2. Neuronal Signaling GPCR/G Protein
  3. Sigma Receptor mAChR
  4. Pentoxyverine

Pentoxyverine  (Synonyms: Carbetapentane)

Cat. No.: HY-134004 Purity: 98.91%
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Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.

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Pentoxyverine Chemical Structure

Pentoxyverine Chemical Structure

CAS No. : 77-23-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Pentoxyverine:

Pentoxyverine Related Antibodies

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Description

Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].

IC50 & Target[1]

σ1

41 nM (Ki)

σ2

894 nM (Ki)

In Vivo

Pentoxyverine (Carbetapentane; 1-32 mg/kg; SC) dose-dependently potentiates the sensitizing effect of capsaicin to the mechanical stimulus when the mice were stimulated in the paw injected with Capsaicin (HY-10448)[4].
Pentoxyverine (16 mg/kg; SC) shows strong potentiation of Capsaicin-induced secondary mechanical allodynia[4].
Pentoxyverine (50 mg/kg; orally; ), used for positive control, increases the percentage of the aqueous ammonia-induced latent period of cough by 121.72%, inhibits cough frequency by 45.45% after administration for 7 days in mice of either sex (22-25 g)[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female wild-type weighing 25 to 30 g[4]
Dosage: 0.5, 1, 2, 4, 8, 16, 32 mg/kg
Administration: SC; 30 min before the intraplantar (i.pl.) administration of capsaicin (0.125 μg)
Result: Dose-dependently potentiated the sensitizing effect of capsaicin to the mechanical stimulus when the mice were stimulated in the paw injected with capsaicin.
Clinical Trial
Molecular Weight

333.47

Formula

C20H31NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1(C2=CC=CC=C2)CCCC1)OCCOCCN(CC)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (749.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9988 mL 14.9939 mL 29.9877 mL
5 mM 0.5998 mL 2.9988 mL 5.9975 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9988 mL 14.9939 mL 29.9877 mL 74.9693 mL
5 mM 0.5998 mL 2.9988 mL 5.9975 mL 14.9939 mL
10 mM 0.2999 mL 1.4994 mL 2.9988 mL 7.4969 mL
15 mM 0.1999 mL 0.9996 mL 1.9992 mL 4.9980 mL
20 mM 0.1499 mL 0.7497 mL 1.4994 mL 3.7485 mL
25 mM 0.1200 mL 0.5998 mL 1.1995 mL 2.9988 mL
30 mM 0.1000 mL 0.4998 mL 0.9996 mL 2.4990 mL
40 mM 0.0750 mL 0.3748 mL 0.7497 mL 1.8742 mL
50 mM 0.0600 mL 0.2999 mL 0.5998 mL 1.4994 mL
60 mM 0.0500 mL 0.2499 mL 0.4998 mL 1.2495 mL
80 mM 0.0375 mL 0.1874 mL 0.3748 mL 0.9371 mL
100 mM 0.0300 mL 0.1499 mL 0.2999 mL 0.7497 mL
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Pentoxyverine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pentoxyverine77-23-6CarbetapentaneSigma ReceptormAChRMuscarinic acetylcholine receptorsigma-1 receptorσ1σ2muscarinicantitussiveanticonvulsantspasmolyticbronchial interceptorcough reflexbronchial smooth muscle relaxationairway resistanceInhibitorinhibitorinhibit

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