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Fenspiride HCl

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Chemical Structure| 5053-08-7 同义名 : 盐酸芬司必利;芬司必利盐酸盐;盐酸芬司匹利 ;Fenspiride (hydrochloride);Decaspiride;Fenspiride hydrochloride
CAS号 : 5053-08-7
货号 : A188332
分子式 : C15H21ClN2O2
纯度 : 98%
分子量 : 296.792
MDL号 : MFCD00133315
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(117.93 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(168.47 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 120 mg/mL clear

生物活性
靶点

  • PDE4

    PDE4, pIC50:4.16

  • PDE3

    PDE3, pIC50:3.44
描述 Fenspiride hydrochloride is used in treating chronic inflammatory diseases, most commonly as a liquid oral solution[3]. Fenspiride is an antagonist of H1-histamine receptors that is used to treat acute and chronic respiratory tract infections and otitis media in children and adolescents. Long-term administration of fenspiride has no negative impact on BMD(bone mineral density) and bone metabolism in young growing rats[4]. Moreover, Fenspiride administration to rats during the acute stage of COPD(Chronic obstructive pulmonary disease) (15 days of NO2 exposure) prevented the bronchial constriction induced by NO2[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.37mL

0.67mL

0.34mL

16.85mL

3.37mL

1.68mL

33.69mL

6.74mL

3.37mL
参考文献

[1]Cortijo J, Naline E, 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.

[2]Cunha FQ, Boukili MA, et al. Blockade by fenspiride of endotoxin-induced neutrophil migration in the rat. Eur J Pharmacol. 1993 Jul 6;238(1):47-52.

[3]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.

[4]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.

[5]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.