Piperoxan hydrochloride (Benodaine hydrochloride)
(Synonyms: 盐酸哌罗克生; Benodaine hydrochloride) 目录号 : GC31782An α2-adrenergic receptor antagonist
Cas No.:135-87-5
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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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. |
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)
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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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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% DMSO % % Tween 80 % saline | ||||||||||
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