur. J. Pharmacol. 348 , 297-304, (1998)

Using the human lung epithelial WI26VA4 cell line, we investigated the capacity of fenspiride, an anti-inflammatory drug with anti-bronchoconstrictor properties, to interfere with histamine-induced in...

Synonyms

Fenspiride (Hydrochloride)

Fenspiride HCl

NDR-5998A

Depiride

Fluiden

Pneumorel

Tegencia hydrochloride

Viarespan hydrochloride

Espiran

8-(2-Phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one hydrochloride

fenspiride hydrochloride

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