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MedKoo Cat#: 464334 | Name: Fenspiride-d5
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). 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). 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 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.

Chemical Structure

Fenspiride-d5
Fenspiride-d5
CAS#1246911-67-0

Theoretical Analysis

MedKoo Cat#: 464334

Name: Fenspiride-d5

CAS#: 1246911-67-0

Chemical Formula: C15H15D5N2O2

Exact Mass: 265.1839

Molecular Weight: 265.37

Elemental Analysis: C, 67.89; H, 9.49; N, 10.56; O, 12.06

Price and Availability

Size Price Availability Quantity
1mg USD 650.00 2 Weeks
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Synonym
Fenspiride d5; Fenspiride-d5; Decaspiride d5; Decaspiride-d5;
IUPAC/Chemical Name
8-(phenethyl-d5)-1-oxa-3,8-diazaspiro[4.5]decan-2-one
InChi Key
FVNFBBAOMBJTST-RALIUCGRSA-N
InChi Code
InChI=1S/C15H20N2O2/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)/i1D,2D,3D,4D,5D
SMILES Code
[2H]C1=C(C([2H])=C(C([2H])=C1CCN2CCC3(CC2)OC(NC3)=O)[2H])[2H]
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 265.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Kalekin RA, Orlova AM, Savchuk SA, Barsegyan SS. Izuchenie fenspirida dlia tseleĭ i zadach khimiko-toksikologicheskogo issledovaniia [The study of fenspiride: goals and objectives for chemical and toxicological studies]. Sud Med Ekspert. 2019;62(4):37-41. Russian. doi: 10.17116/sudmed20196204137. PMID: 31407704. 2: Matuszewska A, Nowak B, Jędrzejuk D, Landwójtowicz M, Bolanowski M, Dziewiszek W, Merwid-Ląd A, Szeląg E, Zduniak K, Kwiatkowska J, Szeląg A. 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. doi: 10.17219/acem/93729. PMID: 30843675. 3: Dang YW, Lin P, Liu LM, He RQ, Zhang LJ, Peng ZG, Li XJ, Chen G. In silico analysis of the potential mechanism of telocinobufagin on breast cancer MCF-7 cells. Pathol Res Pract. 2018 May;214(5):631-643. doi: 10.1016/j.prp.2018.03.029. Epub 2018 Apr 5. PMID: 29656985. 4: Cioroiu BI, Caba IC, Prisăcaru I, Cioroiu ME, Lazar MI, Niculaua M. New approach for determination of the degradation products of fenspiride hydrochloride found in oral liquid formulations. Biomed Chromatogr. 2018 May;32(5):e4176. doi: 10.1002/bmc.4176. Epub 2018 Jan 22. PMID: 29265479. 5: Ryabova MA. Fenspirid v kompleksnom lechenii obostreniia khronicheskogo laringita [The use of fenspiride for the combined treatment of exacerbation of chronic laryngitis]. Vestn Otorinolaringol. 2017;82(6):66-69. Russian. doi: 10.17116/otorino201782666-69. PMID: 29260786. 6: Zhdan VN, Potyazhenko MМ, Khaymenova GS, Lyulka NN, Dubrovinskaya TV, Ivanitsky IV. Intensifying approach to the therapy of patients with constellation of the diseases: chronic obstructive pulmonary disease and osteoarthritis. Wiad Lek. 2017;70(3 pt 2):578-580. PMID: 28713086. 7: Хайменова ГС, Шилкина ЛН, Бабанина МЮ, Волченко ГВ, Ткаченко МВ, Ждан ВН. [Evaluation of therapy efficiency in patients with combined course of copd and osteoarthritis]. Wiad Lek. 2016;69(2 Pt 2):214-8. Russian. PMID: 27487536. 8: Fedin AV. [The assessment of the clinical effectiveness of fenspiride for the treatment of acute obstruction of the Eustachian tube]. Vestn Otorinolaringol. 2015;(1):70-71. Russian. doi: 10.17116/otorino201580170-71. PMID: 25909681. 9: Mel'chinskiĭ AN, Vasilenko DIu, Kiseleva GV. [The assessment of the effectiveness of fenspiride (erespal) for the combined treatment of the patients presenting with exudative otitis media]. Vestn Otorinolaringol. 2013;(6):70-1. Russian. PMID: 24429863. 10: Kuzubova NA, Lebedeva ES, Fedin AN, Dvorakovskaya IV, Preobrazhenskaya TN, Titova ON. Effect of fenspiride on bronchial smooth muscle of rats with chronic obstructive pulmonary disease. J Smooth Muscle Res. 2013;49:46-54. doi: 10.1540/jsmr.49.46. PMID: 24133694; PMCID: PMC5137255. 11: Kuzubova NA, Lebedeva ES, Fedin AN, Dvorakovskaya IV, Titova ON. Protective effect of fenspiride on the bronchi in rats with chronic obstructive pulmonary disease. Bull Exp Biol Med. 2013 Jun;155(2):214-7. doi: 10.1007/s10517-013-2116-2. PMID: 24130993. 12: Lebedenko AA, Mal'tsev SV. Éffektivnost' ispol'zovaniia fenspirida (érespal) pri obostrenii bronkhial'noĭ astmy u deteĭ [The efficacy of application of fenspiride (erespal) for the treatment of exacerbation of bronchial asthma in children]. Vestn Otorinolaringol. 2011;(4):66-7. Russian. PMID: 21983674. 13: Medvedovici A, Udrescu S, Albu F, Tache F, David V. Large-volume injection of sample diluents not miscible with the mobile phase as an alternative approach in sample preparation for bioanalysis: an application for fenspiride bioequivalence. Bioanalysis. 2011 Sep;3(17):1935-47. doi: 10.4155/bio.11.148. PMID: 21899503. 14: Riabova MA. [The use of eurespal for the treatment of chronic laryngitis]. Vestn Otorinolaringol. 2011;(1):70-3. Russian. PMID: 21378745. 15: [The estimation of clinical efficacy of eurespal in the postoperative period following surgical intervention on paranasal sinuses]. Vestn Otorinolaringol. 2011;(6):103-6. Russian. PMID: 22433707. 16: Poliakova SD, Nekrasova EA. [Efficiency of combination therapy for acute otitis media]. Vestn Otorinolaringol. 2010;(5):47-50. Russian. PMID: 21191354. 17: Kim IA, Nosulia EV. [Pathogenetic correction of postoperative inflammation in modern rhinosurgery]. Vestn Otorinolaringol. 2010;(4):78-81. Russian. PMID: 21105352. 18: Chernenkov IuV, Gumeniuk OI, Popova IIu, Raskina EE, Doblo NN. [Experience in using erespal in the treatment of acute respiratory diseases in children in outpatient practice]. Vestn Otorinolaringol. 2010;(1):78-9. Russian. PMID: 20524264. 19: Toropova LA, Zhuĭkova TV, Nikolayeva AI, Maĭorova IuS. [Pathogenetic therapy for inflammatory diseases of the middle ear]. Vestn Otorinolaringol. 2009;(6):77-80. Russian. PMID: 20095104. 20: Baryshevskaia LA, Velikanov AK, Sedykh MI. [Experience with fenspiride in a rhinosurgeon's practice]. Vestn Otorinolaringol. 2009;(2):46-8. Russian. PMID: 19491799.