| Size | Price | |
|---|---|---|
| 10g | ||
| 25g | ||
| Other Sizes |
Purity: ≥98%
Pentoxyverine Citrate (Loucarbate; Carbetapentane Citrate), the citrate salt of Pentoxyverine, is an agonist of the sigma-1 receptor and an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. It is sold over-the-counter/OTC in the United States as Solotuss, or in combination with other medications, especially decongestants. One such product is Certuss, a combination of guaifenesin and pentoxyverine.
| ln Vivo |
1. Current antitussive medications have limited efficacy and often contain the opiate-like agent dextromethorphan (DEX). The mechanism whereby DEX inhibits cough is ill defined. DEX displays affinity at both NMDA and sigma receptors, suggesting that the antitussive activity may involve central or peripheral activity at either of these receptors. This study examined and compared the antitussive activity of DEX and various putative sigma receptor agonists in the guinea-pig citric-acid cough model. [2]
2. Intraperitoneal (i.p.) administration of DEX (30 mg kg(-1)) and the sigma-1 agonists SKF-10,047 (1-5 mg kg(-1)), Pre-084 (5 mg kg(-1)), and carbetapentane (1-5 mg kg(-1)) inhibited citric-acid-induced cough in guinea-pigs. Intraperitoneal administration of a sigma-1 antagonist, BD 1047 (1-5 mg kg(-1)), reversed the inhibition of cough elicited by SKF-10,047. In addition, two structurally dissimilar sigma agonists SKF-10,047 (1 mg ml(-1)) and Pre-084 (1 mg ml(-1)) inhibited cough when administered by aerosol. [2] 3. Aerosolized BD 1047 (1 mg ml(-1), 30 min) prevented the antitussive action of SKF-10,047 (5 mg kg(-1)) or DEX (30 mg kg(-1)) given by i.p. administration and, likewise, i.p. administration of BD 1047 (5 mg kg(-1)) prevented the antitussive action of SKF-10,047 given by aerosol (1 mg ml(-1)).[2] 4. These results therefore support the argument that antitussive effects of DEX may be mediated via sigma receptors, since both systemic and aerosol administration of sigma-1 receptor agonists inhibit citric-acid-induced cough in guinea-pigs. While significant systemic exposure is possible with aerosol administration, the very low doses administered (estimated <0.3 mg kg(-1)) suggest that there may be a peripheral component to the antitussive effect.[2] |
|---|---|
| Animal Protocol |
For i.p. administration, animals were injected with the compounds carbetapentane, SKF-10,047, DEX or PRE 084 (1–30 mg kg−1), 30 min prior to citric acid. In an attempt to investigate the potential peripheral action of the sigma agonists, we administered these agonists by aerosol in addition to systemic administration. For aerosol exposure, the compounds were aerosolized via whole-body exposure using an ultrasonic nebulizer for 30 min prior to citric acid exposure. The inhaled dose of sigma agonists SKF-10,047 and 2-(4-morpholinethyl) 1-phenylcyclohaxanecarboxylate hydrochloride (Pre-084; 1 mgml−1) in this study was estimated to be <0.3 mg kg−1,. For reversal studies, N-(2-(3,4-dichlorophenyl)ethyl)-N-methyl-2-)dimethylamino ethylamine (BD 1047) (a reported sigma-1 antagonist with 10-fold selectivity for the sigma-1 receptor over the sigma-2 receptor, or saline vehicle, was administered, by either aerosol or i.p. route, 30 min prior to agonist administration.[2]
The eligible animals were randomly assigned to eleven groups and orally administered, including control group (distilled water), positive group (aminophylline/125 mg/kg, pentoxyverine/50 mg/kg, or ammonium chloride/1000 mg/kg for antiasthmatic, antitussive, or expectorant experiment, resp.), and the water extract groups (low, medium, and high doses). In the tests, administrated dose were 2.7, 5.4, and 10.8 g/kg for guinea pigs and 4.4, 8.8, and 17.6 g/kg for mice (expressed as being equal to the weight of crude material per body weight), which were calculated by coefficient commutation of somatotypes and yield of extract (the used dosage was the medium dose, being five times by clinical dosage of 15 g crude herb in adults). After treatment for 5–7 days, activities were tested and evaluated.[5] |
| References |
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| Additional Infomation |
Carbetapentane citrate is a carbonyl compound.
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| Molecular Formula |
C20H31NO3.C6H8O7
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|---|---|---|
| Molecular Weight |
525.59
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|
| Exact Mass |
525.257
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|
| CAS # |
23142-01-0
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| Related CAS # |
Pentoxyverine;77-23-6
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| PubChem CID |
90010
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| Appearance |
White to off-white solid powder
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| Boiling Point |
435.5ºC at 760mmHg
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| Melting Point |
84-86?C
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| Flash Point |
217.2ºC
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| LogP |
2.151
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
37
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| Complexity |
583
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AKJDEXBCRLOVTH-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[2-(Diethylamino)ethoxy]ethyl 1-phenylcyclopentane-1-carboxylate citrate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL | |
| 5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | |
| 10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02183649 | Completed | Drug: pentoxyverine citrate Drug: Placebo |
Healthy | Boehringer Ingelheim | November 2009 | Phase 1 |
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