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Fenspiride hydrochloride

Catalog No. T0383 CAS 5053-08-7

Synonyms: Phosphodiesterase (PDE), Inhibitor, Fenspiride HCl, Pneumorel, Fluiden, orally active, Decaspiride, Fenspiride, non-steroidal, Histamine Receptor, antiinflammatory, inhibit, guinea-pigs, Fenspiride hydrochloride, respiratory diseases

Fenspiride, an oxazolidinone spiro compound, is a drug used in the therapy of certain respiratory diseases. It is approved for use in Russia for the therapy of chronic and acute inflammatory diseases of ENT organs and the respiratory tract (like sinusitis, tracheobronchitis, otitis, laryngitis, and rhinopharyngitis), and for maintenance therapy of asthma.

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Fenspiride hydrochloride, CAS 5053-08-7

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Fenspiride, an oxazolidinone spiro compound, is a drug used in the therapy of certain respiratory diseases. It is approved for use in Russia for the therapy of chronic and acute inflammatory diseases of ENT organs and the respiratory tract (like sinusitis, tracheobronchitis, otitis, laryngitis, and rhinopharyngitis), and for maintenance therapy of asthma.
Targets&IC50	PDE3:3.44(pIC50), PDE4:4.16(pIC50)
In vitro	Fenspiride induces potentiation of the effects of isoprenaline and sodium nitroprusside with logEC50 of 4.1 and 3.5, respectively, in human isolated bronchi. [1]
In vivo	Fenspiride, an antiinflammatory drug with low anti-cyclooxygenase activity, administered orally at 60-200 mg/kg inhibits neutrophil migration into peritoneal and air pouches cavities as well as exudation into peritoneal cavities induced by endotoxin but not induced by carrageenin in the rat. Fenspiride (200 mg/kg) inhibits the release of tumour necrosis factor by stimulated macrophages in a dose-dependent manner in the rat. [2] Fenspiride (Topically applied) is found to inhibit the development of sclerotic lesions in myringotomized rats, whereas intraperitoneal injections are ineffective. [3] Fenspiride (60 mg/kg) significantly reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum (4.2 ng/mL vs. 2.3 ng/mL) and in the bronchoalveolar lavage fluid (55.7 ng/mL vs. 19.7 ng/mL) of guinea-pigs with endotoxemia. Fenspiride (60 mg/kg) also significantly reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages, defined as their enhanced release of arachidonic acid metabolites as compared to cells from untreated controls upon stimulation with N-formyl-methionyl-phenylalanine. Fenspiride (60 mg/kg) reduces the increased serum concentrations of extracellular type II phospholipase A2, the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide in guinea-pigs with endotoxemia. [4]

Synonyms	Phosphodiesterase (PDE), Inhibitor, Fenspiride HCl, Pneumorel, Fluiden, orally active, Decaspiride, Fenspiride, non-steroidal, Histamine Receptor, antiinflammatory, inhibit, guinea-pigs, Fenspiride hydrochloride, respiratory diseases
Molecular Weight	296.8
Formula	C15H21ClN2O2
CAS No.	5053-08-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 9 mg/mL (30.32 mM)

Ethanol: <1 mg/mL

H2O: 54 mg/mL (181.9 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature

1. Cortijo J, et al. Eur J Pharmacol, 1998, 341(1), 79-86. 2. Cunha FQ, et al. Eur J Pharmacol, 1993, 238(1), 47-52. 3. Mattsson C, et al. Eur Arch Otorhinolaryngol, 1997, 254(9-10), 425-429. 4. De Castro CM, et al. Eur J Pharmacol, 1995, 294(2-3), 669-676.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library GPCR Compound Library Anti-Cardiovascular Disease Compound Library Histamine & Melatonin Receptor-Targeted Compound Library Endocrinology-Hormone Compound Library Inhibitor Library Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library

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Related compounds with same targets

Quinine HCl Isorhoifolin Clenbuterol Pardoprunox M443 D2343 (±)-Levomepromazine-d6 ZK-90055 hydrochloride

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