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Pentoxyverine Citrate

CAS# 23142-01-0

Pentoxyverine Citrate

2D Structure

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Pentoxyverine Citrate

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Chemical Properties of Pentoxyverine Citrate

Cas No. 23142-01-0 SDF Download SDF
PubChem ID 90010 Appearance Powder
Formula C26H39NO10 M.Wt 525.59
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Pentoxyverine citrate
Solubility Soluble to 75 mM in DMSO
Chemical Name 2-[2-(diethylamino)ethoxy]ethyl 1-phenylcyclopentane-1-carboxylate;2-hydroxypropane-1,2,3-tricarboxylic acid
SMILES CCN(CC)CCOCCOC(=O)C1(CCCC1)C2=CC=CC=C2.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Standard InChIKey AKJDEXBCRLOVTH-UHFFFAOYSA-N
Standard InChI InChI=1S/C20H31NO3.C6H8O7/c1-3-21(4-2)14-15-23-16-17-24-19(22)20(12-8-9-13-20)18-10-6-5-7-11-18;7-3(8)1-6(13,5(11)12)2-4(9)10/h5-7,10-11H,3-4,8-9,12-17H2,1-2H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Pentoxyverine Citrate

DescriptionA selective ligand for the σ1 -site.

Pentoxyverine Citrate Dilution Calculator

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Pentoxyverine Citrate Molarity Calculator

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Preparing Stock Solutions of Pentoxyverine Citrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9026 mL 9.5131 mL 19.0262 mL 38.0525 mL 47.5656 mL
5 mM 0.3805 mL 1.9026 mL 3.8052 mL 7.6105 mL 9.5131 mL
10 mM 0.1903 mL 0.9513 mL 1.9026 mL 3.8052 mL 4.7566 mL
50 mM 0.0381 mL 0.1903 mL 0.3805 mL 0.761 mL 0.9513 mL
100 mM 0.019 mL 0.0951 mL 0.1903 mL 0.3805 mL 0.4757 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Pentoxyverine Citrate

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

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References on Pentoxyverine Citrate

A sensitive liquid chromatography-electrospray ionization-mass spectrometry method for the simultaneous determination of pentoxyverine citrate and guaifenesin in human plasma---application to pharmacokinetic and bioequivalence studies.[Pubmed:19634120]

Biomed Chromatogr. 2010 Apr;24(4):351-7.

A sensitive and specific liquid chromatography-electrospray ionization-mass spectrometry method for the identification and quantification of Pentoxyverine Citrate and guaifenesin in human plasma has been developed. After extraction from plasma samples by ethyl acetate, the internal standard and analytes were separated by high-performance liquid chromatographic on a Shim-pack VP-ODS C(18) column (150 x 2.0 mm) using a mobile phase consisting of A (methanol) and B (0.4% glacial acetic acid and 4 mmol/L ammonium acetate) (A:B, 43 : 57). Analysis was performed on a Shimadzu LC/MS-2010A in selected ion monitoring mode with a positive electrospray ionization interface. The method was linear in the concentration range of 1.0-640.0 ng/mL for Pentoxyverine Citrate and 0.025-6.4 microg/mL for guaifenesin. The inter- and intra- precision were all within 12% and accuracy ranged from 85 to 115%.The lower limits of quantification were 1.0 ng/mL for Pentoxyverine Citrate and 25.0 ng/mL for guaifenesin. The extraction recovery was on average 81.95% for Pentoxyverine Citrate and 89.03% for guaifenesin. This is the first assay method reported for the simultaneous determination of Pentoxyverine Citrate and guaifenesin in plasma using one chromatographic run.

[Bioequivalence evaluation of orally disintegrating tablet of pentoxyverine citrate].[Pubmed:20650784]

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

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.

Flow injection chemiluminescence method for the determination of pentoxyverine citrate based on NCS-dichlorofluorescein post-chemiluminescence reaction.[Pubmed:19155187]

Spectrochim Acta A Mol Biomol Spectrosc. 2009 May;72(4):858-62.

A post-chemiluminescence (PCL) phenomenon was observed when Pentoxyverine Citrate solution was injected into the reaction mixture after the finish of chemiluminescence (CL) reaction of N-chlorosuccinimide (NCS) and alkaline dichlorofluorescein. The possible reaction mechanism was proposed based on the studies of the CL kinetic characteristics, the CL spectra and the fluorescence spectra of some related substances. Based on the PCL reaction, a rapid and sensitive method for the determination of Pentoxyverine Citrate was established. The linear response range of this method was from 6.0x10(-9) to 1.0x10(-6)gmL(-1) with a linear correlation coefficient of 0.9998. The relative standard deviation for 2.0x10(-8)gmL(-1) Pentoxyverine Citrate was 2.1% (n=11). The detection limit was 9x10(-10)gmL(-1). This method has been applied to the determination of Pentoxyverine Citrate in human plasma and pharmaceutical samples with the satisfactory results.

[Quantification of pentoxyverine citrate in human plasma by LC-ESI/MS method and its application].[Pubmed:21351477]

Yao Xue Xue Bao. 2009 Dec;44(12):1402-5.

A rapid and sensitive liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI/ MS) method for quantification of Pentoxyverine Citrate in human plasma has been developed and applied for the bioequivalence and pharmacokinetics study. After extracted from plasma samples with ethyl acetate, analysis was performed in selected ion monitoring (SIM) mode with a positive electrospray ionization (ESI) interface with a mobile phase consisted of methanol and water (0.4% glacial acetic acid and 4 mmol x L(-1) ammonium acetate, 43 : 57, v/v). The linear concentration range of the calibration curves was 1.0-160.0 ng x mL(-1) for Pentoxyverine Citrate, inter- and intra-precision (RSD) was less than 12.5%, accuracy (RE) was in +/- 13.5% and absolute recovery was more than 80%. The method was proved simple, rapid, sensitive, specific and suitable for pharmacokinetic and bioequivalence study of Yufenweilin capsule containing Pentoxyverine Citrate.

Labeling by [3H]1,3-di(2-tolyl)guanidine of two high affinity binding sites in guinea pig brain: evidence for allosteric regulation by calcium channel antagonists and pseudoallosteric modulation by sigma ligands.[Pubmed:1847495]

Mol Pharmacol. 1991 Feb;39(2):222-32.

Equilibrium binding studies with the sigma receptor ligand [3H]1,3-di(2-tolyl)guanidine ([3H]DTG) demonstrated two high affinity binding sites in membranes prepared from guinea pig brain. The apparent Kd values of DTG for sites 1 and 2 were 11.9 and 37.6 nM, respectively. The corresponding Bmax values were 1045 and 1423 fmol/mg of protein. Site 1 had high affinity for (+)-pentazocine, haloperidol, (R)-(+)-PPP, carbepentane, and other sigma ligands, suggesting a similarity with the dextromethorphan/sigma 1 binding site described by Musacchio et al. [Life Sci. 45:1721-1732 (1989)]. Site 2 had high affinity for DTG and haloperidol (Ki = 36.1 nM) and low affinity for most other sigma ligands. Kinetic experiments demonstrated that [3H]DTG dissociated in a biphasic manner from both site 1 and site 2. DTG and haloperidol increased the dissociation rate of [3H]DTG from site 1 and site 2, demonstrating the presence of pseudoallosteric interactions. Inorganic calcium channel blockers such as Cd2+ selectively increased the dissociation rate of [3H]DTG from site 2, suggesting an association of this binding site with calcium channels.

Description

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

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