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Piperoxan hydrochloride (Benodaine hydrochloride) Sale

(Synonyms: 盐酸哌罗克生; Benodaine hydrochloride) 目录号 : GC31782

An α2-adrenergic receptor antagonist

Piperoxan hydrochloride (Benodaine hydrochloride) Chemical Structure

Cas No.:135-87-5

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10mM (in 1mL DMSO)
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2mg
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5mg
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10mg
¥2,250.00
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25mg
¥3,150.00
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50mg
¥4,050.00
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100mg
¥4,950.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

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].

Animal experiment:

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.

References:

[1]. Viemari JC, et al. Nasal trigeminal inputs release the A5 inhibition received by the respiratory rhythm generator of the mouse neonate. J Neurophysiol. 2004 Feb;91(2):746-58.
[2]. Bentley GA, et al. The antinociceptive action of some beta-adrenoceptor agonists in mice. Br J Pharmacol. 1986 Jul;88(3):515-21.

产品描述

Piperoxan is an α2-adrenergic receptor (α2-AR) antagonist (Kis = 5.4, 2, and 1.3 nM for α2A-, α2B-, and α2C-ARs, respectively) and a first generation histamine receptor antagonist.1,2 It reverses decreases in systolic blood pressure induced by clonidine in spontaneously hypertensive rats when administered at a dose of 10 mg/kg.3

1.Blaxall, H.S., Murphy, T.J., Baker, J.C., et al.Characterization of the alpha-2C adrenergic receptor subtype in the opossum kidney and in the OK cell lineJ. Pharmacol. Exp. Ther.259(1)323-329(1991) 2.Parsons, M.E., and Ganellin, C.R.Histamine and its receptorsBr. J. Pharmacol.147(Suppl. 1)S127-S135(2006) 3.Robson, R.D., Antonaccio, M.J., Saelens, J.K., et al.Antagonism by mianserin and classical α-adrenoceptor blocking drugs of some cardiovascular and behavioral effects of clonidineEur. J. Pharmacol.47(4)431-442(1978)

Chemical Properties

Cas No. 135-87-5 SDF
别名 盐酸哌罗克生; Benodaine hydrochloride
Canonical SMILES [H]Cl.N1(CC2OC3=CC=CC=C3OC2)CCCCC1
分子式 C14H20ClNO2 分子量 269.77
溶解度 DMSO : ≥ 31 mg/mL (114.91 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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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
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Research Update

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Lack of specificity of piperoxan hydrochloride test for adrenal medullary tumors

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Effect of piperoxane hydrochloride (benodaine) on the hypertension accompanying Cushing's syndrome

Piperoxan hydrochloride (benzodioxan) test; report of a false positive reaction