1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Piperoxan hydrochloride

Piperoxan hydrochloride  (Synonyms: Benodaine hydrochloride)

Cat. No.: HY-100850 Purity: 99.66%
COA Handling Instructions

Piperoxan (Benodaine) hydrochloride is an α2 adrenoceptor antagonist. Piperoxan hydrochloride is the first-generation antihistamine.

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

Piperoxan hydrochloride Chemical Structure

Piperoxan hydrochloride Chemical Structure

CAS No. : 135-87-5

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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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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Piperoxan (Benodaine) hydrochloride is an α2 adrenoceptor antagonist. Piperoxan hydrochloride is the first-generation antihistamine.

IC50 & Target

adrenoceptor[1]

In Vitro

When the medulla is superfused with α2 adrenoceptor antagonist Piperoxane (50 μM; 5 min) while the pons is with artificial cerebrospinal fluid (ACSF), the three inactive preparations display rhythmic phrenic bursts at a low frequency (2-4 c/min), and the phrenic burst frequency of the 12 active ones significantly increases during the last 3 min of Piperoxane applications (163±12% of the previous mean frequency). In active medullary preparations, the effects of NA applications (25 μM; 5 min) are compared when the preparations sre superfused either by ACSF (n=8) or by the α2 adrenoceptor antagonist Piperoxane (50 μM; PIP-ACSF; n=5). NA applications either alone (NA-ACSF) or with Piperoxane (PIP-ACSF+NA) significantly increases the phrenic burst frequency. However, the blockage of the medullary α2 adrenoceptors by Piperoxane potentiates a phrenic burst frequency increase: during the fifth minute of NA applications, the phrenic burst frequency reached 171±11% of the mean control value when ACSF is applied alone and 234±21% of the mean control value when PIP-ACSF is applied in control condition[1].

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

Molecular Weight

269.77

Formula

C14H20ClNO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.N1(CC2OC3=CC=CC=C3OC2)CCCCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (185.34 mM; Need ultrasonic)

DMSO : ≥ 31 mg/mL (114.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7069 mL 18.5343 mL 37.0686 mL
5 mM 0.7414 mL 3.7069 mL 7.4137 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 25 mg/mL (92.67 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
References
Kinase Assay
[1]

The mouse neonates (P0-P3) are ether-anesthetized and decerebrated; the brain stems and the cervical spinal cords are dissected out and placed ventral sides up in a 2 mL chamber superfused with artificial cerebrospinal fluid (ACSF) at 27±0.25°C (mean±SD), renewed at a rate of 2 mL/min. The ACSF [containing (in mM) 129 NaCl, 3.35 KCl, 1.26 CaCl2, 1.15 MgCl2, 21 NaHCO3, 0.58 NaH2PO4, and 30 glucose] is oxygenated and equilibrated (pH 7.4 at 27°C) by bubbling carbogene (95% O2-5% CO2). In the pharmacological experiments, this is replaced by another ACSF in which bioreactive substances are dissolved: noradrenaline at 25 μM (NA-ACSF) or α2 adrenoceptor antagonists, either Piperoxane at 50 μM (PIP-ACSF) or yohimbine at 50 μM (YO-ACSF). In some of the experiments, a patch-clamp microelectrode (1 μm diameter tip) is lowered within the ventral pons into the A5 nucleus where a solution of either ACSF or NA (1 mM) is pressure-ejected. The ejected volume is estimated 20 nL for a pressure pulse lasting 2 s[1].

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

Animal Administration
[2]

Mice[2]
Male Balb-C mice are used, weighing between 20 and 25 g. In mice pretreated with the α-adrenoceptor antagonist Piperoxan, or with naloxone, both at a dose of 3×10-5 mol /kg s.c. given 15 min before the acetic acid, the antinociceptive action of (-)-isoprenaline is only slightly antagonized. Dose-ratios of 1.45 and 1.7, are produced by these two antagonists.

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

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 (sealed storage, away from moisture). 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 / H2O 1 mM 3.7069 mL 18.5343 mL 37.0686 mL 92.6715 mL
5 mM 0.7414 mL 3.7069 mL 7.4137 mL 18.5343 mL
10 mM 0.3707 mL 1.8534 mL 3.7069 mL 9.2672 mL
15 mM 0.2471 mL 1.2356 mL 2.4712 mL 6.1781 mL
20 mM 0.1853 mL 0.9267 mL 1.8534 mL 4.6336 mL
25 mM 0.1483 mL 0.7414 mL 1.4827 mL 3.7069 mL
30 mM 0.1236 mL 0.6178 mL 1.2356 mL 3.0891 mL
40 mM 0.0927 mL 0.4634 mL 0.9267 mL 2.3168 mL
50 mM 0.0741 mL 0.3707 mL 0.7414 mL 1.8534 mL
60 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5445 mL
80 mM 0.0463 mL 0.2317 mL 0.4634 mL 1.1584 mL
100 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9267 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Piperoxan hydrochloride Related Classifications

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    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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Piperoxan hydrochloride
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