A histamine H1 receptor antagonist
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Labeled Version(s)
33711Fenspiride-d5
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Fenspiride (hydrochloride)

Item No. 25512

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one, monohydrochloride
CAS Number
5053-08-7
Synonyms
  • Decaspiride
Molecular Formula
C15H20N2O2 • HCl
Formula Weight
296.8
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: slightly solublePBS (pH 7.2): 10 mg/ml
λmax
238, 288 nm
SMILES
O=C1NCC2(CCN(CCC3=CC=CC=C3)CC2)O1.Cl
InChi Code
InChI=1S/C15H20N2O2.ClH/c18-14-16-12-15(19-14)7-10-17(11-8-15)9-6-13-4-2-1-3-5-13;/h1-5H,6-12H2,(H,16,18);1H
InChi Key
FIKFLLIUPUVONI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 g

    $62

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    10 g

    $107

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    25 g

    $238

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    50 g

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    Product Description

    Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID).1,2 It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer).3 It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol (Item No. 15592) and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg/ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg/ml, reduces cough induced by citric acid in a guinea pig model of cough.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rognoni, F., Marchini, F., Piacenza, G., et al. Effect of 8-N-phenethyl-1-oxa-2-oxo-3,8-diazaspiro(4,5)decane hydrochloride (decaspiride) on histamine receptors. Boll. Chim. Farm. 117(7), 397-401 (1978).

    2. Laude, E.A., Bee, D., Crambes, O., et al. Antitussive and antibronchoconstriction actions of fenspiride in guinea-pigs. Eur. Respir. J. 8(10), 1699-1704 (1995).

    3. Cortijo, J., Naline, E., Ortiz, J.L., et al. Effects of fenspiride on human bronchial cyclic nucleotide phosphodiesterase isoenzymes: Functional and biochemical study. Eur. J. Pharmacol. 341(1), 79-86 (1998).