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

Pentoxyverine  (Synonyms: Carbetapentane)

Cat. No.: HY-134004 Purity: 98.91%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Pentoxyverine Chemical Structure

Pentoxyverine Chemical Structure

CAS No. : 77-23-6

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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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)

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
10 mM 0.2999 mL 1.4994 mL 2.9988 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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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.

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Pentoxyverine
Cat. No.:
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