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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Piperoxan hydrochloride(also known as Piperoxan HCl, or benodaine) is a novel, selective and potent α2 adrenoceptor antagonist. Moreover, it was the original antihistamine.
Targets |
α2 adrenoceptor
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ln Vitro |
In the event that the medulla is superfused with α2 adrenoceptor antagonist Piperoxane (50 μM; 5 min) and the pons is filled with artificial cerebrospinal fluid (ACSF), three inactive preparations exhibit rhythmic phrenic bursts at a low frequency (2-4 c/min). Meanwhile, the phrenic burst frequency of the twelve active preparations increases significantly during the final 3 min of Piperoxane applications (163±12% of the preceding mean frequency). When the preparations are superfused with either ACSF (n = 8) or the α2 adrenoceptor antagonist Piperoxane (50 μM; PIP-ACSF; n = 5), the effects of NA applications (25 μM; 5 min) are compared. The frequency of phrenic bursts is greatly increased by applying NA, either by itself (NA-ACSF) or in combination with Piperoxane (PIP-ACSF+NA). But piperoxane potentiates a phrenic burst frequency increase by blocking medullary α2 adrenoceptors. In the fifth minute of NA applications, the phrenic burst frequency increased to 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].
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Cell Assay |
The brain stems and cervical spinal cords of the mouse neonates (P0-P3) are removed 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 mice are then given ether anesthesia and decerebrated. By bubbling carbogene (95% O2-5% CO2), the ACSF, which contains (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). In the pharmaceutical tests, this is swapped out for an additional ACSF containing bioreactive materials: either α2 adrenoceptor antagonists, such as piperoxane at 50 μM (PIP-ACSF) or yohimbine at 50 μM (YO-ACSF), or noradrenaline at 25 μM (NA-ACSF). In certain experiments, a solution of either ACSF or NA (1 mM) is pressure-expelled from the A5 nucleus after a patch-clamp microelectrode with a diameter of 1 μm is lowered into the ventral pons. For a two-second pressure pulse, the estimated ejected volume is 20 nL[1].
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Animal Protocol |
Mice: The mice used are male Balb-C mice that weigh 20–25 g. Only slightly opposes the antinociceptive effect of (-)-isoprenaline in mice pretreated with the α-adrenoceptor antagonist Piperoxan or naloxone, both at a dose of 3×10-5 mol /kg s.c. given 15 min before the acetic acid. The antagonists in question yield dose-ratios of 1.45 and 1.7.
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References |
Molecular Formula |
C14H20CLNO2
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Molecular Weight |
269.769
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Exact Mass |
269.12
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Elemental Analysis |
C, 62.33; H, 7.47; Cl, 13.14; N, 5.19; O, 11.86
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CAS # |
135-87-5
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Related CAS # |
59-39-2; 135-87-5 (HCl)
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Appearance |
Solid powder
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SMILES |
C1CCN(CC1)CC2COC3=CC=CC=C3O2.Cl
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InChi Key |
BITRJBQGQMGGQI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H19NO2.ClH/c1-4-8-15(9-5-1)10-12-11-16-13-6-2-3-7-14(13)17-12;/h2-3,6-7,12H,1,4-5,8-11H2;1H
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Chemical Name |
1-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)piperidine;hydrochloride
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Synonyms |
F 933 hydrochloride; Piperoxan HCl; benodaine; Piperoxane hydrochloride; F933; F-933
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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. |
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) |
DMSO: ~54 mg/mL (~200.2 mM)
Water: ~54 mg/mL Ethanol: ~40 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (92.67 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 | |
10 mM | 0.3707 mL | 1.8534 mL | 3.7069 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.