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Pentoxyverine Sale

(Synonyms: 枸橼酸喷托维林,Carbetapentane) 目录号 : GC61838

Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.

Pentoxyverine Chemical Structure

Cas No.:77-23-6

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10mM (in 1mL DMSO)
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10 mg
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25 mg
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50 mg
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100 mg
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产品描述

Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.

Pentoxyverine (Carbetapentane) Citrate has atropine-like and local anaesthetic actions and effectively suppresses acute cough due to common upper respiratory infections. [1] Pentoxyverine suppresses the cough reflex in the central nervous system, but the exact mechanism of action is not known with certainty. The drug acts as an antagonist at muscarinic receptors (subtype M1) and as an agonist at sigma receptors (subtype σ1). Its anticholinergic properties can theoretically relax the pulmonary alveoli and reduce phlegm production. [2]

[1] D?nmez OA, et al. Talanta, 2011, 83(5), 1601-1605. [2] Brown C, et al. Br J Pharmacol, 2004, 141(2), 233-240.

Chemical Properties

Cas No. 77-23-6 SDF
别名 枸橼酸喷托维林,Carbetapentane
Canonical SMILES O=C(C1(C2=CC=CC=C2)CCCC1)OCCOCCN(CC)CC
分子式 C20H31NO3 分子量 333.47
溶解度 DMSO : 250 mg/mL (749.69 mM) 储存条件 Store at -20°C
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1 mM 2.9988 mL 14.9939 mL 29.9877 mL
5 mM 0.5998 mL 2.9988 mL 5.9975 mL
10 mM 0.2999 mL 1.4994 mL 2.9988 mL
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Research Update

Extraction-free spectrophotometric assay of the antitussive drug Pentoxyverine citrate using sulfonephthalein dyes

Spectrochim Acta A Mol Biomol Spectrosc 2019 Nov 5;222:117186.PMID:31176152DOI:10.1016/j.saa.2019.117186.

Pentoxyverine citrate (PEN-citrate) is an antitussive (cough suppressant) drug used for cough associated with illnesses like common cold. In this work, PEN-citrate is quantified by applying a simple, direct and accurate spectrophotometric method in pure form, pharmaceutical formulation (Cabella®, 2.13 mg/mL) and human serum samples. The formation of a stable yellow ion-pair with sulfonephthalein dyes; bromocresol green (BCG), bromophenol blue (BPB), bromothymol blue (BTB), bromocresol purple (BCP), bromochlorophenol blue (BChPB) and bromoxylenol blue (BXB), in three nonpolar solvents (chloroform, dichloromethane, acetonitrile) is used as the basis for this method. This is the first assay method reported for the quantification of PEN-citrate using the sulfonephthaleins as coloring agents. Diverse parameters were investigated in order to optimize the calibration curve conditions. The strategy was validated with respect to linearity range, precision, accuracy, specificity, robustness and limits of detection (LOD) and quantification (LOQ). In addition, solvents of different polarities were utilized to investigate the color reaction, light absorption and to allow for increasing the method sensitivity. Beer's law is obeyed over a wide concentration range (up to 42.05 μg/mL in case of BTB method). LOD and LOQ values reached 0.22 and 0.72 μg/mL, respectively, upon using BChPB. The relative standard deviation (%RSD) was ≤1.91% while correlation coefficient values (r) were ≥ 0.9974. High molar absorptivity values and low values of Sandell's sensitivity were obtained indicating that the proposed methods are highly sensitive. The validated methods were applied to the analysis of PEN-citrate in the dosage form and human serum samples where the drug was successfully resolved from the pharmaceutical additives and serum components with recoveries ≥98.98%.

[Pentoxyverine poisoning via maternal milk in a fully breast-fed newborn infant]

Dtsch Med Wochenschr 1988 Jun 3;113(22):898-900.PMID:3371222DOI:10.1055/s-2008-1067740.

A four-week-old male infant who had been exclusively breast-fed by his mother developed acute respiratory failure with intermittent arrest of breathing for up to 15 sec, in between sighing breaths and normal ones. For two weeks his mother had been taking pentoxyverine-containing cough drops for an upper respiratory tract infection. Pentoxyverine was demonstrated in maternal serum and breast milk, as well as the child's serum and urine, in some in very high concentrations. The course of the illness and comparison with reported instances of Pentoxyverine poisoning in infants makes it likely that this, too, was such a case.

