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Stepronin

(Synonyms: Prostenoglycine; TTPG; Tiase) 目录号 : GC68477

Stepronin (Prostenoglycine) 是一种口服有效的祛痰剂 (吸入给药优于口服给药)。Stepronin 在体外通过减少上皮细胞的 Cl- 分泌和粘膜下腺体的粘液糖蛋白分泌来抑制气道分泌。

Stepronin Chemical Structure

Cas No.:72324-18-6

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产品描述

Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands[1].

Stepronin (0.1-100 µM; 20 min) induces significant reductions in ISOP(Isoproterenol)-evoked SCC (short circuit current) value in a dose-dependent manner in canine tracheal epithelium[1].
Stepronin (10-100 µM; 20 min) significantly inhibits the basal secretion and ISOP-evoked PD (potential difference) value in a dose-dependent manner in canine tracheal epithelium[1].
Stepronin (100 µM; 20 min) significantly inhibits ISOP-induced [3H]-glycoconjugate secretion in submucosal glands[1].

Cell Viability Assay[1]

Cell Line: Canine tracheal epithelium (from adult and 10 to 25 kg-weight mongrel dogs of both sexes)
Concentration: 0.1-100 µM; 10-100 µM
Incubation Time: 20 min (pre-treat)
Result: Significantly inhibited ISOP-induced SCC and PD values, as well as basal secretion.

Cell Viability Assay[1]

Cell Line: Submucosal glands (from adult and 10 to 25 kg-weight mongrel dogs of both sexes)
Concentration: 100 µM
Incubation Time: 20 min (pre-treat)
Result: Significantly inhibited ISOP- induced [3H]-glycoconjugate secretion.

[1]. Yamada K, et al. An expectorant, stepronin, reduces airway secretion in vitro. Respiration. 1994;61(1):42-7.

Chemical Properties

Cas No. 72324-18-6 SDF Download SDF
别名 Prostenoglycine; TTPG; Tiase
分子式 C10H11NO4S2 分子量 273.33
溶解度 DMSO : ≥ 250 mg/mL (914.65 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.6586 mL 18.2929 mL 36.5858 mL
5 mM 0.7317 mL 3.6586 mL 7.3172 mL
10 mM 0.3659 mL 1.8293 mL 3.6586 mL
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Research Update

An expectorant, Stepronin, reduces airway secretion in vitro

Respiration 1994;61(1):42-7.PMID:8177972DOI:10.1159/000196302.

Stepronin (SPN) is clinically used as an expectorant, and thenoic acid (TA) is its metabolite. We examined the effects of these drugs on the bioelectric parameters [potential difference (PD), short circuit current (SCC), conductance (G)] of the posterior epithelial membrane of canine trachea and on those of the mucus glycoprotein secretion from feline tracheal isolated glands. PD and SCC were obtained using an Ussing chamber and G was calculated as the ratio SCC/PD. Neither SPN nor TA significantly altered the baseline values of PD and SCC. However, in the mucosal solution, both SPN and TA significantly inhibited PD and SCC evoked by isoproterenol (ISOP), whereas G remained unchanged. Amirolide did not alter the inhibitory action of SPN and TA. Mucus glycoprotein secretion from isolated glands was estimated by measuring trichloride acetic acid-precipitable [3H]-glycoconjugates. SPN and TA significantly reduced mucus glycoprotein secretion. Further, when stimulated by methacholine, these agents significantly inhibited mucus glycoprotein secretion from isolated glands. These findings suggest that SPN inhibits airway secretion in vitro by both decreasing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands.

Accelerated cell-mediated broncho-obstructive reaction to inhaled Stepronin: a case report

Allergy 1996 Apr;51(4):269-71.PMID:8792926DOI:10.1111/j.1398-9995.1996.tb04605.x.

We describe the case of a 20-year-old man who developed an obstructive bronchial reaction accompanied by a maculopapular facial rash 8 h after an aerosol treatment with the mucolytic drug Stepronin. The results of intradermal and patch testing with Stepronin, together with those of bronchial challenge and histologic findings in patch-tested skin, indicate that the patient's reaction involved an accelerated cell-mediated mechanism of hypersensitivity. Bronchial challenges with methacholine demonstrated a transient increase in nonspecific bronchial hyperreactivity.

[A controlled clinical study on the efficacy and tolerability of Stepronin in chronic alcoholic liver diseases]

Clin Ter 1990 Nov 15;135(3):209-13.PMID:2150022doi

A group of 15 hospitalized chronic alcoholics was treated for 30 days with twice daily doses of 840 mg Stepronin and was compared to 15 patients receiving placebo. The favorable results of this treatment are reported together with statistically significant changes of laboratory tests.

[The therapeutic activity of Stepronin in viral hepatitis]

Minerva Med 1982 Oct 27;73(41):2897-904.PMID:6752758doi

The therapeutic effect of Stepronin in 5% glucosate solution has been evaluated in 55/110 viral hepatitis cases (10/55 of A type, 37/55 of B type and 8/55 of nA type nB type), versus other cases (8/55 of A type, 40/55 of B type of 7/55 of nA nB type), treated with 5% glucose solution only. In 18/110 viral hepatitis case of A type, final results with the two different therapies have not shown statistically significantly changes and were comparable. Particularly favourable, in the patients treated, the results obtained in viral hepatitis of B type and nA nB type, were very significant statistically at the end of therapy. In particular, the 2 transaminasic activities had a beneficial influence. Tolerance was very good: only in there cases nettlerash was observed and therapy interrupted in one patient. Therefore the validity of this sulphydryl pro-drug in the treatment of acute viral hepatitis of B and nA and nB type is confirmed.