Piperoxan hydrochloride (Benodaine hydrochloride)

An α2-adrenergic receptor antagonist

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2mg

￥812.00

650.00

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5mg

￥1625.00

1300.00

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10mg

￥2725.00

2180.00

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25mg

￥3775.00

3020.00

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50mg

￥4850.00

3880.00

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100mg

￥5937.00

4750.00

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Background

Piperoxan is an α₂-adrenergic receptor (α₂-AR) antagonist (K_is = 5.4, 2, and 1.3 nM for α_2A-, α_2B-, and α_2C-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)

Protocol

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.

参考文献:

[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.