Comprehensive analysis of lncRNA-miRNA-mRNA regulatory networks for microbiota-mediated colorectal cancer associated with immune cell infiltration

Bioengineered 2021 Dec;12(1):3410-3425.PMID:34227920DOI:10.1080/21655979.2021.1940614.

Recent findings have identified microbiota as crucial participants in many disease conditions, including cancers. Competing endogenous RNA (ceRNA) is regarded as a candidate mechanism involving relevant biological processes. We therefore constructed a ceRNA network using the TCGA and GEO database, to determine the potential mechanisms of microbiota-mediated colorectal carcinogenesis and progression. We found a total of 75 lncRNAs, 8 miRNAs, and 9 mRNAs in the probiotics-mediated ceRNA network and a total of 49 lncRNAs, 4 miRNAs, and 3 mRNA in the pathobiont-mediated ceRNA network, which could induce the microbiota-mediated carcinogenesis and progression. The GO and KEGG analysis indicated that the ceRNA network is mainly enriched in the metabolic process, and two unique pathways (the p53 signaling pathway and microRNA in cancer), respectively. A four-gene signature (FRMD6-AS2, DIRC3, LIFR-AS1, and MRPL23-AS1) was suggested as an independent prognostic factor. Four lncRNAs (LINC00355, KCNQ1OT1, LINC00491, and HOTAIR) were associated with poor survival. Three small molecule candidate anticancer drugs (Pentoxyverine, Rimexolone, and Doxylamine) were identified. A four-gene signature (FAM129A, BCL2, PMAIP1, and RPS6) is significantly correlated with immune infiltration level. This study provides a promising biomarker reservoir to explore the mechanism by which microbiota regulate the ceRNA network involving the immune response, and further participate in colorectal carcinogenesis and progression.

Characterization of Pentoxyverine metabolites in urine using GC/MS after intoxication with Silomat cough drops

Forensic Sci Int 2012 Feb 10;215(1-3):124-35.PMID:21450423DOI:10.1016/j.forsciint.2011.03.002.

A nearly two and a half year old boy was hospitalized after showing symptoms of disorientation and hallucination. The parents remembered the child playing with a bottle of Silomat cough drops, so that an intoxication was taken into consideration. After liquid/liquid extraction of a urine sample collected in hospital, the underivatized and the acetylated extracts were analyzed by gas chromatography-mass spectrometry (GC/MS) using electron ionization (EI) as well as chemical ionization (CI). In the urine sample high amounts of Pentoxyverine (carbetapentane) and several of its metabolites, e.g., different hydrolyzed, desalkylated and ring-hydroxylated products have been identified. The correlation of the results, the observed symptoms, and the access to the Silomat cough drops reveal an intoxication after ingestion of an unknown amount of the antitussive Pentoxyverine. Corresponding EI- and CI-GC/MS spectra are presented characterizing the structure of its metabolites.

[Bioequivalence evaluation of orally disintegrating tablet of Pentoxyverine citrate]

Nan Fang Yi Ke Da Xue Xue Bao 2010 Jul;30(7):1621-3.PMID:20650784doi

Objective: To evaluate the bioequivalence of orally disintegrating tablets of Pentoxyverine citrate (tested preparation) in healthy male volunteers. Methods: A single oral dose of the tested and reference preparations at 25 mg were given to 20 healthy volunteers in a randomized two-period cross-over design. Plasma Pentoxyverine citrate concentrations were determined by HPLC-MS/ESI+ method. The pharmacokinetic parameters were calculated and the bioequivalence of the two preparations were evaluated using DAS program. Results: The Tmax, Cmax, AUC0 15 and AUC0infinity of tested and reference preparations were 1.62-/+0.75 h and 2.52-/+1.21 h, 62.28-/+33.06 microg/L and 59.72-/+33.25 microg/L, 234.44-/+130.01 microg.h.L(-1) and 228.77-/+129.24 microg.h.L(-1), 246.80-/+136.19 microg.h.L(-1) and 244.11-/+140.73 microg.h.L(-1), respectively. The 90% confidence interval of C(max), AUC0 15 and AUC0infinity of tested preparations were 81.4%-138.4%, 86.0%-123.3% and 86.5%-121.2%, respectively. Conclusion: The tested and reference preparations are bioequivalent.